Literature for peptidase S29.001: hepacivirin

Summary Alignment Tree Sequences Sequence features Distribution Structure Literature Substrates Pharma

(Topics flags: S Structure, A Assay, T Target, P Specificity, E Expression, V Review, M Mutation, I Inhibitor, L Localization. To select only the references relevant to a single topic, click the link above. See explanation.)

    2025
  1. Sarwar,S. and Randall,G.
    HCV NS3/4A protease relocalizes CCTalpha to viral replication sites, enhancing phosphatidylcholine synthesis and viral replication
    Proc Natl Acad Sci U S A122, e2419632122-e2419632122. PubMed  Europe PubMed DOI
  2. 2024
  3. Janin,Y.L.
    On the origins of SARS-CoV-2 main protease inhibitors
    RSC Med Chem15, 81-118. PubMed  Europe PubMed DOI  V  I
  4. Shahab,M., Khan,A., Khan,S.A. and Zheng,G.
    Unraveling the mechanisms of Sofosbuvir resistance in HCV NS3/4A protease: Structural and molecular simulation-based insights
    Int J Biol Macromol267, 131629-131629. PubMed  Europe PubMed DOI
  5. 2023
  6. Ohta,K., Ito,M., Chida,T., Nakashima,K., Sakai,S., Kanegae,Y., Kawasaki,H., Aoshima,T., Takabayashi,S., Takahashi,H., Kawata,K., Shoji,I., Sawasaki,T., Suda,T. and Suzuki,T.
    Role of hepcidin upregulation and proteolytic cleavage of ferroportin 1 in hepatitis C virus-induced iron accumulation
    PLoS Pathog19, e1011591-e1011591. PubMed  Europe PubMed DOI
  7. Samantaray,M., Pattabiraman,R., Murthy,T.P.K., Ramaswamy,A., Murahari,M., Krishna,S. and Kumar,S.B.
    Structure-based virtual screening of natural compounds against wild and mutant (R1155K, A1156T and D1168A) NS3-4A protease of Hepatitis C virus
    J Biomol Struct Dyn1-18. PubMed  Europe PubMed DOI
  8. 2022
  9. Chuang,C.H., Cheng,T.L., Chen,W.C., Huang,Y.J., Wang,H.E., Lo,Y.C., Hsieh,Y.C., Lin,W.W., Hsieh,Y.J., Ke,C.C., Huang,K.C., Lee,J.C. and Huang,M.Y.
    Micro-PET imaging of hepatitis C virus NS3/4A protease activity using a protease-activatable retention probe
    Front Microbiol13, 896588-896588. PubMed  Europe PubMed DOI
  10. Isken,O., Pham,M.T., Schwanke,H., Schlotthauer,F., Bartenschlager,R. and Tautz,N.
    Characterization of a multipurpose NS3 surface patch coordinating HCV replicase assembly and virion morphogenesis
    PLoS Pathog18, e1010895-e1010895. PubMed  Europe PubMed DOI
  11. Khan,M., Rauf,W., Habib,F.E., Rahman,M., Iqbal,S., Shehzad,A. and Iqbal,M.
    Hesperidin identified from Citrus extracts potently inhibits HCV genotype 3a NS3 protease
    BMC Complement Med Ther22, 98-98. PubMed  Europe PubMed DOI
  12. Majerova,T. and Konvalinka,J.
    Viral proteases as therapeutic targets
    Mol Aspects Med88, 101159-101159. PubMed  Europe PubMed DOI  V  I
  13. 2021
  14. Dultz,G., Srikakulam,S.K., Konetschnik,M., Shimakami,T., Doncheva,N.T., Dietz,J., Sarrazin,C., Biondi,R.M., Zeuzem,S., Tampe,R., Kalinina,O.V. and Welsch,C.
    Epistatic interactions promote persistence of NS3-Q80K in HCV infection by compensating for protein folding instability
    J Biol Chem101031-101031. PubMed  Europe PubMed DOI
  15. Kang,X., Chen,X., He,Y., Guo,D., Guo,L., Zhong,J. and Shu,H.B.
    Corrigendum to "DDB1 is a cellular substrate of NS3/4A protease and required for hepatitis C virus replication" [Virology 435 (2013) 385-394]
    Virology PubMed  Europe PubMed DOI
  16. 2020
  17. Chiang,C.H., Lai,Y.L., Huang,Y.N., Yu,C.C., Lu,C.C., Yu,G.Y. and Yu,M.J.
    Sequential phosphorylation of the HCV NS5A protein depends on NS3-mediated auto-cleavage between NS3 and NS4A
    J Virol PubMed  Europe PubMed DOI
  18. Chung,H.K. and Lin,M.Z.
    On the cutting edge: protease-based methods for sensing and controlling cell biology
    Nat Methods PubMed  Europe PubMed DOI  V
  19. Dultz,G., Shimakami,T., Schneider,M., Murai,K., Yamane,D., Marion,A., Zeitler,T.M., Stross,C., Grimm,C., Richter,R.M., Baumer,K., Yi,M., Biondi,R.M., Zeuzem,S., Tampe,R., Antes,I., Lange,C.M. and Welsch,C.
    Extended interaction networks with HCV protease NS3-4A substrates explain the lack of adaptive capability against protease inhibitors
    J Biol Chem PubMed  Europe PubMed DOI
  20. El-Araby,M.E., Omar,A.M., Soror,S.H., Arold,S.T., Khayat,M.T., Asfour,H.Z., Bamane,F. and Elfaky,M.A.
    Synthetic bulky NS4A peptide variants bind to and inhibit HCV NS3 protease
    J Adv Res24, 251-259. PubMed  Europe PubMed DOI  I
  21. Matthew,A.N., Zephyr,J., Nageswara Rao,D., Henes,M., Kamran,W., Kosovrasti,K., Hedger,A.K., Lockbaum,G.J., Timm,J., Ali,A., Kurt Yilmaz,N. and Schiffer,C.A.
    Avoiding drug resistance by substrate envelope-guided design: toward potent and robust HCV NS3/4A protease inhibitors
    MBio11, PubMed  Europe PubMed DOI  I
  22. Omar,A.M., Elfaky,M.A., Arold,S.T., Soror,S.H., Khayat,M.T., Asfour,H.Z., Bamane,F.H. and El-Araby,M.E.
    1H-Imidazole-2,5-dicarboxamides as NS4A peptidomimetics: identification of a new approach to inhibit HCV-NS3 protease
    Biomolecules10, PubMed  Europe PubMed DOI  I
  23. Popielec,A., Ostrowska,N., Wojciechowska,M., Feig,M. and Trylska,J.
    Crowded environment affects the activity and inhibition of the NS3/4A protease
    Biochimie176, 169-180. PubMed  Europe PubMed DOI
  24. Sakhor,W., Teoh,T.C., Yusof,R., Lim,S.K. and Razif,M.F.M.
    Discovery of small molecule inhibitors against the NS3/4A serine protease of Hepatitis C virus genotype 3 via highthroughput virtual screening and in vitro evaluations
    Trop Biomed37, 609-625. PubMed  Europe PubMed DOI
  25. Sun,L.Q., Mull,E., D'Andrea,S., Zheng,B., Hiebert,S., Gillis,E., Bowsher,M., Kandhasamy,S., Baratam,V.R., Puttaswamy,S., Pulicharla,N., Vishwakrishnan,S., Reddy,S., Trivedi,R., Sinha,S., Sivaprasad,S., Rao,A., Desai,S., Ghosh,K., Anumula,R., Kumar,A., Rajamani,R., Wang,Y.K., Fang,H., Mathur,A., Rampulla,R., Zvyaga,T.A., Mosure,K., Jenkins,S., Falk,P., Tagore,D.M., Chen,C., Rendunchintala,K., Loy,J., Meanwell,N.A., McPhee,F. and Scola,P.M.
    Discovery of BMS-986144, a Third-Generation, Pan-Genotype NS3/4A Protease Inhibitor for the Treatment of Hepatitis C Virus Infection
    J Med Chem63, 14740-14760. PubMed  Europe PubMed DOI  I
  26. Tallorin,L., Villareal,V.A., Hsia,C.Y., Rodgers,M.A., Burri,D.J., Pfeil,M.P., Llopis,P.M., Lindenbach,B.D. and Yang,P.L.
    Hepatitis C virus NS3-4A protease regulates the lipid environment for RNA replication by cleaving host enzyme 24-dehydrocholesterol reductase
    J Biol Chem295, 12426-12436. PubMed  Europe PubMed DOI
  27. Tran,H.T.L., Morikawa,K., Anggakusuma, Zibi,R., Thi,V.L.D., Penin,F., Heim,M.H., Quadroni,M., Pietschmann,T., Gouttenoire,J. and Moradpour,D.
    OCIAD1 is a host mitochondrial substrate of the hepatitis C virus NS3-4A protease
    PLoS ONE15, e0236447-e0236447. PubMed  Europe PubMed DOI
  28. Wei,Y., Yang,J., Kishore Sakharkar,M., Wang,X., Liu,Q., Du,J. and Zhang,J.J.
    Evaluating the inhibitory effect of eight compounds from Daphne papyracea against the NS3/4A protease of hepatitis C virus
    Nat Prod Res34, 1607-1610. PubMed  Europe PubMed DOI  I
  29. Wypych,R.M., LaPlante,S.R., White,P.W. and Martin,S.F.
    Structure-thermodynamics-relationships of hepatitis C viral NS3 protease inhibitors
    Eur J Med Chem192, 112195-112195. PubMed  Europe PubMed DOI  I
  30. Xu,L., Yu,D., Yao,Y.L., Gu,T., Zheng,X., Wu,Y., Luo,R.H., Zheng,Y.T., Zhong,J. and Yao,Y.G.
    Tupaia MAVS Is a Dual Target during Hepatitis C Virus Infection for Innate Immune Evasion and Viral Replication via NF-kappaB
    J Immunol205, 2091-2099. PubMed  Europe PubMed DOI
  31. 2019
  32. Ezat,A.A., Elfiky,A.A., Elshemey,W.M. and Saleh,N.A.
    Novel inhibitors against wild-type and mutated HCV NS3 serine protease: an in silico study
    Virusdisease30, 207-213. PubMed  Europe PubMed DOI  I
  33. Hawas,U.W., Abou El-Kassem,L.T., Shaher,F. and Al-Farawati,R.
    In vitro inhibition of hepatitis C virus protease and antioxidant by flavonoid glycosides from the Saudi costal plant Sarcocornia fruticosa
    Nat Prod Res33, 3364-3371. PubMed  Europe PubMed DOI  I
  34. Jensen,S.B., Fahnoe,U., Pham,L.V., Serre,S.B.N., Tang,Q., Ghanem,L., Pedersen,M.S., Ramirez,S., Humes,D., Pihl,A.F., Filskov,J., Solund,C.S., Dietz,J., Fourati,S., Pawlotsky,J.M., Sarrazin,C., Weis,N., Schonning,K., Krarup,H., Bukh,J. and Gottwein,J.M.
    Evolutionary pathways to persistence of highly fit and resistant hepatitis C virus protease inhibitor escape variants
    Hepatology70, 771-787. PubMed  Europe PubMed DOI  I
  35. Kammarabutr,J., Mahalapbutr,P., Nutho,B., Kungwan,N. and Rungrotmongkol,T.
    Low susceptibility of asunaprevir towards R155K and D168A point mutations in HCV NS3/4A protease: a molecular dynamics simulation
    J Mol Graph Model89, 122-130. PubMed  Europe PubMed DOI  I
  36. Mayberry,J. and Lee,W.M.
    The revolution in treatment of hepatitis C
    Med Clin North Am103, 43-55. PubMed  Europe PubMed DOI  I
  37. Naguib,M.M., Mohamed,M.R., M Ali,M.A. and Karim,A.M.
    Development of an efficient in vivo cell-based assay system for monitoring hepatitis C virus genotype 4a NS3/4A protease activity
    Indian J Pathol Microbiol62, 391-398. PubMed  Europe PubMed DOI  A
  38. Ozen,A., Prachanronarong,K., Matthew,A.N., Soumana,D.I. and Schiffer,C.A.
    Resistance outside the substrate envelope: hepatitis C NS3/4A protease inhibitors
    Crit Rev Biochem Mol Biol54, 11-26. PubMed  Europe PubMed DOI  S
  39. Pethe,M.A., Rubenstein,A.B. and Khare,S.D.
    Data-driven supervised learning of a viral protease specificity landscape from deep sequencing and molecular simulations
    Proc Natl Acad Sci U S A116, 168-176. PubMed  Europe PubMed DOI  P
  40. Pham,L.V., Jensen,S.B., Fahnoe,U., Pedersen,M.S., Tang,Q., Ghanem,L., Ramirez,S., Humes,D., Serre,S.B.N., Schonning,K., Bukh,J. and Gottwein,J.M.
    HCV genotype 1-6 NS3 residue 80 substitutions impact protease inhibitor activity and promote viral escape
    J Hepatol70, 388-397. PubMed  Europe PubMed DOI  I
  41. Ren,J., Ojeda,I., Patel,M., Johnson,M.E. and Lee,H.
    Exploring small molecules with pan-genotypic inhibitory activities against hepatitis C virus NS3/4A serine protease
    Bioorg Med Chem Lett29, 2349-2353. PubMed  Europe PubMed DOI  I
  42. 2018
  43. Belfrage,A.K., Abdurakhmanov,E., Akerblom,E., Brandt,P., Alogheli,H., Neyts,J., Danielson,U.H. and Sandstrom,A.
    Pan-NS3 protease inhibitors of hepatitis C virus based on an R(3)-elongated pyrazinone scaffold
    Eur J Med Chem148, 453-464. PubMed  Europe PubMed DOI  I
  44. Bowsher,M., Hiebert,S., Li,R., Wang,A.X., Friborg,J., Yu,F., Hernandez,D., Wang,Y.K., Klei,H., Rajamani,R., Mosure,K., Knipe,J.O., Meanwell,N.A., McPhee,F. and Scola,P.M.
    The discovery and optimization of naphthalene-linked P2-P4 macrocycles as inhibitors of HCV NS3 protease
    Bioorg Med Chem Lett28, 43-48. PubMed  Europe PubMed DOI  I
  45. El-Sayed,S.M., Ali,M.A.M., El-Gendy,B.E.M., Dandash,S.S., Issac,Y., Saad,R., Azab,M.M. and Mohamed,M.R.
    Identification of novel small molecule inhibitors against the NS3/4A protease of hepatitis C virus genotype 4a
    Curr Pharm Des24, 4484-4491. PubMed  Europe PubMed DOI  I
  46. Lawitz,E., Yang,J.C., Stamm,L.M., Taylor,J.G., Cheng,G., Brainard,D.M., Miller,M.D., Mo,H. and Dvory-Sobol,H.
    Characterization of HCV resistance from a 3-day monotherapy study of voxilaprevir, a novel pangenotypic NS3/4A protease inhibitor
    Antivir Ther23, 325-334. PubMed  Europe PubMed DOI  I
  47. Matthew,A.N., Leidner,F., Newton,A., Petropoulos,C.J., Huang,W., Ali,A., KurtYilmaz,N. and Schiffer,C.A.
    Molecular mechanism of resistance in a clinically significant double-mutant variant of HCV NS3/4A protease
    Structure26, 1360-1372. PubMed  Europe PubMed DOI  I
  48. Nitsche,C.
    Strategies towards protease inhibitors for emerging flaviviruses
    Adv Exp Med Biol1062, 175-186. PubMed  Europe PubMed DOI  I
  49. Palanisamy,N. and Lennerstrand,J.
    Biophysical studies on HCV 1a NS3/4A protease and its catalytic triad in wild type and mutants by the in silico approach
    Interdiscip Sci10, 143-156. PubMed  Europe PubMed DOI  I
  50. Rusere,L.N., Matthew,A.N., Lockbaum,G.J., Jahangir,M., Newton,A., Petropoulos,C.J., Huang,W., Kurt Yilmaz,N., Schiffer,C.A. and Ali,A.
    Quinoxaline-based linear HCV NS3/4A protease inhibitors exhibit potent activity against drug resistant variants
    ACS Med Chem Lett9, 691-696. PubMed  Europe PubMed DOI  I
  51. Schwartz,N., Pellach,M., Glick,Y., Gil,R., Levy,G., Avrahami,D., Barbiro-Michaely,E., Nahmias,Y. and Gerber,D.
    Neuregulin 1 discovered as a cleavage target for the HCV NS3/4A protease by a microfluidic membrane protein array
    N Biotechnol45, 113-122. PubMed  Europe PubMed DOI
  52. Venables,B.L., Sin,N., Wang,A.X., Sun,L.Q., Tu,Y., Hernandez,D., Sheaffer,A., Lee,M., Dunaj,C., Zhai,G., Barry,D., Friborg,J., Yu,F., Knipe,J., Sandquist,J., Falk,P., Parker,D., Good,A.C., Rajamani,R., McPhee,F., Meanwell,N.A. and Scola,P.M.
    P3-P4 ureas and reverse carbamates as potent HCV NS3 protease inhibitors: effective transposition of the P4 hydrogen bond donor
    Bioorg Med Chem Lett28, 1853-1859. PubMed  Europe PubMed DOI  I
  53. Youngberg,S., Brandt,E., Barve,A., Machineni,S., Jones,C.T., Dabovic,K., Jones,C.L. and Colvin,R.A.
    A first-in-human, randomized, double-blind, placebo-controlled, single and multiple ascending oral dose study to assess the safety, tolerability, and pharmacokinetics of BZF961 with and without ritonavir in healthy adult volunteers
    J Drug Assess7, 66-74. PubMed  Europe PubMed DOI  I
  54. Zhai,P.B., Qing,J., Li,B., Zhang,L.Q., Ma,L. and Chen,L.
    GP205, a new hepatitis C virus NS3/4A protease inhibitor, displays higher metabolic stability in vitro and drug exposure in vivo
    Acta Pharmacol Sin39, 1746-1752. PubMed  Europe PubMed DOI  I
  55. Zheng,B., D'Andrea,S.V., Sun,L.Q., Wang,A.X., Chen,Y., Hrnciar,P., Friborg,J., Falk,P., Hernandez,D., Yu,F., Sheaffer,A.K., Knipe,J.O., Mosure,K., Rajamani,R., Good,A.C., Kish,K., Tredup,J., Klei,H.E., Paruchuri,M., Ng,A., Gao,Q., Rampulla,R.A., Mathur,A., Meanwell,N.A., McPhee,F. and Scola,P.M.
    Potent inhibitors of hepatitis C virus NS3 protease: employment of a difluoromethyl group as a hydrogen-bond donor
    ACS Med Chem Lett9, 143-148. PubMed  Europe PubMed DOI  S  I
  56. 2017
  57. Abdulrahman,A.Y., Rothan,H.A., Rashid,N.N., Lim,S.K., Sakhor,W., Tee,K.C., Teoh,T.C., Rahman,N.A. and Yusof,R.
    Identification of peptide leads to inhibit hepatitis C virus: inhibitory effect of plectasin peptide against hepatitis C serine protease
    Int J Pept Res Ther23, 163-170. DOI  I
  58. Guo,Z., Black,S., Hu,Y., McMonagle,P., Ingravallo,P., Chase,R., Curry,S. and Asante-Appiah,E.
    Unraveling the structural basis of grazoprevir potency against clinically relevant substitutions in hepatitis C virus NS3/4A protease from genotype 1a
    J Biol Chem292, 6202-6212. PubMed  Europe PubMed DOI  I
  59. Jin,G., Lee,J. and Lee,K.
    Chemical genetics-based development of small molecules targeting hepatitis C virus
    Arch Pharm Res40, 1021-1036. PubMed  Europe PubMed DOI  I
  60. Jindal,G., Mondal,D. and Warshel,A.
    Exploring the drug resistance of HCV protease
    J Phys Chem B121, 6831-6840. PubMed  Europe PubMed DOI  I
  61. Matthew,A.N., Zephyr,J., Hill,C.J., Jahangir,M., Newton,A., Petropoulos,C.J., Huang,W., Kurt-Yilmaz,N., Schiffer,C.A. and Ali,A.
    Hepatitis C virus NS3/4A protease inhibitors incorporating flexible P2 quinoxalines target drug resistant viral variants
    J Med Chem60, 5699-5716. PubMed  Europe PubMed DOI  I
  62. Naeem,A. and Waheed,Y.
    Sequence analysis of hepatitis C virus nonstructural protein 3-4A serine protease and prediction of conserved B and T cell epitopes
    Biomed Rep7, 563-566. PubMed  Europe PubMed DOI
  63. Ozdemir Isik,G. and Ozer,A.N.
    Prediction of substrate specificity in NS3/4A serine protease by biased sequence search threading
    J Biomol Struct Dyn35, 1102-1114. PubMed  Europe PubMed DOI  P
  64. Portela,A.C., Barros,T.G., Lima,C.H.D.S., Dias,L.R.S., Azevedo,P.H.R.A., Dantas,A.S.C.L., Mohana-Borges,R., Ventura,G.T., Pinheiro,S. and Muri,E.M.F.
    Isosorbide-based peptidomimetics as inhibitors of hepatitis C virus serine protease
    Bioorg Med Chem Lett27, 3661-3665. PubMed  Europe PubMed DOI  I
  65. Shunmugam,L., Ramharack,P. and Soliman,M.E.S.
    Road map for the structure-based design of selective covalent HCV NS3/4A protease inhibitors
    Protein J36, 397-406. PubMed  Europe PubMed DOI  I
  66. Skorenski,M., Pachota,M., Pyrc,K., Sienczyk,M. and Oleksyszyn,J.
    Novel peptidyl alpha-aminoalkylphosphonates as inhibitors of hepatitis C virus NS3/4A protease
    Antiviral Res144, 286-298. PubMed  Europe PubMed DOI  I
  67. Wang,A.X., Chen,J., Zhao,Q., Sun,L.Q., Friborg,J., Yu,F., Hernandez,D., Good,A.C., Klei,H.E., Rajamani,R., Mosure,K., Knipe,J.O., Li,D., Zhu,J., Levesque,P.C., McPhee,F., Meanwell,N.A. and Scola,P.M.
    Structure-activity relationships of 4-hydroxy-4-biaryl-proline acylsulfonamide tripeptides: a series of potent NS3 protease inhibitors for the treatment of hepatitis C virus
    Bioorg Med Chem Lett27, 590-596. PubMed  Europe PubMed DOI  I
  68. Wang,H., Guo,C., Chen,B.Z. and Ji,M.
    Computational study on the drug resistance mechanism of HCV NS3 protease to BMS-605339
    Biotechnol Appl Biochem64, 153-164. PubMed  Europe PubMed DOI  I
  69. Wang,S., Wang,Y., Wang,J., Sato,T., Izawa,K., Soloshonok,V.A. and Liu,H.
    The second-generation of highly potent hepatitis C virus (HCV) NS3/4A protease inhibitors: evolutionary design based on tailor-made amino acids, synthesis and major features of bio-activity
    Curr Pharm Des23, 4493-4554. PubMed  Europe PubMed DOI  I
  70. Yang,C.M., Yoon,J.C., Park,J.H. and Lee,J.M.
    Hepatitis C virus impairs natural killer cell activity via viral serine protease NS3
    PLoS ONE12, e0175793-e0175793. PubMed  Europe PubMed DOI  I
  71. Yang,L., Lin,J., Zhou,B., Liu,Y. and Zhu,B.
    Activity of compounds from Taxillus sutchuenensis as inhibitors of HCV NS3 serine protease
    Nat Prod Res31, 487-491. PubMed  Europe PubMed DOI  I
  72. 2016
  73. Chung,C.K., Cleator,E., Dumas,A.M., Hicks,J.D., Humphrey,G.R., Maligres,P.E., Nolting,A.F., Rivera,N., Ruck,R.T. and Shevlin,M.
    A synthesis of a spirocyclic macrocyclic protease inhibitor for the treatment of hepatitis C
    Org Lett18, 1394-1397. PubMed  Europe PubMed DOI  I
  74. Ferreira,A.R., Magalhaes,A.C., Camoes,F., Gouveia,A., Vieira,M., Kagan,J.C. and Ribeiro,D.
    Hepatitis C virus NS3-4A inhibits the peroxisomal MAVS-dependent antiviral signalling response
    J Cell Mol Med20, 750-757. PubMed  Europe PubMed DOI
  75. Gotte,M. and Feld,J.J.
    Direct-acting antiviral agents for hepatitis C: structural and mechanistic insights
    Nat Rev Gastroenterol Hepatol13, 338-351. PubMed  Europe PubMed DOI  I
  76. Guo,Y., Wang,Y., Cao,L., Wang,P., Qing,J., Zheng,Q., Shang,L., Yin,Z. and Sun,Y.
    A conserved inhibitory mechanism of a lycorine derivative against enterovirus and hepatitis C virus
    Antimicrob Agents Chemother60, 913-924. PubMed  Europe PubMed DOI  I
  77. Hamad,H.A., Thurston,J., Teague,T., Ackad,E. and Yousef,M.S.
    The NS4A cofactor dependent enhancement of HCV NS3 protease activity correlates with a 4D geometrical measure of the catalytic triad region
    PLoS ONE11, e0168002-e0168002. PubMed  Europe PubMed DOI  S
  78. Liang,L., Hu,J., Du,W., Zuo,K., Liu,W. and Gou,X.
    Molecular recognition mechanism and motion of HCV NS3/4A protease with Faldaprevir analogue
    Sheng Wu Gong Cheng Xue Bao32, 669-682. DOI  I
  79. McCauley,J.A. and Rudd,M.T.
    Hepatitis C virus NS3/4a protease inhibitors
    Curr Opin Pharmacol30, 84-92. PubMed  Europe PubMed DOI  I
  80. Meeprasert,A., Hannongbua,S., Kungwan,N. and Rungrotmongkol,T.
    Effect of D168V mutation in NS3/4A HCV protease on susceptibilities of faldaprevir and danoprevir
    Mol Biosyst12, 3666-3673. PubMed  Europe PubMed DOI  I
  81. Neelamkavil,S.F., Agrawal,S., Bara,T., Bennett,C., Bhat,S., Biswas,D., Brockunier,L., Buist,N., Burnette,D., Cartwright,M., Chackalamannil,S., Chase,R., Chelliah,M., Chen,A., Clasby,M., Colandrea,V.J., Davies,I.W., Eagen,K., Guo,Z., Han,Y., Howe,J., Jayne,C., Josien,H., Kargman,S., Marcantonio,K., Miao,S., Miller,R., Nolting,A., Pinto,P., Rajagopalan,M., Ruck,R.T., Shah,U., Soriano,A., Sperbeck,D., Velazquez,F., Wu,J., Xia,Y. and Venkatraman,S.
    Discovery of MK-8831, a novel spiro-proline macrocycle as a pan-genotypic HCV-NS3/4a protease inhibitor
    ACS Med Chem Lett7, 111-116. PubMed  Europe PubMed DOI  I
  82. Pillaiyar,T., Namasivayam,V. and Manickam,M.
    Macrocyclic hepatitis C virus NS3/4A protease inhibitors: An overview of medicinal chemistry
    Curr Med Chem23, 3404-3447. PubMed  Europe PubMed DOI  V  I
  83. Rodriguez-Torres,M., Glass,S., Hill,J., Freilich,B., Hassman,D., Di Bisceglie,A.M., Taylor,J.G., Kirby,B.J., Dvory-Sobol,H., Yang,J.C., An,D., Stamm,L.M., Brainard,D.M., Kim,S., Krefetz,D., Smith,W., Marbury,T. and Lawitz,E.
    GS-9857 in patients with chronic hepatitis C virus genotype 1-4 infection: a randomized, double-blind, dose-ranging phase 1 study
    J Viral Hepat23, 614-622. PubMed  Europe PubMed DOI  I
  84. Serre,S.B., Jensen,S.B., Ghanem,L., Humes,D.G., Ramirez,S., Li,Y.P., Krarup,H., Bukh,J. and Gottwein,J.M.
    Hepatitis C virus genotype 1 to 6 protease inhibitor escape variants: in vitro selection, fitness, and resistance patterns in the context of the infectious viral life cycle
    Antimicrob Agents Chemother60, 3563-3578. PubMed  Europe PubMed DOI  I
  85. Sun,L.Q., Mull,E., Zheng,B., D'Andrea,S., Zhao,Q., Wang,A.X., Sin,N., Venables,B.L., Sit,S.Y., Chen,Y., Chen,J., Cocuzza,A., Bilder,D.M., Mathur,A., Rampulla,R., Chen,B.C., Palani,T., Ganesan,S., Arunachalam,P.N., Falk,P., LeVine,S., Chen,C., Friborg,J., Yu,F., Hernandez,D., Sheaffer,A.K., Knipe,J.O., Han,Y.H., Schartman,R., Donoso,M., Mosure,K., Sinz,M.W., Zvyaga,T., Rajamani,R., Kish,K., Tredup,J., Klei,H.E., Gao,Q., Ng,A., Mueller,L., Grasela,D.M., Adams,S., Loy,J., Levesque,P.C., Sun,H., Shi,H., Sun,L., Warner,W., Li,D., Zhu,J., Wang,Y.K., Fang,H., Cockett,M.I., Meanwell,N.A., McPhee,F. and Scola,P.M.
    Discovery of a potent acyclic, tripeptidic, acyl sulfonamide inhibitor of hepatitis C virus NS3 protease as a back-up to asunaprevir with the potential for once-daily dosing
    J Med Chem59, 8042-8060. PubMed  Europe PubMed DOI  I
  86. Yao,M., Lu,X., Lei,Y., Yang,J., Zhao,H., Qiao,Q., Han,P., Xu,Z. and Yin,W.
    Conditional inducible triple-transgenic mouse model for rapid real-time detection of HCV NS3/4A protease activity
    PLoS ONE11, e0150894-e0150894. PubMed  Europe PubMed DOI  A  L
  87. 2015
  88. Alexandre,F.R., Brandt,G., Caillet,C., Chaves,D., Convard,T., Derock,M., Gloux,D., Griffon,Y., Lallos,L., Leroy,F., Liuzzi,M., Loi,A.G., Moulat,L., Musiu,C., Parsy,C., Rahali,H., Roques,V., Seifer,M., Standring,D. and Surleraux,D.
    Synthesis and antiviral evaluation of a novel series of homoserine-based inhibitors of the hepatitis C virus NS3/4A serine protease
    Bioorg Med Chem Lett25, 3984-3991. PubMed  Europe PubMed DOI  I
  89. Fu,J. and Wei,J.
    Molecular dynamics study on drug resistance mechanism of HCV NS3/4A protease inhibitor: BI201335
    Mol Simul41, 674-682. DOI  I
  90. Hajji,H., Aherfi,S., Motte,A., Ravaux,I., Mokhtari,S., Ruiz,J.-M., Poizot-Martin,I., Tourres,C., Tivoli,N., Gerolami,R., Tamalet,C. and Colson,P.
    Diversity of 1,213 hepatitis C virus NS3 protease sequences from a clinical virology laboratory database in Marseille university hospitals, southeastern France
    J Med Virol87, 1921-1933. PubMed  Europe PubMed DOI
  91. Han,B., Dvory-Sobol,H., Greenstein,A., McCarville,J.F., Hung,M., Liu,X., Miller,M.D. and Mo,H.
    Development and application of a fast, reproducible assay to measure HCV NS3 protease activity using Escherichia coli lysate
    J Virol Methods225, 76-86. PubMed  Europe PubMed DOI  A
  92. Hoffmann,L., Faffe,D.S., Lima,J.F.C., Capitanio,T.A., Cabral,B.C.A., Urmenyi,T.P., Coelho,H.S.M., Rondinelli,E., Villela-Nogueira,C.A. and Silva,R.
    No correspondence between resistance mutations in the HCV-NS3 protease at baseline and early telaprevir-based triple therapy
    BBA Clin3, 146-151. PubMed  Europe PubMed DOI  I
  93. Kutova,R., Puskova,L., Stepanova,V., Machac,J. and Plisek,S.
    Determination of the naturally occurring Q80K mutation in the HCV NS3 protease gene
    Klin Mikrobiol Infekc Lek21, 126-129.  I
  94. Martinez-Gonzalez,J.A., Rodriguez,A., Puyuelo,M.P., Gonzalez,M. and Martinez,R.
    Further theoretical insight into the reaction mechanism of the hepatitis C NS3/NS4A serine protease
    Chem Phys Lett619, 97-102. DOI
  95. Martinez-Gonzalez,J.A., Gonzalez,M., Masgrau,L. and Martinez,R.
    Theoretical study of the free energy surface and kinetics of the hepatitis C virus NS3/NS4A serine protease reaction with the NS5A/5B substrate. Does the generally accepted tetrahedral intermediate really exist?
    ACS Catal5, 246-255. DOI
  96. Nagpal,N., Goyal,S., Wahi,D., Jain,R., Jamal,S., Singh,A., Rana,P. and Grover,A.
    Molecular principles behind Boceprevir resistance due to mutations in hepatitis C NS3/4A protease
    Gene570, 115-121. PubMed  Europe PubMed DOI  I
  97. Ndjomou,J., Corby,M.J., Sweeney,N.L., Hanson,A.M., Aydin,C., Ali,A., Schiffer,C.A., Li,K., Frankowski,K.J., Schoenen,F.J. and Frick,D.N.
    Simultaneously targeting the NS3 protease and helicase activities for more effective hepatitis C virus therapy
    ACS Chem Biol10, 1887-1896. PubMed  Europe PubMed DOI  I
  98. Rudd,M.T., Butcher,J.W., Nguyen,K.T., McIntyre,C.J., Romano,J.J., Gilbert,K.F., Bush,K.J., Liverton,N.J., Holloway,M.K., Harper,S., Ferrara,M., DiFilippo,M., Summa,V., Swestock,J., Fritzen,J., Carroll,S.S., Burlein,C., DiMuzio,J.M., Gates,A., Graham,D.J., Huang,Q., McClain,S., McHale,C., Stahlhut,M.W., Black,S., Chase,R., Soriano,A., Fandozzi,C.M., Taylor,A., Trainor,N., Olsen,D.B., Coleman,P.J., Ludmerer,S.W. and McCauley,J.A.
    P2-Quinazolinones and bis-macrocycles as new templates for next-generation hepatitis C virus NS3/4a protease inhibitors: discovery of MK-2748 and MK-6325
    ChemMedChem10, 727-735. PubMed  Europe PubMed DOI  I
  99. Shi,F., Zhang,Y. and Xu,W.
    Discovery of a series of novel compounds with moderate anti-hepatitis C virus NS3 protease activity in vitro
    Bioorg Med Chem23, 5539-5545. PubMed  Europe PubMed DOI  I
  100. Verbinnen,T., Fevery,B., Vijgen,L., Jacobs,T., De Meyer,S. and Lenz,O.
    In vitro activity of simeprevir against hepatitis C virus genotype 1 clinical isolates and its correlation with NS3 sequence and site-directed mutants
    Antimicrob Agents Chemother59, 7548-7557. PubMed  Europe PubMed DOI  I
  101. Wang,M., Xuan,S., Yan,A. and Yu,C.
    Classification models of HCV NS3 protease inhibitors based on support vector machine (SVM)
    Comb Chem High Throughput Screen18, 24-32. PubMed  Europe PubMed  I
  102. Wu,D.W., Mao,F., Ye,Y., Li,J., Xu,C.L., Luo,X.M., Chen,J. and Shen,X.
    Policresulen, a novel NS2B/NS3 protease inhibitor, effectively inhibits the replication of DENV2 virus in BHK-21 cells
    Acta Pharmacol Sin36, 1126-1136. PubMed  Europe PubMed DOI  I
  103. Yang,N., Sun,Q., Xu,Z., Wang,X., Zhao,X., Cao,Y., Chen,L. and Fan,G.
    LC-ESI-MS/MS analysis and pharmacokinetics of GP205, an innovative potent macrocyclic inhibitor of hepatitis C virus NS3/4A protease in rats
    Molecules20, 4319-4336. PubMed  Europe PubMed DOI  I
  104. 2014
  105. Abrahim-Vieira,B., Da Costa,E.C.B., de A.Azevedo,P.H.R., Portela,A.C., Dias,L.R.S., Pinheiro,S., Tanuri,A., Capaccia,A.M., Ventura,G.T., Mohana-Borges,R., Rodrigues,C.R., de Souza,A.M.T. and Muri,E.M.F.
    Novel isomannide-based peptide mimetics containing a tartaric acid backbone as serine protease inhibitors
    Med Chem Res23, 5305-5320. DOI  I
  106. De Clercq,E.
    Current race in the development of DAAs (direct-acting antivirals) against HCV
    Biochem Pharmacol89, 441-452. PubMed  Europe PubMed DOI  I
  107. Ehrenberg,A.E., Schmuck,B., Anwar,M.I., Gustafsson,S.S., Stenberg,G. and Danielson,U.H.
    Accounting for strain variations and resistance mutations in the characterization of hepatitis C NS3 protease inhibitors
    J Enzyme Inhib Med Chem29, 868-876. PubMed  Europe PubMed DOI  I
  108. Ehret,R., Neifer,S., Walter,H., Baumgarten,A. and Obermeier,M.
    Appearance of NS3 Q80K mutation in HCV genotype 1a mono- or HIV/HCV co-infected patients in a Berlin laboratory
    J Int AIDS Soc17, 19741-19741. PubMed  Europe PubMed  M  I
  109. Ezat,A.A., El-Bialy,N.S., Mostafa,H.I. and Ibrahim,M.A.
    Molecular docking investigation of the binding interactions of macrocyclic inhibitors with HCV NS3 protease and its mutants (R155K, D168A and A156V)
    Protein J33, 32-47. PubMed  Europe PubMed DOI  I
  110. Gentile,I., Buonomo,A.R., Borgia,F., Zappulo,E., Castaldo,G. and Borgia,G.
    MK-5172 : a second-generation protease inhibitor for the treatment of hepatitis C virus infection
    Expert Opin Investig Drugs23, 719-728. PubMed  Europe PubMed DOI  I
  111. Gentile,I., Borgia,F., Buonomo,A.R., Zappulo,E., Castaldo,G. and Borgia,G.
    ABT-450: a novel protease inhibitor for the treatment of hepatitis C virus infection
    Curr Med Chem21, 3261-3270. PubMed  Europe PubMed DOI  I
  112. Ghosh,A.K., Schiltz,G.E., Rusere,L.N., Osswald,H.L., Walters,D.E., Amano,M. and Mitsuya,H.
    Design and synthesis of potent macrocyclic HIV-1 protease inhibitors involving P1-P2 ligands
    Org Biomol Chem12, 6842-6854. PubMed  Europe PubMed DOI  I
  113. Gising,J., Belfrage,A.K., Alogheli,H., Ehrenberg,A., Akerblom,E., Svensson,R., Artursson,P., Karlen,A., Danielson,U.H., Larhed,M. and Sandstrom,A.
    Achiral pyrazinone-based inhibitors of the hepatitis C virus NS3 protease and drug-resistant variants with elongated substituents directed toward the S2 pocket
    J Med Chem57, 1790-1801. PubMed  Europe PubMed DOI  I
  114. Guan,Y., Sun,H., Li,Y., Pan,P., Li,D. and Hou,T.
    The competitive binding between inhibitors and substrates of HCV NS3/4A protease: a general mechanism of drug resistance
    Antiviral Res103, 60-70. PubMed  Europe PubMed DOI  I
  115. Jenkins,S., Scola,P., McPhee,F., Knipe,J., Gesenberg,C., Sinz,M., Arora,V., Pilcher,G. and Santone,K.
    Preclinical pharmacokinetics and in vitro metabolism of BMS-605339: a novel HCV NS3 protease inhibitor
    J Pharm Sci103, 1891-1902. PubMed  Europe PubMed DOI  I
  116. Kirschberg,T.A., Squires,N.H., Yang,H., Corsa,A.C., Tian,Y., Tirunagari,N., Sheng,X.C. and Kim,C.U.
    Novel, sulfonamide linked inhibitors of the hepatitis C virus NS3 protease
    Bioorg Med Chem Lett24, 969-972. PubMed  Europe PubMed DOI  I
  117. Kramer,M., Halleran,D., Rahman,M., Iqbal,M., Anwar,M.I., Sabet,S., Ackad,E., Yousef,M.S. and Yousef,M.
    Comparative molecular dynamics simulation of hepatitis C virus NS3/4A protease (genotypes 1b, 3a and 4b) predicts conformational instability of the catalytic triad in drug resistant strains
    PLoS ONE9, e104425-e104425. PubMed  Europe PubMed DOI
  118. Lampa,A., Alogheli,H., Ehrenberg,A.E., Akerblom,E., Svensson,R., Artursson,P., Danielson,U.H., Karlen,A. and Sandstrom,A.
    Vinylated linear P2 pyrimidinyloxyphenylglycine based inhibitors of the HCV NS3/4A protease and corresponding macrocycles
    Bioorg Med Chem22, 6595-6615. PubMed  Europe PubMed DOI  I
  119. Lampa,A.K., Bergman,S.M., Gustafsson,S.S., Alogheli,H., Akerblom,E.B., Lindeberg,G.G., Svensson,R.M., Artursson,P., Danielson,U.H., Karlen,A. and Sandstrom,A.
    Novel peptidomimetic hepatitis C virus NS3/4A protease inhibitors spanning the P2-P1' region
    ACS Med Chem Lett5, 249-254. PubMed  Europe PubMed DOI  I
  120. Lan,H.Y., Zhao,Y., Yang,J., Sun,M.N., Lei,Y.F., Yao,M., Huang,X.J., Zhang,J.M., Xu,Z.K., Lu,X. and Yin,W.
    Establishment of a novel triple-transgenic mouse: conditionally and liver-specifically expressing hepatitis C virus NS3/4A protease
    Mol Biol Rep41, 7349-7359. PubMed  Europe PubMed DOI
  121. Manns,M.P., Vierling,J.M., Bacon,B.R., Bruno,S., Shibolet,O., Baruch,Y., Marcellin,P., Caro,L., Howe,A.Y., Fandozzi,C., Gress,J., Gilbert,C.L., Shaw,P.M., Cooreman,M.P., Robertson,M.N., Hwang,P., Dutko,F.J., Wahl,J. and Mobashery,N.
    The combination of MK-5172, peginterferon, and ribavirin is effective in treatment-naive patients with hepatitis C virus genotype 1 infection without cirrhosis
    Gastroenterology147, 366-376. PubMed  Europe PubMed DOI  I
  122. Meeprasert,A., Rungrotmongkol,T., Li,M.S. and Hannongbua,S.
    In silico screening for potent inhibitors against the NS3/4A protease of hepatitis C virus
    Curr Pharm Des20, 3465-3477. PubMed  Europe PubMed DOI  I
  123. Meeprasert,A., Hannongbua,S. and Rungrotmongkol,T.
    Key binding and susceptibility of NS3/4A serine protease inhibitors against hepatitis C virus
    J Chem Inf Model54, 1208-1217. PubMed  Europe PubMed DOI  I
  124. Moreau,B., O'Meara,J.A., Bordeleau,J., Garneau,M., Godbout,C., Gorys,V., Leblanc,M., Villemure,E., White,P.W. and Llinas-Brunet,M.
    Discovery of hepatitis C virus NS3-4A protease inhibitors with improved barrier to resistance and favorable liver distribution
    J Med Chem57, 1770-1776. PubMed  Europe PubMed DOI  S  I
  125. Morikawa,K., Gouttenoire,J., Hernandez,C., Dao Thi,V.L., Tran,H.T., Lange,C.M., Dill,M.T., Heim,M.H., Donze,O., Penin,F., Quadroni,M. and Moradpour,D.
    Quantitative proteomics identifies the membrane-associated peroxidase GPx8 as a cellular substrate of the hepatitis C virus NS3-4A protease
    Hepatology59, 423-433. PubMed  Europe PubMed DOI  P
  126. Mostafa,H.I.A., El-Bialy,N.S., Ezat,A.A., Saleh,N.A. and Ibrahim,M.A.
    QSAR analysis and molecular docking simulation of suggested peptidomimetic NS3 protease inhibitors
    Curr Comput -Aided Drug Des10, 28-40. PubMed  Europe PubMed DOI  I
  127. Parsy,C., Alexandre,F.R., Brandt,G., Caillet,C., Cappelle,S., Chaves,D., Convard,T., Derock,M., Gloux,D., Griffon,Y., Lallos,L., Leroy,F., Liuzzi,M., Loi,A.G., Moulat,L., Musiu,C., Rahali,H., Roques,V., Seifer,M., Standring,D. and Surleraux,D.
    Structure-based design of a novel series of azetidine inhibitors of the hepatitis C virus NS3/4A serine protease
    Bioorg Med Chem Lett24, 4444-4449. PubMed  Europe PubMed DOI  I
  128. Poordad,F., Hezode,C., Trinh,R., Kowdley,K.V., Zeuzem,S., Agarwal,K., Shiffman,M.L., Wedemeyer,H., Berg,T., Yoshida,E.M., Forns,X., Lovell,S.S., Da Silva-Tillmann,B., Collins,C.A., Campbell,A.L., Podsadecki,T. and Bernstein,B.
    ABT-450/r-ombitasvir and dasabuvir with ribavirin for hepatitis C with cirrhosis
    N Engl J Med370, 1973-1982. PubMed  Europe PubMed DOI  I
  129. Qiao,J., Yu,J., Yang,H. and Wei,H.
    PCR-Based in vitro synthesis of hepatitis C virus NS3 protease for rapid phenotypic resistance testing of protease inhibitors
    J Clin Microbiol52, 1139-1145. PubMed  Europe PubMed DOI  E
  130. Reddy,B.U., Mullick,R., Kumar,A., Sudha,G., Srinivasan,N. and Das,S.
    Small molecule inhibitors of HCV replication from Pomegranate
    Sci Rep4, 5411-5411. PubMed  Europe PubMed DOI  I
  131. Rimmert,B., Sabet,S., Ackad,E. and Yousef,M.S.
    A 3D structural model and dynamics of hepatitis C virus NS3/4A protease (genotype 4a, strain ED43) suggest conformational instability of the catalytic triad: implications in catalysis and drug resistivity
    J Biomol Struct Dyn32, 950-958. PubMed  Europe PubMed DOI  S
  132. Scola,P.M., Wang,A.X., Good,A.C., Sun,L.Q., Combrink,K.D., Campbell,J.A., Chen,J., Tu,Y., Sin,N., Venables,B.L., Sit,S.Y., Chen,Y., Cocuzza,A., Bilder,D.M., D'Andrea,S., Zheng,B., Hewawasam,P., Ding,M., Thuring,J., Li,J., Hernandez,D., Yu,F., Falk,P., Zhai,G., Sheaffer,A.K., Chen,C., Lee,M.S., Barry,D., Knipe,J.O., Li,W., Han,Y.H., Jenkins,S., Gesenberg,C., Gao,Q., Sinz,M.W., Santone,K.S., Zvyaga,T., Rajamani,R., Klei,H.E., Colonno,R.J., Grasela,D.M., Hughes,E., Chien,C., Adams,S., Levesque,P.C., Li,D., Zhu,J., Meanwell,N.A. and McPhee,F.
    Discovery and early clinical evaluation of BMS-605339, a potent and orally efficacious tripeptidic acylsulfonamide NS3 protease inhibitor for the treatment of hepatitis C virus infection
    J Med Chem57, 1708-1729. PubMed  Europe PubMed DOI  I
  133. Shah,U., Jayne,C., Chackalamannil,S., Velazquez,F., Guo,Z., Buevich,A., Howe,J.A., Chase,R., Soriano,A., Agrawal,S., Rudd,M.T., McCauley,J.A., Liverton,N.J., Romano,J., Bush,K., Coleman,P.J., Grise-Bard,C., Brochu,M.C., Charron,S., Aulakh,V., Bachand,B., Beaulieu,P., Zaghdane,H., Bhat,S., Han,Y., Vacca,J.P., Davies,I.W., Weber,A.E. and Venkatraman,S.
    Novel quinoline-based P2-P4 macrocyclic derivatives as pan-genotypic HCV NS3/4a protease inhibitors
    ACS Med Chem Lett5, 264-269. PubMed  Europe PubMed DOI  I
  134. Shang,L., Lin,K. and Yin,Z.
    Resistance mutations against HCV protease inhibitors and antiviral drug design
    Curr Pharm Des20, 694-703. PubMed  Europe PubMed DOI  M  I
  135. Wadood,A., Riaz,M., Jamal,S.B. and Shah,M.
    Interactions of ketoamide inhibitors on HCV NS3/4A protease target: molecular docking studies
    Mol Biol Rep41, 337-345. PubMed  Europe PubMed DOI  I
  136. Wang,H., Geng,L., Chen,B.Z. and Ji,M.
    Computational study on the molecular mechanisms of drug resistance of narlaprevir due to V36M, R155K, V36M+R155K, T54A, and A156T mutations of HCV NS3/4A protease
    Biochem Cell Biol92, 357-369. PubMed  Europe PubMed DOI  I
  137. Xue,W., Ban,Y., Liu,H. and Yao,X.
    Computational study on the drug resistance mechanism against HCV NS3/4A protease inhibitors vaniprevir and MK-5172 by the combination use of molecular dynamics simulation, residue interaction network, and substrate envelope analysis
    J Chem Inf Model54, 621-633. PubMed  Europe PubMed DOI  I
  138. Yang,H., Robinson,M., Corsa,A.C., Peng,B., Cheng,G., Tian,Y., Wang,Y., Pakdaman,R., Shen,M., Qi,X., Mo,H., Tay,C., Krawczyk,S., Sheng,X.C., Kim,C.U., Yang,C. and Delaney,W.E.4.
    Preclinical characterization of the novel hepatitis C virus NS3 protease inhibitor GS-9451
    Antimicrob Agents Chemother58, 647-653. PubMed  Europe PubMed DOI  I
  139. 2013
  140. Abian,O., Vega,S., Sancho,J. and Velazquez-Campoy,A.
    Allosteric inhibitors of the NS3 protease from the hepatitis C virus
    PLoS ONE8, e69773-e69773. PubMed  Europe PubMed DOI  I
  141. Akuta,N., Suzuki,F., Seko,Y., Kawamura,Y., Sezaki,H., Suzuki,Y., Hosaka,T., Kobayashi,M., Hara,T., Kobayashi,M., Saitoh,S., Arase,Y., Ikeda,K. and Kumada,H.
    Emergence of telaprevir-resistant variants detected by ultra-deep sequencing after triple therapy in patients infected with HCV genotype 1
    J Med Virol85, 1028-1036. PubMed  Europe PubMed DOI  I
  142. Ali,A., Aydin,C., Gildemeister,R., Romano,K.P., Cao,H., Ozen,A., Soumana,D., Newton,A., Petropoulos,C.J., Huang,W. and Schiffer,C.A.
    Evaluating the role of macrocycles in the susceptibility of hepatitis C virus NS3/4A protease inhibitors to drug resistance
    ACS Chem Biol8, 1469-1478. PubMed  Europe PubMed DOI  I
  143. Arumugasamy,J., Arunachalam,K., Bauer,D., Becker,A., Caillet,C.A., Glynn,R., Latham,G.M., Lim,J., Liu,J., Mayes,B.A., Moussa,A., Rosinovsky,E., Salanson,A.E., Soret,A.F., Stewart,A., Wang,J. and Wu,X.
    Development of related HCV protease inhibitors: macrocyclization of two highly functionalized dienyl-ureas via ring-closing metathesis
    Org Process Res Dev17, 811-828. DOI  I
  144. Bailey,M.D., Bordeleau,J., Garneau,M., Leblanc,M., Lemke,C.T., O'Meara,J., White,P.W. and Llinas-Brunet,M.
    Peptide backbone replacement of hepatitis C virus NS3 serine protease C-terminal cleavage product analogs: discovery of potent succinamide inhibitors
    Bioorg Med Chem Lett23, 4447-4452. PubMed  Europe PubMed DOI  I
  145. Bailey,M.D., Halmos,T. and Lemke,C.T.
    Discovery of novel P2 substituted 4-biaryl proline inhibitors of hepatitis C virus NS3 serine protease
    Bioorg Med Chem Lett23, 4436-4440. PubMed  Europe PubMed DOI  I
  146. Bilodeau,F., Bailey,M.D., Bhardwaj,P.K., Bordeleau,J., Forgione,P., Garneau,M., Ghiro,E., Gorys,V., Halmos,T., Jolicoeur,E.S., Leblanc,M., Lemke,C.T., Naud,J., O'Meara,J., White,P.W. and Llinas-Brunet,M.
    Synthesis and optimization of a novel series of HCV NS3 protease inhibitors: 4-arylproline analogs
    Bioorg Med Chem Lett23, 4267-4271. PubMed  Europe PubMed DOI  I
  147. Bondada,L., Rondla,R., Pradere,U., Liu,P., Li,C., Bobeck,D., McBrayer,T., Tharnish,P., Courcambeck,J., Halfon,P., Whitaker,T., Amblard,F., Coats,S.J. and Schinazi,R.F.
    Azetidines and spiro azetidines as novel P2 units in hepatitis C virus NS3 protease inhibitors
    Bioorg Med Chem Lett23, 6325-6330. PubMed  Europe PubMed DOI  I
  148. Clark,V.C., Peter,J.A. and Nelson,D.R.
    New therapeutic strategies in HCV: second-generation protease inhibitors
    Liver Int33 Suppl 1, 80-84. PubMed  Europe PubMed DOI  I
  149. Da Cunha,E.F.F., Matos,K.S. and Ramalho,T.C.
    QSAR and docking studies of HCV NS3 serine protease inhibitors
    Med Chem9, 774-805. PubMed  Europe PubMed DOI  I
  150. De Bruijne,J., Thomas,X.V., Rebers,S.P., Weegink,C.J., Treitel,M.A., Hughes,E., Bergmann,J.F., de Knegt,R.J., Janssen,H.L.A., Reesink,H.W., Molenkamp,R. and Schinkel,J.
    Evolutionary dynamics of hepatitis C virus NS3 protease domain during and following treatment with narlaprevir, a potent NS3 protease inhibitor
    J Viral Hepat20, 779-789. PubMed  Europe PubMed DOI  I
  151. Hui,C.Y., Xie,X.B., Cao,H. and Huang,S.H.
    The development of novel HCV NS3-4A protease inhibitors
    Anti-Infect Agents11, 125-135. DOI  V  I
  152. Ismail,M.A., Abouzid,K.A., Mohamed,N.S. and Dokla,E.M.
    Ligand design, synthesis and biological anti-HCV evaluations for genotypes 1b and 4a of certain 4-(3- & 4-[3-(3,5-dibromo-4-hydroxyphenyl)-propylamino]phenyl) butyric acids and 3-(3,5-dibromo-4-hydroxyphenyl)-propylamino-acetamidobenzoic acid esters
    J Enzyme Inhib Med Chem28, 1274-1290. PubMed  Europe PubMed DOI  I
  153. Kang,X., Chen,X., He,Y., Guo,D., Guo,L., Zhong,J. and Shu,H.B.
    DDB1 is a cellular substrate of NS3/4A protease and required for hepatitis C virus replication
    Virology435, 385-394. PubMed  Europe PubMed DOI  P
  154. Lasheen,D.S., Ismail,M.A., Abou El Ella,D.A., Ismail,N.S., Eid,S., Vleck,S., Glenn,J.S., Watts,A.G. and Abouzid,K.A.
    Analogs design, synthesis and biological evaluation of peptidomimetics with potential anti-HCV activity
    Bioorg Med Chem21, 2742-2755. PubMed  Europe PubMed DOI  I
  155. Lee,H., Zhu,T., Patel,K., Zhang,Y.Y., Truong,L., Hevener,K.E., Gatuz,J.L., Subramanya,G., Jeong,H.Y., Uprichard,S.L. and Johnson,M.E.
    High-throughput screening (HTS) and hit validation to identify small molecule inhibitors with activity against NS3/4A proteases from multiple hepatitis C virus genotypes
    PLoS ONE8, e75144-e75144. PubMed  Europe PubMed DOI  I
  156. Li,J., Liu,X., Li,S., Wang,Y., Zhou,N., Luo,C., Luo,X., Zheng,M., Jiang,H. and Chen,K.
    Identification of novel small molecules as inhibitors of hepatitis C virus by structure-based virtual screening
    Int J Mol Sci14, 22845-22856. PubMed  Europe PubMed DOI  I
  157. Mawatari,S., Uto,H., Ido,A., Nakashima,K., Suzuki,T., Kanmura,S., Kumagai,K., Oda,K., Tabu,K., Tamai,T., Moriuchi,A., Oketani,M., Shimada,Y., Sudoh,M., Shoji,I. and Tsubouchi,H.
    Hepatitis C virus NS3/4A protease inhibits complement activation by cleaving complement component 4
    PLoS ONE8, e82094-e82094. PubMed  Europe PubMed DOI
  158. O'Meara,J.A., Lemke,C.T., Godbout,C., Kukolj,G., Lagace,L., Moreau,B., Thibeault,D., White,P.W. and Llinas-Brunet,M.
    Molecular mechanism by which a potent hepatitis C virus NS3-NS4A protease inhibitor overcomes emergence of resistance
    J Biol Chem288, 5673-5681. PubMed  Europe PubMed DOI  I
  159. Ray,U., Roy,C.L., Kumar,A., Mani,P., Joseph,A.P., Sudha,G., Sarkar,D.P., Srinivasan,N. and Das,S.
    Inhibition of the interaction between NS3 protease and HCV IRES with a small peptide: a novel therapeutic strategy
    Mol Ther21, 57-67. PubMed  Europe PubMed DOI
  160. Sandhiya,R., Dayshy,A.R., Shanthi,V. and Ramanathan,K.
    Investigation of MK-5172 resistance against R155K NS3/4A protease by molecular simulation approach
    Der Pharm Lett5, 13-20.  I
  161. Wadood,A., Riaz,M., Jamal,S.B., Shah,M. and Lodhi,M.A.
    Molecular docking study of P4-Benzoxaborole substituted ligands as inhibitors of HCV NS3/4A protease
    Bioinformation9, 309-314. PubMed  Europe PubMed DOI  I
  162. Zeminian,L.B., Padovani,J.L., Corvino,S.M., Silva,G.F., Pardini,M.I. and Grotto,R.M.
    Variability and resistance mutations in the hepatitis C virus NS3 protease in patients not treated with protease inhibitors
    Mem Inst Oswaldo Cruz108, 13-17. PubMed  Europe PubMed DOI
  163. Zhang,R. and Windsor,W.T.
    In vitro kinetic profiling of hepatitis C virus NS3 protease inhibitors by progress curve analysis
    Methods Mol Biol1030, 59-79. PubMed  Europe PubMed DOI  A
  164. 2012
  165. Agarwal,A., Zhang,B., Olek,E., Robison,H., Robarge,L. and Deshpande,M.
    Rapid and sharp decline in HCV upon monotherapy with NS3 protease inhibitor, ACH-1625
    Antivir Ther17, 1533-1539. PubMed  Europe PubMed DOI  I
  166. Alkhouri,N. and Zein,N.N.
    Protease inhibitors: silver bullets for chronic hepatitis C infection?
    Cleve Clin J Med79, 213-222. PubMed  Europe PubMed DOI  I
  167. Bachmetov,L., Gal-Tanamy,M., Shapira,A., Vorobeychik,M., Giterman-Galam,T., Sathiyamoorthy,P., Golan-Goldhirsh,A., Benhar,I., Tur-Kaspa,R. and Zemel,R.
    Suppression of hepatitis C virus by the flavonoid quercetin is mediated by inhibition of NS3 protease activity
    J Viral Hepat19, e81-e88. PubMed  Europe PubMed DOI  I
  168. Barros,T.G., Zorzanelli,B.C., Pinheiro,S., De Brito,M.A., Tanuri,A., Da Costa,E.C.B., Mohana-Borges,R.S., Rodrigues,C.R., Souza,A.T.M., Ferreira,V.F. and Muri,E.M.F.
    Novel peptide mimetics based on N-Protected amino acids derived from isomannide as potential inhibitors of NS3 serine protease of hepatitis C virus
    Lett Org Chem9, 239-249.  I
  169. Brown,A.N., McSharry,J.J., Adams,J.R., Kulawy,R., Barnard,R.J., Newhard,W., Corbin,A., Hazuda,D.J., Louie,A. and Drusano,G.L.
    Pharmacodynamic analysis of a serine protease inhibitor, MK-4519, against hepatitis C virus using a novel in vitro pharmacodynamic system
    Antimicrob Agents Chemother56, 1170-1181. PubMed  Europe PubMed DOI  I
  170. Cento,V., Mirabelli,C., Salpini,R., Dimonte,S., Artese,A., Costa,G., Mercurio,F., Svicher,V., Parrotta,L., Bertoli,A., Ciotti,M., Di Paolo,D., Sarrecchia,C., Andreoni,M., Alcaro,S., Angelico,M., Perno,C.F. and Ceccherini-Silberstein,F.
    HCV genotypes are differently prone to the development of resistance to linear and macrocyclic protease inhibitors
    PLoS ONE7, e39652-e39652. PubMed  Europe PubMed DOI  S  I
  171. Chaudhuri,R., Lee,H., Truong,L., Torres,J., Patel,K. and Johnson,M.E.
    Identification of non-macrocyclic small molecule inhibitors against the NS3/4A serine protease of hepatitis C virus through in silico screening
    J Chem Inf Model52, 2245-2256. PubMed  Europe PubMed DOI  I
  172. Clarke,M.O., Byun,D., Chen,X., Doerffler,E., Leavitt,S.A., Sheng,X.C., Yang,C.Y. and Kim,C.U.
    Novel, potent and orally bioavailable indolizidinone-derived inhibitors of the hepatitis C virus NS3 protease
    Bioorg Med Chem Lett22, 1095-1098. PubMed  Europe PubMed DOI  I
  173. Colson,P., Purgus,R., Borentain,P. and Gerolami,R.
    Natural presence of NS3 protease R155K hepatitis C virus variants with decreased sensitivity to protease inhibitors
    J Clin Virol53, 178-180. PubMed  Europe PubMed DOI  M
  174. De Bruijne,J., Van Vliet,A., Weegink,C.J., Mazur,W., Wiercinska-Drapalo,A., Simon,K., Cholewinska-Szymanska,G., Kapocsi,J., Varkonyi,I., Zhou,X.J., Temam,M.F., Molles,J., Chen,J., Pietropaolo,K., McCarville,J.F., Sullivan-Bolyai,J.Z., Mayers,D. and Reesink,H.
    Rapid decline of viral RNA in chronic hepatitis C patients treated once daily with IDX320: a novel macrocyclic HCV protease inhibitor
    Antivir Ther17, 633-642. PubMed  Europe PubMed DOI  I
  175. Duan,M., Kazmierski,W., Crosby,R., Gartland,M., Ji,J., Tallant,M., Wang,A., Hamatake,R., Wright,L., Wu,M., Zhang,Y.K., Ding,C.Z., Li,X., Liu,Y., Zhang,S., Zhou,Y., Plattner,J.J. and Baker,S.J.
    Discovery of novel P3-oxo inhibitor of hepatitis C virus NS3/4A serine protease
    Bioorg Med Chem Lett22, 2993-2996. PubMed  Europe PubMed DOI  I
  176. Harper,S., McCauley,J.A., Rudd,M.T., Ferrara,M., DiFilippo,M., Crescenzi,B., Koch,U., Petrocchi,A., Holloway,M.K., Butcher,J.W., Romano,J.J., Bush,K.J., Gilbert,K.F., McIntyre,C.J., Nguyen,K.T., Nizi,E., Carroll,S.S., Ludmerer,S.W., Burlein,C., DiMuzio,J.M., Graham,D.J., McHale,C.M., Stahlhut,M.W., Olsen,D.B., Monteagudo,E., Cianetti,S., Giuliano,C., Pucci,V., Trainor,N., Fandozzi,C.M., Rowley,M., Coleman,P.J., Vacca,J.P., Summa,V. and Liverton,N.J.
    Discovery of MK-5172, a macrocyclic hepatitis C virus NS3/4a protease inhibitor
    ACS Med Chem Lett3, 332-336. PubMed  Europe PubMed DOI  I
  177. Horner,S.M., Park,H.S. and Gale,M., Jr.
    Control of innate immune signaling and membrane targeting by the hepatitis C virus NS3/4A protease are governed by the NS3 helix alpha0
    J Virol86, 3112-3120. PubMed  Europe PubMed DOI
  178. Hotho,D.M., De Bruijne,J., O'Farrell,A.M., Boyea,T., Li,J., Bracken,M., Li,X., Campbell,D., Guler,H.P., Weegink,C.J., Schinkel,J., Molenkamp,R., van de Wetering de Rooij, Van Vliet,A., Janssen,H.L., de Knegt,R.J. and Reesink,H.W.
    Pharmacokinetics and antiviral activity of PHX1766, a novel HCV protease inhibitor, using an accelerated Phase I study design
    Antivir Ther17, 365-375. PubMed  Europe PubMed DOI  I
  179. Jeong,J.K., Szabo,G., Kelly,K. and Diano,S.
    Prolyl carboxypeptidase regulates energy expenditure and the thyroid axis
    Endocrinology153, 683-689. PubMed  Europe PubMed DOI
  180. Kazmierski,W.M., Hamatake,R., Duan,M., Wright,L.L., Smith,G.K., Jarvest,R.L., Ji,J.J., Cooper,J.P., Tallant,M.D., Crosby,R.M., Creech,K., Wang,A., Li,X., Zhang,S., Zhang,Y.K., Liu,Y., Ding,C.Z., Zhou,Y., Plattner,J.J., Baker,S.J., Bu,W. and Liu,L.
    Discovery of novel urea-based hepatitis C protease inhibitors with high potency against protease-inhibitor-resistant mutants
    J Med Chem55, 3021-3026. PubMed  Europe PubMed DOI  I
  181. Kugler,J., Schmelz,S., Gentzsch,J., Haid,S., Pollmann,E., van den Heuvel,J., Franke,R., Pietschmann,T., Heinz,D.W. and Collins,J.
    High affinity peptide inhibitors of the hepatitis C virus NS3-4A protease refractory to common resistant mutants
    J Biol Chem287, 39224-39232. PubMed  Europe PubMed DOI  I
  182. Li,X., Liu,Y., Zhang,Y.K., Plattner,J.J., Baker,S.J., Bu,W., Liu,L., Zhou,Y., Ding,C.Z., Zhang,S., Kazmierski,W.M., Hamatake,R., Duan,M., Wright,L.L., Smith,G.K., Jarvest,R.L., Ji,J.J., Cooper,J.P., Tallant,M.D., Crosby,R.M., Creech,K. and Wang,A.
    Synthesis and antiviral activity of novel HCV NS3 protease inhibitors with P4 capping groups
    Bioorg Med Chem Lett22, 7351-7356. PubMed  Europe PubMed DOI  I
  183. Lim,S.R., Qin,X., Susser,S., Nicholas,J.B., Lange,C., Herrmann,E., Hong,J., Arfsten,A., Hooi,L., Bradford,W., Najera,I., Smith,P., Zeuzem,S., Kossen,K., Sarrazin,C. and Seiwert,S.D.
    Virologic escape during danoprevir (ITMN-191/RG7227) monotherapy is hepatitis C virus subtype dependent and associated with R155K substitution
    Antimicrob Agents Chemother56, 271-279. PubMed  Europe PubMed DOI  I
  184. Matthews,S.J. and Lancaster,J.W.
    Telaprevir: a hepatitis C NS3/4A protease inhibitor
    Clin Ther34, 1857-1882. PubMed  Europe PubMed DOI  I
  185. McPhee,F., Friborg,J., LeVine,S., Chen,C., Falk,P., Yu,F., Hernandez,D., Lee,M.S., Chaniewski,S., Sheaffer,A.K. and Pasquinelli,C.
    Resistance analysis of the hepatitis C virus NS3 protease inhibitor asunaprevir
    Antimicrob Agents Chemother56, 3670-3681. PubMed  Europe PubMed DOI  I
  186. Paolucci,S., Fiorina,L., Piralla,A., Gulminetti,R., Novati,S., Barbarini,G., Sacchi,P., Gatti,M., Dossena,L. and Baldanti,F.
    Naturally occurring mutations to HCV protease inhibitors in treatment-naive patients
    Virol J9, 245-245. PubMed  Europe PubMed DOI  I
  187. Parera,M., Martrus,G., Franco,S., Clotet,B. and Martinez,M.A.
    Canine hepacivirus NS3 serine protease can cleave the human adaptor proteins MAVS and TRIF
    PLoS ONE7, e42481-e42481. PubMed  Europe PubMed DOI
  188. Romano,K.P., Ali,A., Aydin,C., Soumana,D., Ozen,A., Deveau,L.M., Silver,C., Cao,H., Newton,A., Petropoulos,C.J., Huang,W. and Schiffer,C.A.
    The Molecular Basis of Drug Resistance against Hepatitis C Virus NS3/4A Protease Inhibitors
    PLoS Pathog8, e1002832-e1002832. PubMed  Europe PubMed DOI  S  I
  189. Rudd,M.T., McCauley,J.A., Romano,J.J., Butcher,J.W., Bush,K., McIntyre,C.J., Nguyen,K.T., Gilbert,K.F., Lyle,T.A., Holloway,M.K., Wan,B.L., Vacca,J.P., Summa,V., Harper,S., Rowley,M., Carroll,S.S., Burlein,C., DiMuzio,J.M., Gates,A., Graham,D.J., Huang,Q., Ludmerer,S.W., McClain,S., McHale,C., Stahlhut,M., Fandozzi,C., Taylor,A., Trainor,N., Olsen,D.B. and Liverton,N.J.
    Development of potent macrocyclic inhibitors of genotype 3a HCV NS3/4A protease
    Bioorg Med Chem Lett22, 7201-7206. PubMed  Europe PubMed DOI  I
  190. Rudd,M.T., McIntyre,C.J., Romano,J.J., Butcher,J.W., Holloway,M.K., Bush,K., Nguyen,K.T., Gilbert,K.F., Lyle,T.A., Liverton,N.J., Wan,B.L., Summa,V., Harper,S., Rowley,M., Vacca,J.P., Carroll,S.S., Burlein,C., DiMuzio,J.M., Gates,A., Graham,D.J., Huang,Q., Ludmerer,S.W., McClain,S., McHale,C., Stahlhut,M., Fandozzi,C., Taylor,A., Trainor,N., Olsen,D.B. and McCauley,J.A.
    Development of macrocyclic inhibitors of HCV NS3/4A protease with cyclic constrained P2-P4 linkers
    Bioorg Med Chem Lett22, 7207-7213. PubMed  Europe PubMed DOI  I
  191. Saalau-Bethell,S.M., Woodhead,A.J., Chessari,G., Carr,M.G., Coyle,J., Graham,B., Hiscock,S.D., Murray,C.W., Pathuri,P., Rich,S.J., Richardson,C.J., Williams,P.A. and Jhoti,H.
    Discovery of an allosteric mechanism for the regulation of HCV NS3 protein function
    Nat Chem Biol8, 920-925. PubMed  Europe PubMed DOI  I
  192. Sheng,X.C., Casarez,A., Cai,R., Clarke,M.O., Chen,X., Cho,A., Delaney,W.E., Doerffler,E., Ji,M., Mertzman,M., Pakdaman,R., Pyun,H.J., Rowe,T., Wu,Q., Xu,J. and Kim,C.U.
    Discovery of GS-9256: a novel phosphinic acid derived inhibitor of the hepatitis C virus NS3/4A protease with potent clinical activity
    Bioorg Med Chem Lett22, 1394-1396. PubMed  Europe PubMed DOI  I
  193. Sheng,X.C., Appleby,T., Butler,T., Cai,R., Chen,X., Cho,A., Clarke,M.O., Cottell,J., Delaney,W.E., Doerffler,E., Link,J., Ji,M., Pakdaman,R., Pyun,H.J., Wu,Q., Xu,J. and Kim,C.U.
    Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease
    Bioorg Med Chem Lett22, 2629-2634. PubMed  Europe PubMed DOI  I
  194. Shiryaev,S.A., Cheltsov,A.V. and Strongin,A.Y.
    Probing of exosites leads to novel inhibitor scaffolds of HCV NS3/4A proteinase
    PLoS ONE7, e40029-e40029. PubMed  Europe PubMed DOI  I
  195. Shiryaev,S.A., Thomsen,E.R., Cieplak,P., Chudin,E., Cheltsov,A.V., Chee,M.S., Kozlov,I.A. and Strongin,A.Y.
    New details of HCV NS3/4A proteinase functionality revealed by a high-throughput cleavage assay
    PLoS ONE7, e35759-e35759. PubMed  Europe PubMed DOI  P
  196. Steinkuhler,C.
    Hepacivirin
    [ISSN:978-0-12-407742-3]3, 3120-3130. DOI
  197. Summa,V., Ludmerer,S.W., McCauley,J.A., Fandozzi,C., Burlein,C., Claudio,G., Coleman,P.J., DiMuzio,J.M., Ferrara,M., Filippo,M.D., Gates,A.T., Graham,D.J., Harper,S., Hazuda,D.J., Huang,Q., McHale,C., Monteagudo,E., Pucci,V., Rowley,M., Rudd,M.T., Soriano,A., Stahlhut,M.W., Vacca,J.P., Olsen,D.B., Liverton,N.J. and Carroll,S.S.
    MK-5172, a selective inhibitor of hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants
    Antimicrob Agents Chemother58, 4995-4995. PubMed  Europe PubMed DOI  I
  198. Tanwar,S., Trembling,P.M. and Dusheiko,G.M.
    TMC435 for the treatment of chronic hepatitis C
    Expert Opin Investig Drugs21, 1193-1209. PubMed  Europe PubMed DOI  I
  199. Verma,V.A., Rossman,R., Bennett,F., Chen,L., Gavalas,S., Girijavallabhan,V., Huang,Y., Kim,S.H., Kosinski,A., Pinto,P., Rizvi,R., Shankar,B., Tong,L., Velazquez,F., Venkatraman,S., Kozlowski,J., MacCoss,M., Kwong,C.D., Bansal,N., Kezar,H.S.3., Reynolds,R.C., Maddry,J.A., Ananthan,S., Secrist,J.A.3., Li,C., Chase,R., Curry,S., Huang,H.C., Tong,X., Njoroge,F.G. and Arasappan,A.
    Synthesis and SAR of geminal substitutions at the C5' carbosugar position of pyrimidine-derived HCV inhibitors
    Bioorg Med Chem Lett22, 6967-6973. PubMed  Europe PubMed DOI  I
  200. Vermehren,J., Susser,S., Lange,C.M., Forestier,N., Karey,U., Hughes,E., Ralston,R., Tong,X., Zeuzem,S. and Sarrazin,C.
    Mutations selected in the hepatitis C virus NS3 protease domain during sequential treatment with boceprevir with and without pegylated interferon alfa-2b
    J Viral Hepat19, 120-127. PubMed  Europe PubMed DOI  M  I
  201. Welsch,C., Schweizer,S., Shimakami,T., Domingues,F.S., Kim,S., Lemon,S.M. and Antes,I.
    Ketoamide resistance and hepatitis C virus fitness in Val55 variants of the NS3 serine protease
    Antimicrob Agents Chemother56, 1907-1915. PubMed  Europe PubMed DOI  I
  202. Welsch,C., Shimakami,T., Hartmann,C., Yang,Y., Domingues,F.S., Lengauer,T., Zeuzem,S. and Lemon,S.M.
    Peptidomimetic escape mechanisms arise via genetic diversity in the ligand-binding site of the hepatitis c virus NS3/4A serine protease
    Gastroenterology142, 654-663. PubMed  Europe PubMed DOI  I
  203. Xue,W., Pan,D., Yang,Y., Liu,H. and Yao,X.
    Molecular modeling study on the resistance mechanism of HCV NS3/4A serine protease mutants R155K, A156V and D168A to TMC435
    Antiviral Res93, 126-137. PubMed  Europe PubMed DOI  I
  204. Yee,N.K., Wei,X., Busacca,C.A., Zeng,X., Fandrick,D.R., Song,J.J. and Senanayake,C.H.
    9.19 Synthesis of the leading HCV protease inhibitors
    Compr Chirality9, 483-506. DOI  I
  205. Zeuzem,S., Buggisch,P., Agarwal,K., Marcellin,P., Sereni,D., Klinker,H., Moreno,C., Zarski,J.P., Horsmans,Y., Mo,H., Arterburn,S., Knox,S., Oldach,D., McHutchison,J.G., Manns,M.P. and Foster,G.R.
    The protease inhibitor, GS-9256, and non-nucleoside polymerase inhibitor tegobuvir alone, with ribavirin, or pegylated interferon plus ribavirin in hepatitis C
    Hepatology55, 749-758. PubMed  Europe PubMed DOI  I
  206. Zhu,J., Li,Y., Yu,H., Zhang,L., Mao,X. and Hou,T.
    Insight into the structural requirements of narlaprevir-type inhibitors of NS3/NS4A protease based on HQSAR and molecular field analyses
    Comb Chem High Throughput Screen15, 439-450. PubMed  Europe PubMed DOI  I
  207. 2011
  208. Aparicio,E., Franco,S., Parera,M., Andres,C., Tural,C., Clotet,B. and Martinez,M.A.
    Complexity and catalytic efficiency of hepatitis C virus (HCV) NS3 and NS4A protease quasispecies influence responsiveness to treatment with pegylated interferon plus ribavirin in HCV/HIV-coinfected patients
    J Virol85, 5961-5969. PubMed  Europe PubMed DOI
  209. Arnaud,N., Dabo,S., Akazawa,D., Fukasawa,M., Shinkai-Ouchi,F., Hugon,J., Wakita,T. and Meurs,E.F.
    Hepatitis C virus reveals a novel early control in acute immune response
    PLoS Pathog7, e1002289-e1002289. PubMed  Europe PubMed DOI
  210. Binder,J., Tetangco,S., Weinshank,M., Maegley,K., Lingardo,L., Diehl,W., Love,R., Patick,A.K. and Smith,G.J., III
    Development of hepatitis C virus chimeric replicons for identifying broad spectrum NS3 protease inhibitors
    Antiviral Res91, 102-111. PubMed  Europe PubMed DOI  A  I
  211. Clarke,M.O., Chen,X., Cho,A., Delaney,W.E., Doerffler,E., Fardis,M., Ji,M., Mertzman,M., Pakdaman,R., Pyun,H.J., Rowe,T., Yang,C.Y., Sheng,X.C. and Kim,C.U.
    Novel, potent, and orally bioavailable phosphinic acid inhibitors of the hepatitis C virus NS3 protease
    Bioorg Med Chem Lett21, 3568-3572. PubMed  Europe PubMed DOI  I
  212. Desai,M.M., Gong,B., Chan,T., Davey,R.A., Soong,L., Kolokoltsov,A.A. and Sun,J.
    Differential, type I interferon-mediated autophagic trafficking of hepatitis C virus proteins in mouse liver
    Gastroenterology141, 674-685. PubMed  Europe PubMed DOI
  213. Fatima,K., Tahir,M. and Qadri,I.
    Development of robust in vitro serine protease assay based on recombinant Pakistani HCV NS3-4A protease
    Virus Res160, 230-237. PubMed  Europe PubMed DOI  A
  214. Franco,S., Bellido,R., Aparicio,E., Canete,N., Garcia-Retortillo,M., Sola,R., Tural,C., Clotet,B., Paredes,R. and Martinez,M.A.
    Natural prevalence of HCV minority variants that are highly resistant to NS3/4A protease inhibitors
    J Viral Hepat18, e578-e582. PubMed  Europe PubMed DOI  I
  215. Fusco,D.N. and Chung,R.T.
    New protease inhibitors for HCV - help is on the way
    J Hepatol54, 1087-1089. PubMed  Europe PubMed DOI  I
  216. Gottwein,J.M., Scheel,T.K., Jensen,T.B., Ghanem,L. and Bukh,J.
    Differential efficacy of protease inhibitors against HCV genotypes 2a, 3a, 5a, and 6a NS3/4A protease recombinant viruses
    Gastroenterology141, 1067-1079. PubMed  Europe PubMed DOI  I
  217. Hagel,M., Niu,D., St Martin,T., Sheets,M.P., Qiao,L., Bernard,H., Karp,R.M., Zhu,Z., Labenski,M.T., Chaturvedi,P., Nacht,M., Westlin,W.F., Petter,R.C. and Singh,J.
    Selective irreversible inhibition of a protease by targeting a noncatalytic cysteine
    Nat Chem Biol7, 22-24. PubMed  Europe PubMed DOI  I
  218. Hung,M., Wang,R. and Liu,X.
    Preparation of HCV NS3 and NS5B proteins to support small-molecule drug discovery
    Curr Protoc PharmacolChapter 13, PubMed  Europe PubMed DOI  E
  219. Ismail,N.S. and Hattori,M.
    Molecular modeling based approach, synthesis and in vitro assay to new indole inhibitors of hepatitis C NS3/4A serine protease
    Bioorg Med Chem19, 374-383. PubMed  Europe PubMed DOI  I
  220. Jian Rui,L., Yan Bin,W., Shu Yi,S., Hong Shan,C., Jian Dong,J. and Zong-Gen,B.
    Establishment and application of high throughput screening model for hepatitis C virus NS3-4A protease inhibitors in vitro
    Zhongguo Yi Xue Ke Xue Yuan Xue Bao33, 98-101. PubMed  Europe PubMed DOI  A  I
  221. Lampa,A., Ehrenberg,A.E., Vema,A., Kerblom,E., Lindeberg,G., Helena Danielson,U., Karlen,A. and Sandstrom,A.
    P2-P1' macrocyclization of P2 phenylglycine based HCV NS3 protease inhibitors using ring-closing metathesis
    Bioorg Med Chem19, 4917-4927. PubMed  Europe PubMed DOI  I
  222. Lemke,C.T., Goudreau,N., Zhao,S., Hucke,O., Thibeault,D., Llinas-Brunet,M. and White,P.W.
    Combined X-ray, NMR, and kinetic analyses reveal uncommon binding characteristics of the hepatitis C virus NS3-NS4A protease inhibitor BI 201335
    J Biol Chem286, 11434-11443. PubMed  Europe PubMed DOI  I
  223. Liu,Y.H., Ramanathan,L., Malcolm,B., Njoroge,G., Chan,T.Y. and Pramanik,B.N.
    Screening and rank ordering of reversible mechanism-based inhibitors of hepatitis C virus NS3 protease using electrospray ionization mass spectrometry
    J Mass Spectrom46, 764-771. PubMed  Europe PubMed DOI  I
  224. Martin,M.M., Condotta,S.A., Fenn,J., Olmstead,A.D. and Jean,F.
    In-cell selectivity profiling of membrane-anchored and replicase-associated hepatitis C virus NS3-4A protease reveals a common, stringent substrate recognition profile
    Biol Chem392, 927-935. PubMed  Europe PubMed DOI  P
  225. Morikawa,K., Lange,C.M., Gouttenoire,J., Meylan,E., Brass,V., Penin,F. and Moradpour,D.
    Nonstructural protein 3-4A: the Swiss army knife of hepatitis C virus
    J Viral Hepat18, 305-315. PubMed  Europe PubMed DOI  V
  226. Romano,K.P., Laine,J.M., Deveau,L.M., Cao,H., Massi,F. and Schiffer,C.A.
    Molecular mechanisms of viral and host cell substrate recognition by hepatitis C virus NS3/4A protease
    J Virol85, 6106-6116. PubMed  Europe PubMed DOI  P  S
  227. Rudd,M.T., McCauley,J.A., Butcher,J.W., Romano,J.J., McIntyre,C.J., Nguyen,K.T., Gilbert,K.F., Bush,K.J., Holloway,M.K., Swestock,J., Wan,B.L., Carroll,S.S., DiMuzio,J.M., Graham,D.J., Ludmerer,S.W., Stahlhut,M.W., Fandozzi,C.M., Trainor,N., Olsen,D.B., Vacca,J.P. and Liverton,N.J.
    Discovery of MK-1220: a macrocyclic inhibitor of hepatitis C virus NS3/4A protease with improved preclinical plasma exposure
    ACS Med Chem Lett2, 207-212. PubMed  Europe PubMed DOI  I
  228. Schaefer,C.J., Kossen,K., Lim,S.R., Lin,J.H., Pan,L., Bradford,W., Smith,P.F. and Seiwert,S.D.
    Danoprevir monotherapy decreases inflammatory markers in patients with chronic hepatitis C virus infection
    Antimicrob Agents Chemother55, 3125-3132. PubMed  Europe PubMed DOI  I
  229. Schiering,N., D'arcy,A., Villard,F., Simic,O., Kamke,M., Monnet,G., Hassiepen,U., Svergun,D.I., Pulfer,R., Eder,J., Raman,P. and Bodendorf,U.
    A macrocyclic HCV NS3/4A protease inhibitor interacts with protease and helicase residues in the complex with its full-length target
    Proc Natl Acad Sci U S A108, 21052-21056. PubMed  Europe PubMed DOI  S  I
  230. Schultz,B., Yang,H. and Delaney,W.E.
    Biochemical evaluation of HCV NS3 protease inhibitors
    Curr Protoc PharmacolChapter 13, PubMed  Europe PubMed DOI  I
  231. Shapira,A., Gal-Tanamy,M., Nahary,L., Litvak-Greenfeld,D., Zemel,R., Tur-Kaspa,R. and Benhar,I.
    Engineered toxins "zymoxins" are activated by the HCV NS3 protease by removal of an inhibitory protein domain
    PLoS ONE6, e15916-e15916. PubMed  Europe PubMed DOI
  232. Shindo,H., Maekawa,S., Komase,K., Sueki,R., Miura,M., Kadokura,M., Shindo,K., Amemiya,F., Kitamura,T., Nakayama,Y., Inoue,T., Sakamoto,M., Okada,S., Asahina,Y., Izumi,N., Honda,M., Kaneko,S. and Enomoto,N.
    Characterization of naturally occurring protease inhibitor-resistance mutations in genotype 1b hepatitis C virus patients
    Hepatol Int6, 482-490. PubMed  Europe PubMed DOI  I
  233. Srivastava,A.K. and Pandey,A.
    QSAR-based modelling of macrocyclic inhibitors of hepatitis C virus NS3-4A serine protease
    Oxid Commun34, 108-116.  I
  234. Susser,S., Vermehren,J., Forestier,N., Welker,M.W., Grigorian,N., Fuller,C., Perner,D., Zeuzem,S. and Sarrazin,C.
    Analysis of long-term persistence of resistance mutations within the hepatitis C virus NS3 protease after treatment with telaprevir or boceprevir
    J Clin Virol52, 321-327. PubMed  Europe PubMed DOI  I
  235. Thompson,A.J., Locarnini,S.A. and Beard,M.R.
    Resistance to anti-HCV protease inhibitors
    Curr Opin Virol1, 599-606. PubMed  Europe PubMed DOI  I
  236. Vachon,M.L. and Dieterich,D.T.
    The era of direct-acting antivirals has begun: the beginning of the end for HCV?
    Semin Liver Dis31, 399-409. PubMed  Europe PubMed DOI  I
  237. Vallet,S., Viron,F., Henquell,C., Le Guillou-Guillemette,H., Lagathu,G., Abravanel,F., Trimoulet,P., Soussan,P., Schvoerer,E., Rosenberg,A., Gouriou,S., Colson,P., Izopet,J. and Payan,C.
    NS3 protease polymorphism and natural resistance to protease inhibitors in French patients infected with HCV genotypes 1-5
    Antivir Ther16, 1093-1102. PubMed  Europe PubMed DOI  I
  238. Zhu,H. and Briggs,J.M.
    Mechanistic role of NS4A and substrate in the activation of HCV NS3 protease
    Proteins79, 2428-2443. PubMed  Europe PubMed DOI
  239. 2010
  240. Abian,O., Vega,S., Neira,J.L. and Velazquez-Campoy,A.
    Conformational stability of hepatitis C virus NS3 protease
    Biophys J99, 3811-3820. PubMed  Europe PubMed DOI
  241. Avolio,S. and Summa,V.
    Advances in the development of macrocyclic inhibitors of hepatitis C virus NS3-4A protease
    Curr Top Med Chem10, 1403-1422. PubMed  Europe PubMed DOI  I
  242. Bae,A., Sun,S.C., Qi,X., Chen,X., Ku,K., Worth,A., Wong,K.A., Harris,J., Miller,M.D. and Mo,H.
    Susceptibility of treatment-naive hepatitis C virus (HCV) clinical isolates to HCV protease inhibitors
    Antimicrob Agents Chemother54, 5288-5297. PubMed  Europe PubMed DOI  I
  243. Barbotte,L., Ahmed-Belkacem,A., Chevaliez,S., Soulier,A., Hezode,C., Wajcman,H., Bartels,D.J., Zhou,Y., Ardzinski,A., Mani,N., Rao,B.G., George,S., Kwong,A. and Pawlotsky,J.M.
    Characterization of V36C, a novel amino acid substitution conferring hepatitis C virus (HCV) resistance to telaprevir, a potent peptidomimetic inhibitor of HCV protease
    Antimicrob Agents Chemother54, 2681-2683. PubMed  Europe PubMed DOI  M  I
  244. Bennett,F., Huang,Y., Hendrata,S., Lovey,R., Bogen,S.L., Pan,W., Guo,Z., Prongay,A., Chen,K.X., Arasappan,A., Venkatraman,S., Velazquez,F., Nair,L., Sannigrahi,M., Tong,X., Pichardo,J., Cheng,K.C., Girijavallabhan,V.M., Saksena,A.K. and Njoroge,F.G.
    The introduction of P4 substituted 1-methylcyclohexyl groups into boceprevir: a change in direction in the search for a second generation HCV NS3 protease inhibitor
    Bioorg Med Chem Lett20, 2617-2621. PubMed  Europe PubMed DOI  I
  245. Benureau,Y., Warter,L., Malcolm,B.A. and Martin,A.
    A comparative analysis of the substrate permissiveness of HCV and GBV-B NS3/4A proteases reveals genetic evidence for an interaction with NS4B protein during genome replication
    Virology406, 228-240. PubMed  Europe PubMed DOI  P
  246. Bogen,S.L., Arasappan,A., Velazquez,F., Blackman,M., Huelgas,R., Pan,W., Siegel,E., Nair,L.G., Venkatraman,S., Guo,Z., Doll,R., Shih,N.Y. and Njoroge,F.G.
    Discovery of potent sulfonamide P4-capped ketoamide second generation inhibitors of hepatitis C virus NS3 serine protease with favorable pharmacokinetic profiles in preclinical species
    Bioorg Med Chem18, 1854-1865. PubMed  Europe PubMed DOI  I
  247. Chatel-Chaix,L., Baril,M. and Lamarre,D.
    Hepatitis C virus NS3/4A protease inhibitors: a light at the end of the tunnel
    Viruses2, 1752-1765. PubMed  Europe PubMed DOI  I
  248. Cummings,M.D., Lindberg,J., Lin,T.I., de Kock,H., Lenz,O., Lilja,E., Fellander,S., Baraznenok,V., Nystrom,S., Nilsson,M., Vrang,L., Edlund,M., Rosenquist,A., Samuelsson,B., Raboisson,P. and Simmen,K.
    Inside cover: Induced-fit binding of the macrocyclic noncovalent inhibitor TMC435 to its HCV NS3/NS4A protease target
    Angew Chem Int Ed Engl49, 1510-1510. PubMed  Europe PubMed DOI  S  I
  249. Cummings,M.D., Lindberg,J., Lin,T.I., de Kock,H., Lenz,O., Lilja,E., Fellander,S., Baraznenok,V., Nystrom,S., Nilsson,M., Vrang,L., Edlund,M., Rosenquist,A., Samuelsson,B., Raboisson,P. and Simmen,K.
    Induced-fit binding of the macrocyclic noncovalent inhibitor TMC435 to its HCV NS3/NS4A protease target
    Angew Chem Int Ed Engl49, 1652-1655. PubMed  Europe PubMed DOI  S  I
  250. Deutsch,M. and Papatheodoridis,G.V.
    Danoprevir, a small-molecule NS3/4A protease inhibitor for the potential oral treatment of HCV infection
    Curr Opin Investig Drugs11, 951-963. PubMed  Europe PubMed  I
  251. Ding,C.Z., Zhang,Y.K., Li,X., Liu,Y., Zhang,S., Zhou,Y., Plattner,J.J., Baker,S.J., Liu,L., Duan,M., Jarvest,R.L., Ji,J., Kazmierski,W.M., Tallant,M.D., Wright,L.L., Smith,G.K., Crosby,R.M., Wang,A.A., Ni,Z.J., Zou,W. and Wright,J.
    Synthesis and biological evaluations of P4-benzoxaborole-substituted macrocyclic inhibitors of HCV NS3 protease
    Bioorg Med Chem Lett20, 7317-7322. PubMed  Europe PubMed DOI  I
  252. Fu,Q.X., Wang,L.C., Jia,S.Z., Gao,B., Zhou,Y., Du,J., Wang,Y.L., Wang,X.H., Peng,J.C. and Zhan,L.S.
    Screening compounds against HCV based on MAVS/IFN-beta pathway in a replicon model
    World J Gastroenterol16, 5582-5587. PubMed  Europe PubMed DOI  A
  253. Gallo,M., Bottomley,M.J., Pennestri,M., Eliseo,T., Paci,M., Koch,U., Bazzo,R., Summa,V., Carfi,A. and Cicero,D.O.
    Structural characterization of the hepatitis C virus NS3 protease from genotype 3a: the basis of the genotype 1b vs. 3a inhibitor potency shift
    Virology405, 424-438. PubMed  Europe PubMed DOI  I
  254. Kawai,S.H., LaPlante,S.R., Llinas-Brunet,M. and Hucke,O.
    The effect of the P1 side chain on the binding of optimized carboxylate and activated carbonyl inhibitors of the hepatitis C virus NS3 protease
    Future Med Chem2, 1073-1081. PubMed  Europe PubMed DOI  I
  255. Lampa,A., Ehrenberg,A.E., Gustafsson,S.S., Vema,A., Kerblom,E., Lindeberg,G., Karlen,A., Danielson,U.H. and Sandstrom,A.
    Improved P2 phenylglycine-based hepatitis C virus NS3 protease inhibitors with alkenylic prime-side substituents
    Bioorg Med Chem18, 5413-5424. PubMed  Europe PubMed DOI  I
  256. Li,X., Zhang,Y.K., Liu,Y., Zhang,S., Ding,C.Z., Zhou,Y., Plattner,J.J., Baker,S.J., Liu,L., Bu,W., Kazmierski,W.M., Wright,L.L., Smith,G.K., Jarvest,R.L., Duan,M., Ji,J.J., Cooper,J.P., Tallant,M.D., Crosby,R.M., Creech,K., Ni,Z.J., Zou,W. and Wright,J.
    Synthesis of new acylsulfamoyl benzoxaboroles as potent inhibitors of HCV NS3 protease
    Bioorg Med Chem Lett20, 7493-7497. PubMed  Europe PubMed DOI  I
  257. Li,X., Zhang,Y.K., Liu,Y., Ding,C.Z., Zhou,Y., Li,Q., Plattner,J.J., Baker,S.J., Zhang,S., Kazmierski,W.M., Wright,L.L., Smith,G.K., Grimes,R.M., Crosby,R.M., Creech,K.L., Carballo,L.H., Slater,M.J., Jarvest,R.L., Thommes,P., Hubbard,J.A., Convery,M.A., Nassau,P.M., McDowell,W., Skarzynski,T.J., Qian,X., Fan,D., Liao,L., Ni,Z.J., Pennicott,L.E., Zou,W. and Wright,J.
    Novel macrocyclic HCV NS3 protease inhibitors derived from alpha-amino cyclic boronates
    Bioorg Med Chem Lett20, 5695-5700. PubMed  Europe PubMed DOI  S  I
  258. Li,X., Zhang,Y.K., Liu,Y., Ding,C.Z., Li,Q., Zhou,Y., Plattner,J.J., Baker,S.J., Qian,X., Fan,D., Liao,L., Ni,Z.J., White,G.V., Mordaunt,J.E., Lazarides,L.X., Slater,M.J., Jarvest,R.L., Thommes,P., Ellis,M., Edge,C.M., Hubbard,J.A., Somers,D., Rowland,P., Nassau,P., McDowell,B., Skarzynski,T.J., Kazmierski,W.M., Grimes,R.M., Wright,L.L., Smith,G.K., Zou,W., Wright,J. and Pennicott,L.E.
    Synthesis and evaluation of novel alpha-amino cyclic boronates as inhibitors of HCV NS3 protease
    Bioorg Med Chem Lett20, 3550-3556. PubMed  Europe PubMed DOI  I
  259. Liverton,N.J., Carroll,S.S., Dimuzio,J., Fandozzi,C., Graham,D.J., Hazuda,D., Holloway,M.K., Ludmerer,S.W., McCauley,J.A., McIntyre,C.J., Olsen,D.B., Rudd,M.T., Stahlhut,M. and Vacca,J.P.
    MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease
    Antimicrobial Agents Chemother54, 305-311. PubMed  Europe PubMed DOI  I
  260. Llinas-Brunet,M., Bailey,M.D., Goudreau,N., Bhardwaj,P.K., Bordeleau,J., Bos,M., Bousquet,Y., Cordingley,M.G., Duan,J., Forgione,P., Garneau,M., Ghiro,E., Gorys,V., Goulet,S., Halmos,T., Kawai,S.H., Naud,J., Poupart,M.A. and White,P.W.
    Discovery of a potent and selective noncovalent linear inhibitor of the hepatitis C virus NS3 protease (BI 201335)
    J Med Chem53, 6466-6476. PubMed  Europe PubMed DOI  I
  261. Massariol,M.J., Zhao,S., Marquis,M., Thibeault,D. and White,P.W.
    Protease and helicase activities of hepatitis C virus genotype 4, 5, and 6 NS3-NS4A proteins
    Biochem Biophys Res Commun391, 692-697. PubMed  Europe PubMed DOI  I
  262. McCauley,J.A., McIntyre,C.J., Rudd,M.T., Nguyen,K.T., Romano,J.J., Butcher,J.W., Gilbert,K.F., Bush,K.J., Holloway,M.K., Swestock,J., Wan,B.L., Carroll,S.S., DiMuzio,J.M., Graham,D.J., Ludmerer,S.W., Mao,S.S., Stahlhut,M.W., Fandozzi,C.M., Trainor,N., Olsen,D.B., Vacca,J.P. and Liverton,N.J.
    Discovery of vaniprevir (MK-7009), a macrocyclic hepatitis C virus NS3/4a protease inhibitor
    J Med Chem53, 2443-2463. PubMed  Europe PubMed DOI  I
  263. Monteagudo,E., Fonsi,M., Chu,X., Bleasby,K., Evers,R., Pucci,V., Orsale,M.V., Cianetti,S., Ferrara,M., Harper,S., Laufer,R., Rowley,M. and Summa,V.
    The metabolism and disposition of a potent inhibitor of hepatitis C virus NS3/4A protease
    Xenobiotica40, 826-839. PubMed  Europe PubMed DOI  I
  264. Naggie,S., Patel,K. and McHutchison,J.
    Hepatitis C virus directly acting antivirals: current developments with NS3/4A HCV serine protease inhibitors
    J Antimicrob Chemother65, 2063-2069. PubMed  Europe PubMed DOI  I
  265. Nair,L.G., Bogen,S., Doll,R.J., Shih,N.Y. and Njoroge,F.G.
    Synthesis of sterically hindered 3,5,5-trimethyl 2,6-dioxo tetrahydro pyrimidine as HCV protease inhibitors
    Tetrahedron Lett51, 1276-1279. DOI  I
  266. Nair,L.G., Bogen,S., Ruan,S., Pan,W., Pike,R., Tong,X., Cheng,K.C., Guo,Z., Doll,R.J. and Njoroge,F.G.
    Towards the second generation of boceprevir: dithianes as an alternative P2 substituent for 2,2-dimethyl cycloproyl proline in HCV NS3 protease inhibitors
    Bioorg Med Chem Lett20, 1689-1692. PubMed  Europe PubMed DOI  I
  267. Nair,L.G., Sannigrahi,M., Bogen,S., Pinto,P., Chen,K.X., Prongay,A., Tong,X., Cheng,K.C., Girijavallabhan,V. and George Njoroge,F.
    P4 capped amides and lactams as HCV NS3 protease inhibitors with improved potency and DMPK profile
    Bioorg Med Chem Lett20, 567-570. PubMed  Europe PubMed DOI  I
  268. Nilsson,M., Belfrage,A.K., Lindstrom,S., Wahling,H., Lindquist,C., Ayesa,S., Kahnberg,P., Pelcman,M., Benkestock,K., Agback,T., Vrang,L., Terelius,Y., Wikstrom,K., Hamelink,E., Rydergard,C., Edlund,M., Eneroth,A., Raboisson,P., Lin,T.I., de Kock,H., Wigerinck,P., Simmen,K., Samuelsson,B. and Rosenquist,S.
    Synthesis and SAR of potent inhibitors of the hepatitis C virus NS3/4A protease: exploration of P2 quinazoline substituents
    Bioorg Med Chem Lett20, 4004-4011. PubMed  Europe PubMed DOI  I
  269. Ortqvist,P., Vema,A., Ehrenberg,A.E., Dahl,G., Ronn,R., Akerblom,E., Karlen,A., Danielson,U.H. and Sandstrom,A.
    Structure-activity relationships of HCV NS3 protease inhibitors evaluated on the drug-resistant variants A156T and D168V
    Antivir Ther15, 841-852. PubMed  Europe PubMed DOI  I
  270. Ortqvist,P., Gising,J., Ehrenberg,A.E., Vema,A., Borg,A., Karlen,A., Larhed,M., Danielson,U.H. and Sandstrom,A.
    Discovery of achiral inhibitors of the hepatitis C virus NS3 protease based on 2(1H)-pyrazinones
    Bioorg Med Chem18, 6512-6525. PubMed  Europe PubMed DOI  I
  271. Pan,R.Y., Hung,T.M., Kou,Y.H., Chan,N.L., Chang,M.F. and Chang,S.C.
    In trans interaction of hepatitis C virus helicase domains mediates protease activity critical for internal NS3 cleavage and cell transformation
    FEBS Lett584, 482-486. PubMed  Europe PubMed DOI
  272. Peres-da-Silva,A., de Almeida,A.J. and Lampe,E.
    Mutations in hepatitis C virus NS3 protease domain associated with resistance to specific protease inhibitors in antiviral therapy naive patients
    Arch Virol155, 807-811. PubMed  Europe PubMed DOI  M
  273. Pompei,M., Di Francesco,M.E., Pesci,S., Koch,U., Vignetti,S.E., Veneziano,M., Pace,P. and Summa,V.
    Novel P2-P4 macrocyclic inhibitors of HCV NS3/4A protease by P3 succinamide fragment depeptidization strategy
    Bioorg Med Chem Lett20, 168-174. PubMed  Europe PubMed DOI  I
  274. Romano,K.P., Ali,A., Royer,W.E. and Schiffer,C.A.
    Drug resistance against HCV NS3/4A inhibitors is defined by the balance of substrate recognition versus inhibitor binding
    Proc Natl Acad Sci U S A107, 20986-20991. PubMed  Europe PubMed DOI  S  I
  275. Salloum,S., Kluge,S.F., Kim,A.Y., Roggendorf,M. and Timm,J.
    The resistance mutation R155K in the NS3/4A protease of hepatitis C virus also leads the virus to escape from HLA-A*68-restricted CD8 T cells
    Antiviral Res87, 272-275. PubMed  Europe PubMed DOI
  276. Steuber,H. and Hilgenfeld,R.
    Recent advances in targeting viral proteases for the discovery of novel antivirals
    Curr Top Med Chem10, 323-345. PubMed  Europe PubMed DOI  V
  277. Tong,X., Arasappan,A., Bennett,F., Chase,R., Feld,B., Guo,Z., Hart,A., Madison,V., Malcolm,B., Pichardo,J., Prongay,A., Ralston,R., Skelton,A., Xia,E., Zhang,R. and Njoroge,F.G.
    Preclinical characterization of the antiviral activity of SCH 900518 (narlaprevir), a novel mechanism-based inhibitor of hepatitis C virus NS3 protease
    Antimicrob Agents Chemother54, 2365-2370. PubMed  Europe PubMed DOI  I
  278. Velazquez,F., Sannigrahi,M., Bennett,F., Lovey,R.G., Arasappan,A., Bogen,S., Nair,L., Venkatraman,S., Blackman,M., Hendrata,S., Huang,Y., Huelgas,R., Pinto,P., Cheng,K.C., Tong,X., McPhail,A.T. and Njoroge,F.G.
    Cyclic sulfones as novel P3-caps for hepatitis C virus NS3/4A (HCV NS3/4A) protease inhibitors: synthesis and evaluation of inhibitors with improved potency and pharmacokinetic profiles
    J Med Chem53, 3075-3085. PubMed  Europe PubMed DOI  I
  279. Venkatraman,S., Velazquez,F., Wu,W., Blackman,M., Madison,V. and Njoroge,F.G.
    Potent ketoamide inhibitors of HCV NS3 protease derived from quaternized P1 groups
    Bioorg Med Chem Lett20, 2151-2155. PubMed  Europe PubMed DOI  I
  280. White,P.W., Llinas-Brunet,M., Amad,M., Bethell,R.C., Bolger,G., Cordingley,M.G., Duan,J., Garneau,M., Lagace,L., Thibeault,D. and Kukolj,G.
    Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease
    Antimicrob Agents Chemother54, 4611-4618. PubMed  Europe PubMed DOI  I
  281. Zhu,Z., Wilson,A.T., Luxon,B.A., Brown,K.E., Mathahs,M.M., Bandyopadhyay,S., McCaffrey,A.P. and Schmidt,W.N.
    Biliverdin inhibits hepatitis C virus nonstructural 3/4A protease activity: mechanism for the antiviral effects of heme oxygenase?
    Hepatology52, 1897-1905. PubMed  Europe PubMed DOI  I
  282. 2009

  283. Trial watch: protease inhibitors show promise against HCV
    Nat Rev Drug Discov8, 11-11. PubMed  Europe PubMed DOI  I
  284. Abian,O., Neira,J.L. and Velazquez-Campoy,A.
    Thermodynamics of zinc binding to hepatitis C virus NS3 protease: a folding by binding event
    Proteins77, 624-636. PubMed  Europe PubMed DOI
  285. Akhavan,S., Schnuriger,A., Lebray,P., Benhamou,Y., Poynard,T. and Thibault,V.
    Natural variability of NS3 protease in patients infected with genotype 4 hepatitis C virus (HCV): implications for antiviral treatment using specifically targeted antiviral therapy for HCV
    J Infect Dis200, 524-527. PubMed  Europe PubMed DOI  M
  286. Anderson,M.D., Breidinger,S.A. and Woolf,E.J.
    Effect of disease state on ionization during bioanalysis of MK-7009, a selective HCV NS3/NS4 protease inhibitor, in human plasma and human Tween-treated urine by high-performance liquid chromatography with tandem mass spectrometric detection
    J Chromatogr B Analyt Technol Biomed Life Sci877, 1047-1056. PubMed  Europe PubMed DOI  I
  287. Arasappan,A., Padilla,A.I., Jao,E., Bennett,F., Bogen,S.L., Chen,K.X., Pike,R.E., Sannigrahi,M., Soares,J., Venkatraman,S., Vibulbhan,B., Saksena,A.K., Girijavallabhan,V., Tong,X., Cheng,K.C. and Njoroge,F.G.
    Toward second generation hepatitis C virus NS3 serine protease inhibitors: discovery of novel P4 modified analogues with improved potency and pharmacokinetic profile
    J Med Chem52, 2806-2817. PubMed  Europe PubMed DOI  I
  288. Avolio,S., Robertson,K., Hernando,J.I., Dimuzio,J. and Summa,V.
    Inhibitors of hepatitis C virus NS3/4A: alpha-ketoamide based macrocyclic inhibitors
    Bioorg Med Chem Lett19, 2295-2298. PubMed  Europe PubMed DOI  I
  289. Bermudez-Aguirre,A.D., Padilla-Noriega,L., Zenteno,E. and Reyes-Leyva,J.
    Identification of amino acid variants in the hepatitis C virus non-structural protein 4A
    Tohoku J Exp Med218, 165-175. PubMed  Europe PubMed DOI
  290. Bogen,S.L., Pan,W., Ruan,S., Nair,L.G., Arasappan,A., Bennett,F., Chen,K.X., Jao,E., Venkatraman,S., Vibulbhan,B., Liu,R., Cheng,K.C., Guo,Z., Tong,X., Saksena,A.K., Girijavallabhan,V. and Njoroge,F.G.
    Toward the back-up of boceprevir (SCH 503034): discovery of new extended P4-capped ketoamide inhibitors of hepatitis C virus NS3 serine protease with improved potency and pharmacokinetic profiles
    J Med Chem52, 3679-3688. PubMed  Europe PubMed DOI  I
  291. Boloor,A., Hanway,D., Joshi,M., Winn,D.T., Mendez,G., Walls,M., Wei,P., Qian,F., Zhang,X., Zhang,Y., Hepperle,M.E., Li,X., Campbell,D.A. and Betancort,J.M.
    Synthesis and antiviral activity of HCV NS3/4A peptidomimetic boronic acid inhibitors
    Bioorg Med Chem Lett19, 5708-5711. PubMed  Europe PubMed DOI  I
  292. Brenndorfer,E.D., Karthe,J., Frelin,L., Cebula,P., Erhardt,A., Schulte am Esch,J., Hengel,H., Bartenschlager,R., Sallberg,M., Haussinger,D. and Bode,J.G.
    Nonstructural 3/4A protease of hepatitis C virus activates epithelial growth factor-induced signal transduction by cleavage of the T-cell protein tyrosine phosphatase
    Hepatology49, 1810-1820. PubMed  Europe PubMed DOI
  293. Chase,R., Skelton,A., Xia,E., Curry,S., Liu,S., McMonagle,P., Huang,H.C. and Tong,X.
    A novel HCV NS3 protease mutation selected by combination treatment of the protease inhibitor boceprevir and NS5B polymerase inhibitors
    Antiviral Res84, 178-184. PubMed  Europe PubMed DOI  I
  294. Chen,K.X. and Njoroge,F.G.
    A review of HCV protease inhibitors
    Curr Opin Investig Drugs10, 821-837. PubMed  Europe PubMed  I
  295. Chen,K.X., Vibulbhan,B., Yang,W., Nair,L.G., Tong,X., Cheng,K.C. and Njoroge,F.G.
    Novel potent inhibitors of hepatitis C virus (HCV) NS3 protease with cyclic sulfonyl P3 cappings
    Bioorg Med Chem Lett19, 1105-1109. PubMed  Europe PubMed DOI  I
  296. Chen,K.X., Nair,L., Vibulbhan,B., Yang,W., Arasappan,A., Bogen,S.L., Venkatraman,S., Bennett,F., Pan,W., Blackman,M.L., Padilla,A.I., Prongay,A., Cheng,K.C., Tong,X., Shih,N.Y. and Njoroge,F.G.
    Second-generation highly potent and selective inhibitors of the hepatitis C virus NS3 serine protease
    J Med Chem52, 1370-1379. PubMed  Europe PubMed DOI  S  I
  297. Dahl,G., Arenas,O.G. and Danielson,U.H.
    Hepatitis C virus NS3 protease is activated by low concentrations of protease inhibitors
    Biochemistry48, 11592-11602. PubMed  Europe PubMed DOI
  298. Di Francesco,M.E., Dessole,G., Nizi,E., Pace,P., Koch,U., Fiore,F., Pesci,S., Di Muzio,J., Monteagudo,E., Rowley,M. and Summa,V.
    Novel macrocyclic inhibitors of hepatitis C NS3/4A protease featuring a 2-amino-1,3-thiazole as a P4 carbamate replacement
    J Med Chem52, 7014-7028. PubMed  Europe PubMed DOI  I
  299. Flores,M.V., Strawbridge,J., Ciaramella,G. and Corbau,R.
    HCV-NS3 inhibitors: determination of their kinetic parameters and mechanism
    Biochim Biophys Acta1794, 1441-1448. PubMed  Europe PubMed DOI  I
  300. Gallo,M., Pennestri,M., Bottomley,M.J., Barbato,G., Eliseo,T., Paci,M., Narjes,F., De Francesco,R., Summa,V., Koch,U., Bazzo,R. and Cicero,D.O.
    Binding of a noncovalent inhibitor exploiting the S' region stabilizes the hepatitis C virus NS3 protease conformation in the absence of cofactor
    J Mol Biol385, 1142-1155. PubMed  Europe PubMed DOI  S  I
  301. Harper,S., Ferrara,M., Crescenzi,B., Pompei,M., Palumbi,M.C., DiMuzio,J.M., Donghi,M., Fiore,F., Koch,U., Liverton,N.J., Pesci,S., Petrocchi,A., Rowley,M., Summa,V. and Gardelli,C.
    Inhibitors of the hepatitis C virus NS3 protease with basic amine functionality at the P3-amino acid N-terminus: discovery and optimization of a new series of P2-P4 macrocycles
    J Med Chem52, 4820-4837. PubMed  Europe PubMed DOI  I
  302. Kawai,S.H., Aubry,N., Duceppe,J.S., Llinas-Brunet,M. and LaPlante,S.R.
    Dimethylthiazolidine carboxylic acid as a rigid P3 unit in inhibitors of serine proteases: application to two targets
    Chem Biol Drug Des74, 517-522. PubMed  Europe PubMed DOI  I
  303. Li,K.
    Regulation of interferon regulatory factor 3-dependent innate immunity by the HCV NS3/4A protease
    Methods Mol Biol510, 211-226. PubMed  Europe PubMed DOI
  304. Lin,T.I., Lenz,O., Fanning,G., Verbinnen,T., Delouvroy,F., Scholliers,A., Vermeiren,K., Rosenquist,A., Edlund,M., Samuelsson,B., Vrang,L., de Kock,H., Wigerinck,P., Raboisson,P. and Simmen,K.
    In vitro activity and preclinical profile of TMC435350, a potent hepatitis C virus protease inhibitor
    Antimicrobial Agents Chemother53, 1377-1385. PubMed  Europe PubMed DOI  I
  305. Misialek,S., Rajagopalan,R., Stevens,S.K., Beigelman,L., Seiwert,S.D. and Kossen,K.
    Optimization of the multiple enzymatic activities of the hepatitis C virus NS3 protein
    Anal Biochem394, 138-140. PubMed  Europe PubMed DOI
  306. Phuong,d.T., Ma,C.M., Hattori,M. and Jin,J.S.
    Inhibitory effects of antrodins A-E from Antrodia cinnamomea and their metabolites on hepatitis C virus protease
    Phytother Res23, 582-584. PubMed  Europe PubMed DOI  I
  307. Pyun,H.J., Chaudhary,K., Somoza,J.R., Sheng,X.C. and Kim,C.U.
    Synthesis and resolution of diethyl (1S,2S)-1-amino-2-vinylcyclopropane-1-phosphonate for HCV NS3 protease inhibitors
    Tetrahedron Lett50, 3833-3835. DOI  I
  308. Rajagopalan,R., Misialek,S., Stevens,S.K., Myszka,D.G., Brandhuber,B.J., Ballard,J.A., Andrews,S.W., Seiwert,S.D. and Kossen,K.
    Inhibition and binding kinetics of the hepatitis C virus NS3 protease inhibitor ITMN-191 reveals tight binding and slow dissociative behavior
    Biochemistry48, 2559-2568. PubMed  Europe PubMed DOI  I
  309. Rognvaldsson,T., Etchells,T.A., You,L., Garwicz,D., Jarman,I. and Lisboa,P.J.
    How to find simple and accurate rules for viral protease cleavage specificities
    BMC Bioinformatics10, 149-149. PubMed  Europe PubMed DOI  P
  310. Sabariegos,R., Picazo,F., Domingo,B., Franco,S., Martinez,M.A. and Llopis,J.
    Fluorescence resonance energy transfer-based assay for characterization of hepatitis C virus NS3-4A protease activity in live cells
    Antimicrobial Agents Chemother53, 728-734. PubMed  Europe PubMed DOI  A
  311. Sheng,X.C., Pyun,H.J., Chaudhary,K., Wang,J., Doerffler,E., Fleury,M., McMurtrie,D., Chen,X., Delaney,W.E. and Kim,C.U.
    Discovery of novel phosphonate derivatives as hepatitis C virus NS3 protease inhibitors
    Bioorg Med Chem Lett19, 3453-3457. PubMed  Europe PubMed DOI  I
  312. Tsantrizos,Y.S.
    TMC-435, an NS3/4A protease inhibitor for the treatment of HCV infection
    Curr Opin Investig Drugs10, 871-881. PubMed  Europe PubMed  I
  313. Venkatraman,S. and Njoroge,F.G.
    Macrocyclic inhibitors of HCV NS3 protease
    Expert Opin Ther Pat19, 1277-1303. PubMed  Europe PubMed DOI  I
  314. Venkatraman,S., Wu,W., Shih,N.Y. and George Njoroge,F.
    Potent aza-peptide derived inhibitors of HCV NS3 protease
    Bioorg Med Chem Lett19, 4760-4763. PubMed  Europe PubMed DOI  I
  315. Venkatraman,S., Blackman,M., Wu,W., Nair,L., Arasappan,A., Padilla,A., Bogen,S., Bennett,F., Chen,K., Pichardo,J., Tong,X., Prongay,A., Cheng,K.C., Girijavallabhan,V. and George Njoroge,F.
    Discovery of novel P3 sulfonamide-capped inhibitors of HCV NS3 protease. Inhibitors with improved cellular potencies
    Bioorg Med Chem17, 4486-4495. PubMed  Europe PubMed DOI  I
  316. Venkatraman,S., Wu,W., Prongay,A., Girijavallabhan,V. and George Njoroge,F.
    Potent inhibitors of HCV-NS3 protease derived from boronic acids
    Bioorg Med Chem Lett19, 180-183. PubMed  Europe PubMed DOI  S  I
  317. Venkatraman,S., Velazquez,F., Wu,W., Blackman,M., Chen,K.X., Bogen,S., Nair,L., Tong,X., Chase,R., Hart,A., Agrawal,S., Pichardo,J., Prongay,A., Cheng,K.C., Girijavallabhan,V., Piwinski,J., Shih,N.Y. and Njoroge,F.G.
    Discovery and structure-activity relationship of P1-P3 ketoamide derived macrocyclic inhibitors of hepatitis C virus NS3 protease
    J Med Chem52, 336-346. PubMed  Europe PubMed DOI  I
  318. Wang,X.P., Li,F.J., Deng,L., Nagano-Fujii,M., An,C., Jiang,D., Kitayama,K. and Hotta,H.
    Hepatitis C virus NS3/4A with different secondary structures at amino-terminus has different serine protease activities and inhibitory activities on host cell functions
    Zhonghua Yi Xue Za Zhi89, 2649-2653. DOI
  319. Wang,X.P., Li,F.J., Deng,L., Nagano-Fujii,M., An,C., Jiang,D., Kitayama,K. and Hotta,H.
    [Hepatitis C virus NS3/4A with different secondary structures at amino-terminus has different serine protease activities and inhibitory activities on host cell]
    Zhonghua Yi Xue Za Zhi89, 2649-2653. PubMed  Europe PubMed
  320. 2008
  321. Beran,R.K. and Pyle,A.M.
    Hepatitis C viral NS3-4A protease activity is enhanced by the NS3 helicase
    J Biol Chem283, 29929-29937. PubMed  Europe PubMed DOI
  322. Bogen,S., Arasappan,A., Pan,W., Ruan,S., Padilla,A., Saksena,A.K., Girijavallabhan,V. and Njoroge,F.G.
    Hepatitis C virus NS3-4A serine protease inhibitors: SAR of new P1 derivatives of SCH 503034
    Bioorg Med Chem Lett18, 4219-4223. PubMed  Europe PubMed DOI  I
  323. Chen,K.X., Vibulbhan,B., Yang,W., Cheng,K.C., Liu,R., Pichardo,J., Butkiewicz,N. and Njoroge,F.G.
    Potent and selective small molecule NS3 serine protease inhibitors of hepatitis C virus with dichlorocyclopropylproline as P2 residue
    Bioorg Med Chem16, 1874-1883. PubMed  Europe PubMed DOI  I
  324. Cubero,M., Esteban,J.I., Otero,T., Sauleda,S., Bes,M., Esteban,R., Guardia,J. and Quer,J.
    Naturally occurring NS3-protease-inhibitor resistant mutant A156T in the liver of an untreated chronic hepatitis C patient
    Virology370, 237-245. PubMed  Europe PubMed DOI
  325. Franco,S., Clotet,B. and Martinez,M.A.
    A wide range of NS3/4A protease catalytic efficiencies in HCV-infected individuals
    Virus Res131, 260-270. PubMed  Europe PubMed DOI
  326. Ismail,N.S., El Dine,R.S., Hattori,M., Takahashi,K. and Ihara,M.
    Computer based design, synthesis and biological evaluation of novel indole derivatives as HCV NS3-4A serine protease inhibitors
    Bioorg Med Chem16, 7877-7887. PubMed  Europe PubMed DOI  I
  327. Kawai,S.H., Bailey,M.D., Halmos,T., Forgione,P., LaPlante,S.R., Llinas-Brunet,M., Naud,J. and Goudreau,N.
    The use of chemical double-mutant cycles in biomolecular recognition studies: application to HCV NS3 protease inhibitors
    ChemMedChem3, 1654-1657. PubMed  Europe PubMed DOI  I
  328. Kuntzen,T., Timm,J., Berical,A., Lennon,N., Berlin,A.M., Young,S.K., Lee,B., Heckerman,D., Carlson,J., Reyor,L.L., Kleyman,M., McMahon,C.M., Birch,C., Schulze Zur Wiesch,J., Ledlie,T., Koehrsen,M., Kodira,C., Roberts,A.D., Lauer,G.M., Rosen,H.R., Bihl,F., Cerny,A., Spengler,U., Liu,Z., Kim,A.Y., Xing,Y., Schneidewind,A., Madey,M.A., Fleckenstein,J.F., Park,V.M., Galagan,J.E., Nusbaum,C., Walker,B.D., Lake-Bakaar,G.V., Daar,E.S., Jacobson,I.M., Gomperts,E.D., Edlin,B.R., Donfield,S.M., Chung,R.T., Talal,A.H., Marion,T., Birren,B.W., Henn,M.R. and Allen,T.M.
    Naturally occurring dominant resistance mutations to hepatitis C virus protease and polymerase inhibitors in treatment-naive patients
    Hepatology48, 1769-1778. PubMed  Europe PubMed DOI  I
  329. Kwong,A.D., McNair,L., Jacobson,I. and George,S.
    Recent progress in the development of selected hepatitis C virus NS3.4A protease and NS5B polymerase inhibitors
    Curr Opin Pharmacol8, 522-531. PubMed  Europe PubMed DOI  V  I
  330. Lei,Y.F., Yin,W., Yang,J., Lv,X., Wei,S.H., An,Q.X., Hu,X.B. and Xu,Z.K.
    Development of a cell-based assay for monitoring hepatitis C virus NS3/4A protease activity
    Acta Virol52, 133-141. PubMed  Europe PubMed  A
  331. Li,C., Liu,T., Broske,L., Brisson,J.M., Uss,A.S., Njoroge,F.G., Morrison,R.A. and Cheng,K.C.
    Permeability evaluation of peptidic HCV protease inhibitors in Caco-2 cells-correlation with in vivo absorption predicted in humans
    Biochem Pharmacol76, 1757-1764. PubMed  Europe PubMed DOI  I
  332. Liang,Y., Ishida,H., Lenz,O., Lin,T.I., Nyanguile,O., Simmen,K., Pyles,R.B., Bourne,N., Yi,M., Li,K. and Lemon,S.M.
    Antiviral suppression vs restoration of RIG-I signaling by hepatitis C protease and polymerase inhibitors
    Gastroenterology135, 1710-1718. PubMed  Europe PubMed DOI  I
  333. Liverton,N.J., Holloway,M.K., McCauley,J.A., Rudd,M.T., Butcher,J.W., Carroll,S.S., Dimuzio,J., Fandozzi,C., Gilbert,K.F., Mao,S.S., McIntyre,C.J., Nguyen,K.T., Romano,J.J., Stahlhut,M., Wan,B.L., Olsen,D.B. and Vacca,J.P.
    Molecular modeling based approach to potent P2-P4 macrocyclic inhibitors of hepatitis C NS3/4A protease
    J Am Chem Soc130, 4607-4609. PubMed  Europe PubMed DOI  I
  334. Lopez-Labrador,F.X.
    Hepatitis C virus NS3/4A protease inhibitors
    Recent Patents Anti-Infect Drug Disc3, 157-167. PubMed  Europe PubMed  I
  335. Lopez-Labrador,F.X., Moya,A. and Gonzalez-Candelas,F.
    Mapping natural polymorphisms of hepatitis C virus NS3/4A protease and antiviral resistance to inhibitors in worldwide isolates
    Antivir Ther13, 481-494. PubMed  Europe PubMed  I
  336. Mao,S.S., Dimuzio,J., McHale,C., Burlein,C., Olsen,D. and Carroll,S.S.
    A time-resolved, internally quenched fluorescence assay to characterize inhibition of hepatitis C virus nonstructural protein 3-4A protease at low enzyme concentrations
    Anal Biochem373, 1-8. PubMed  Europe PubMed DOI  A
  337. McCauley,J.A., Rudd,M.T., Nguyen,K.T., McIntyre,C.J., Romano,J.J., Bush,K.J., Varga,S.L., Ross,C.W., III, Carroll,S.S., Dimuzio,J., Stahlhut,M.W., Olsen,D.B., Lyle,T.A., Vacca,J.P. and Liverton,N.J.
    Bismacrocyclic inhibitors of hepatitis C NS3/4a protease
    Angew Chem Int Ed Engl47, 9104-9107. PubMed  Europe PubMed DOI  I
  338. Naud,J., Lemke,C., Goudreau,N., Beaulieu,E., White,P.D., Llinas-Brunet,M. and Forgione,P.
    Potent triazolyl-proline-based inhibitors of HCV NS3 protease
    Bioorg Med Chem Lett18, 3400-3404. PubMed  Europe PubMed DOI  I
  339. Njoroge,F.G., Chen,K.X., Shih,N.Y. and Piwinski,J.J.
    Challenges in modern drug discovery: a case study of boceprevir, an HCV protease inhibitor for the treatment of hepatitis C virus infection
    Acc Chem Res41, 50-59. PubMed  Europe PubMed DOI  I
  340. Nurbo,J., Peterson,S.D., Dahl,G., Helena Danielson,U., Karlen,A. and Sandstrom,A.
    beta-Amino acid substitutions and structure-based CoMFA modeling of hepatitis C virus NS3 protease inhibitors
    Bioorg Med Chem16, 5590-5605. PubMed  Europe PubMed DOI  I
  341. Raboisson,P., Lin,T.I., Kock,H., Vendeville,S., Vreken,W.V., McGowan,D., Tahri,A., Hu,L., Lenz,O., Delouvroy,F., Surleraux,D., Wigerinck,P., Nilsson,M., Rosenquist,S., Samuelsson,B. and Simmen,K.
    Discovery of novel potent and selective dipeptide hepatitis C virus NS3/4A serine protease inhibitors
    Bioorg Med Chem Lett18, 5095-5100. PubMed  Europe PubMed DOI  I
  342. Raboisson,P., de Kock,H., Rosenquist,A., Nilsson,M., Salvador-Oden,L., Lin,T.I., Roue,N., Ivanov,V., Wahling,H., Wickstrom,K., Hamelink,E., Edlund,M., Vrang,L., Vendeville,S., Van de Vreken,W., McGowan,D., Tahri,A., Hu,L., Boutton,C., Lenz,O., Delouvroy,F., Pille,G., Surleraux,D., Wigerinck,P., Samuelsson,B. and Simmen,K.
    Structure-activity relationship study on a novel series of cyclopentane-containing macrocyclic inhibitors of the hepatitis C virus NS3/4A protease leading to the discovery of TMC435350
    Bioorg Med Chem Lett18, 4853-4858. PubMed  Europe PubMed DOI  I
  343. Randolph,J.T., Zhang,X., Huang,P.P., Klein,L.L., Kurtz,K.A., Konstantinidis,A.K., He,W., Kati,W.M. and Kempf,D.J.
    Synthesis, antiviral activity, and conformational studies of a P3 aza-peptide analog of a potent macrocyclic tripeptide HCV protease inhibitor
    Bioorg Med Chem Lett18, 2745-2750. PubMed  Europe PubMed DOI  I
  344. Ronn,R., Lampa,A., Peterson,S.D., Gossas,T., Akerblom,E., Danielson,U.H., Karlen,A. and Sandstrom,A.
    Hepatitis C virus NS3 protease inhibitors comprising a novel aromatic P1 moiety
    Bioorg Med Chem16, 2955-2967. PubMed  Europe PubMed DOI  I
  345. Saito,T. and Gale,M., Jr.
    Regulation of innate immunity against hepatitis C virus infection
    Hepatol Res38, 115-122. PubMed  Europe PubMed DOI
  346. Seiwert,S.D., Andrews,S.W., Jiang,Y., Serebryany,V., Tan,H., Kossen,K., Rajagopalan,P.T., Misialek,S., Stevens,S.K., Stoycheva,A., Hong,J., Lim,S.R., Qin,X., Rieger,R., Condroski,K.R., Zhang,H., Do,M.G., Lemieux,C., Hingorani,G.P., Hartley,D.P., Josey,J.A., Pan,L., Beigelman,L. and Blatt,L.M.
    Preclinical characteristics of the hepatitis C virus NS3/4A protease inhibitor ITMN-191 (R7227)
    Antimicrobial Agents Chemother52, 4432-4441. PubMed  Europe PubMed DOI  I
  347. Tong,X., Bogen,S., Chase,R., Girijavallabhan,V., Guo,Z., Njoroge,F.G., Prongay,A., Saksena,A., Skelton,A., Xia,E. and Ralston,R.
    Characterization of resistance mutations against HCV ketoamide protease inhibitors
    Antiviral Res77, 177-185. PubMed  Europe PubMed DOI  I
  348. Wei,H.Y., Lu,C.S. and Lin,T.H.
    Exploring the P2 and P3 ligand binding features for hepatitis C virus NS3 protease using some 3D QSAR techniques
    J Mol Graph Model26, 1131-1144. PubMed  Europe PubMed DOI  I
  349. Welsch,C., Domingues,F.S., Susser,S., Antes,I., Hartmann,C., Mayr,G., Schlicker,A., Sarrazin,C., Albrecht,M., Zeuzem,S. and Lengauer,T.
    Molecular basis of telaprevir resistance due to V36 and T54 mutations in the NS3-4A protease of the hepatitis C virus
    Genome Biol9, R16-R16. PubMed  Europe PubMed DOI  I
  350. Zhou,Y., Bartels,D.J., Hanzelka,B.L., Muh,U., Wei,Y., Chu,H.M., Tigges,A.M., Brennan,D.L., Rao,B.G., Swenson,L., Kwong,A.D. and Lin,C.
    Phenotypic characterization of resistant Val36 variants of hepatitis C virus NS3-4A serine protease
    Antimicrob Agents Chemother52, 110-120. PubMed  Europe PubMed DOI  S  I
  351. 2007
  352. Back,M., Johansson,P.O., Wangsell,F., Thorstensson,F., Kvarnstrom,I., Ayesa,S., Wahling,H., Pelcman,M., Jansson,K., Lindstrom,S., Wallberg,H., Classon,B., Rydergard,C., Vrang,L., Hamelink,E., Hallberg,A., Rosenquist,S. and Samuelsson,B.
    Novel potent macrocyclic inhibitors of the hepatitis C virus NS3 protease: use of cyclopentane and cyclopentene P2-motifs
    Bioorg Med Chem15, 7184-7202. PubMed  Europe PubMed DOI  I
  353. Beran,R.K., Serebrov,V. and Pyle,A.M.
    The serine protease domain of hepatitis C viral NS3 activates RNA helicase activity by promoting the binding of RNA substrate
    J Biol Chem282, 34913-34920. PubMed  Europe PubMed DOI
  354. Dahl,G., Sandstrom,A., Akerblom,E. and Danielson,U.H.
    Resistance profiling of hepatitis C virus protease inhibitors using full-length NS3
    Antivir Ther12, 733-740. PubMed  Europe PubMed  I
  355. Dahl,G., Sandstrom,A., Akerblom,E. and Danielson,U.H.
    Effects on protease inhibition by modifying of helicase residues in hepatitis C virus nonstructural protein 3
    FEBS J274, 5979-5986. PubMed  Europe PubMed DOI
  356. Forestier,N., Reesink,H.W., Weegink,C.J., McNair,L., Kieffer,T.L., Chu,H.M., Purdy,S., Jansen,P.L. and Zeuzem,S.
    Antiviral activity of telaprevir (VX-950) and peginterferon alfa-2a in patients with hepatitis C
    Hepatology46, 640-648. PubMed  Europe PubMed DOI  I
  357. Franco,S., Parera,M., Aparicio,E., Clotet,B. and Martinez,M.A.
    Genetic and catalytic efficiency structure of an HCV protease quasispecies
    Hepatology45, 899-910. PubMed  Europe PubMed DOI
  358. Konstantinidis,A.K., Richardson,P.L., Kurtz,K.A., Tripathi,R., Chen,C.M., Huang,P., Randolph,J., Towne,D., Donnelly,J., Warrior,U., Middleton,T. and Kati,W.M.
    Longer wavelength fluorescence resonance energy transfer depsipeptide substrates for hepatitis C virus NS3 protease
    Anal Biochem368, 156-167. PubMed  Europe PubMed DOI  A
  359. Li,X., Zhang,W., Qiao,X. and Xu,X.
    Prediction of binding for a kind of non-peptic HCV NS3 serine protease inhibitors from plants by molecular docking and MM-PBSA method
    Bioorg Med Chem15, 220-226. PubMed  Europe PubMed DOI  I
  360. Liu,R., Abid,K., Pichardo,J., Pazienza,V., Ingravallo,P., Kong,R., Agrawal,S., Bogen,S., Saksena,A., Cheng,K.C., Prongay,A., Njoroge,F.G., Baroudy,B.M. and Negro,F.
    In vitro antiviral activity of SCH446211 (SCH6), a novel inhibitor of the hepatitis C virus NS3 serine protease
    J Antimicrob Chemother59, 51-58. PubMed  Europe PubMed DOI  I
  361. Oliva,C., Rodriguez,A., Gonzalez,M. and Yang,W.
    A quantum mechanics/molecular mechanics study of the reaction mechanism of the hepatitis C virus NS3 protease with the NS5A/5B substrate
    Proteins66, 444-455. PubMed  Europe PubMed DOI
  362. Ortqvist,P., Peterson,S.D., Kerblom,E., Gossas,T., Sabnis,Y.A., Fransson,R., Lindeberg,G., Helena Danielson,U., Karlen,A. and Sandstrom,A.
    Phenylglycine as a novel P2 scaffold in hepatitis C virus NS3 protease inhibitors
    Bioorg Med Chem15, 1448-1474. PubMed  Europe PubMed DOI  I
  363. Perni,R.B., Chandorkar,G., Cottrell,K.M., Gates,C.A., Lin,C., Lin,K., Luong,Y.P., Maxwell,J.P., Murcko,M.A., Pitlik,J., Rao,G., Schairer,W.C., Van Drie,J. and Wei,Y.
    Inhibitors of hepatitis C virus NS3.4A protease. Effect of P4 capping groups on inhibitory potency and pharmacokinetics
    Bioorg Med Chem Lett17, 3406-3411. PubMed  Europe PubMed DOI  I
  364. Poliakov,A., Sandstrom,A., Akerblom,E. and Danielson,U.H.
    Mechanistic studies of electrophilic protease inhibitors of full length hepatic C virus (HCV) NS3
    J Enzyme Inhib Med Chem22, 191-199. PubMed  Europe PubMed DOI  I
  365. Rodriguez,A., Oliva,C., Gonzalez,M., van der Kamp,M. and Mulholland,A.J.
    Comparison of different quantum mechanical/molecular mechanics boundary treatments in the reaction of the hepatitis C Virus NS3 protease with the NS5A/5B substrate
    J Phys Chem B111, 12909-12915. PubMed  Europe PubMed DOI
  366. Ronn,R., Gossas,T., Sabnis,Y.A., Daoud,H., Kerblom,E., Danielson,U.H. and Sandstrom,A.
    Evaluation of a diverse set of potential P1 carboxylic acid bioisosteres in hepatitis C virus NS3 protease inhibitors
    Bioorg Med Chem15, 4057-4068. PubMed  Europe PubMed DOI  T  I
  367. Sarrazin,C., Kieffer,T.L., Bartels,D., Hanzelka,B., Muh,U., Welker,M., Wincheringer,D., Zhou,Y., Chu,H.M., Lin,C., Weegink,C., Reesink,H., Zeuzem,S. and Kwong,A.D.
    Dynamic hepatitis C virus genotypic and phenotypic changes in patients treated with the protease inhibitor telaprevir
    Gastroenterology132, 1767-1777. PubMed  Europe PubMed DOI  I
  368. Sarrazin,C., Rouzier,R., Wagner,F., Forestier,N., Larrey,D., Gupta,S.K., Hussain,M., Shah,A., Cutler,D., Zhang,J. and Zeuzem,S.
    SCH 503034, a novel hepatitis C virus protease inhibitor, plus pegylated interferon alpha-2b for genotype 1 nonresponders
    Gastroenterology132, 1270-1278. PubMed  Europe PubMed DOI  I
  369. Sulkowski,M.S.
    Specific targeted antiviral therapy for hepatitis C
    Curr Gastroenterol Rep9, 5-13. PubMed  Europe PubMed DOI  V  I
  370. Thorstensson,F., Wangsell,F., Kvarnstrom,I., Vrang,L., Hamelink,E., Jansson,K., Hallberg,A., Rosenquist,S. and Samuelsson,B.
    Synthesis of novel potent hepatitis C virus NS3 protease inhibitors: discovery of 4-hydroxy-cyclopent-2-ene-1,2-dicarboxylic acid as a N-acyl-l-hydroxyproline bioisostere
    Bioorg Med Chem15, 827-838. PubMed  Europe PubMed DOI  I
  371. Velazquez,F., Venkatraman,S., Wu,W., Blackman,M., Prongay,A., Girijavallabhan,V., Shih,N.Y. and Njoroge,F.G.
    Application of ring-closing metathesis for the synthesis of macrocyclic peptidomimetics as inhibitors of HCV NS3 protease
    Org Lett9, 3061-3064. PubMed  Europe PubMed DOI  I
  372. Venkatraman,S. and Njoroge,F.G.
    Macrocyclic inhibitors of HCV NS3-4A protease: design and structure activity relationship
    Curr Top Med Chem7, 1290-1301. PubMed  Europe PubMed DOI  V  S  I
  373. Yang,Z.R.
    A probabilistic peptide machine for predicting hepatitis C virus protease cleavage sites
    IEEE Trans Inf Technol Biomed11, 593-595. PubMed  Europe PubMed DOI  P
  374. Zhou,Y., Muh,U., Hanzelka,B.L., Bartels,D.J., Wei,Y., Rao,B.G., Brennan,D.L., Tigges,A.M., Swenson,L., Kwong,A.D. and Lin,C.
    Phenotypic and structural analyses of hepatitis C virus NS3 protease ARG155 variants: sensitivity to telaprevir (VX-950) and interferon alpha
    J Biol Chem282, 22619-22628. PubMed  Europe PubMed DOI  I
  375. Zuo,G., Li,Z., Chen,L. and Xu,X.
    Activity of compounds from Chinese herbal medicine Rhodiola kirilowii (Regel) Maxim against HCV NS3 serine protease
    Antiviral Res76, 86-92. PubMed  Europe PubMed DOI  I
  376. 2006
  377. [YEAR:25-5-2006]Arasappan,A., Njoroge,F.G., Chen,K.X., Venkatraman,S., Parekh,T.N., Gu,H., Pichardo,J., Butkiewicz,N., Prongay,A., Madison,V. and Girijavallabhan,V.
    P2-P4 Macrocyclic inhibitors of hepatitis C virus NS3-4A serine protease
    Bioorg Med Chem Lett16, 3960-3965. PubMed  Europe PubMed DOI  S  I
  378. [YEAR:29-12-2006]Bogen,S.L., Ruan,S., Liu,R., Agrawal,S., Pichardo,J., Prongay,A., Baroudy,B., Saksena,A.K., Girijavallabhan,V. and Njoroge,F.G.
    Depeptidization efforts on P3-P2' alpha-ketoamide inhibitors of HCV NS3-4A serine protease: effect on HCV replicon activity
    Bioorg Med Chem Lett16, 1621-1627. PubMed  Europe PubMed DOI  I
  379. [YEAR:4-5-2006]Bogen,S.L., Arasappan,A., Bennett,F., Chen,K., Jao,E., Liu,Y.T., Lovey,R.G., Venkatraman,S., Pan,W., Parekh,T., Pike,R.E., Ruan,S., Liu,R., Baroudy,B., Agrawal,S., Chase,R., Ingravallo,P., Pichardo,J., Prongay,A., Brisson,J.M., Hsieh,T.Y., Cheng,K.C., Kemp,S.J., Levy,O.E., Lim-Wilby,M., Tamura,S.Y., Saksena,A.K., Girijavallabhan,V. and Njoroge,F.G.
    Discovery of SCH446211 (SCH6): a new ketoamide inhibitor of the HCV NS3 serine protease and HCV subgenomic RNA replication
    J Med Chem49, 2750-2757. PubMed  Europe PubMed DOI  I
  380. Breiman,A., Vitour,D., Vilasco,M., Ottone,C., Molina,S., Pichard,L., Fournier,C., Delgrange,D., Charneau,P., Duverlie,G., Wychowski,C., Maurel,P. and Meurs,E.F.
    A hepatitis C virus (HCV) NS3/4A protease-dependent strategy for the identification and purification of HCV-infected cells
    J Gen Virol87, 3587-3598. PubMed  Europe PubMed DOI
  381. [YEAR:9-2-2006]Chen,K.X., Njoroge,F.G., Arasappan,A., Venkatraman,S., Vibulbhan,B., Yang,W., Parekh,T.N., Pichardo,J., Prongay,A., Cheng,K.C., Butkiewicz,N., Yao,N., Madison,V. and Girijavallabhan,V.
    Novel potent hepatitis C virus NS3 serine protease inhibitors derived from proline-based macrocycles
    J Med Chem49, 995-1005. PubMed  Europe PubMed DOI  I
  382. [YEAR:26-1-2006]Chen,K.X., Njoroge,F.G., Pichardo,J., Prongay,A., Butkiewicz,N., Yao,N., Madison,V. and Girijavallabhan,V.
    Potent 7-hydroxy-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid-based macrocyclic inhibitors of hepatitis C virus NS3 protease
    J Med Chem49, 567-574. PubMed  Europe PubMed DOI  I
  383. Courcambeck,J., Bouzidi,M., Perbost,R., Jouirou,B., Amrani,N., Cacoub,P., Pepe,G., Sabatier,J.M. and Halfon,P.
    Resistance of hepatitis C virus to NS3-4A protease inhibitors: mechanisms of drug resistance induced by R155Q, A156T, D168A and D168V mutations
    Antivir Ther11, 847-855. PubMed  Europe PubMed  I
  384. Da Cunha,E.F.F., Ramalho,T.C., Taft,C.A. and de Alencastro,R.B.
    Computer-assisted analysis of the interactions of macrocyclic inhibitors with wild type and mutant D168A hepatitis C virus NS3 serine protease
    Lett Drug Des Discov3, 17-28.  I
  385. [YEAR:22-2-2006]Evans,J.D. and Seeger,C.
    Cardif: A protein central to innate immunity is inactivated by the HCV NS3 serine protease
    Hepatology43, 615-617. PubMed  Europe PubMed DOI
  386. Guo,Z., Prongay,A., Tong,X., Fischmann,T., Bogen,S., Velazquez,F., Venkatraman,S., Njoroge,F.G. and Madison,V.
    Computational study of the effects of mutations A156T, D168V, and D168Q on the binding of HCV protease inhibitors
    J Chem Theory Comput2, 1657-1663. PubMed  Europe PubMed DOI  I
  387. Herrmann,E., Zeuzem,S., Sarrazin,C., Hinrichsen,H., Benhamou,Y., Manns,M.P., Reiser,M., Reesink,H., Calleja,J.L., Forns,X., Steinmann,G.G. and Nehmiz,G.
    Viral kinetics in patients with chronic hepatitis C treated with the serine protease inhibitor BILN 2061
    Antivir Ther11, 371-376. PubMed  Europe PubMed  I
  388. [YEAR:2-5-2006]Johansson,P.O., Back,M., Kvarnstrom,I., Jansson,K., Vrang,L., Hamelink,E., Hallberg,A., Rosenquist,A. and Samuelsson,B.
    Potent inhibitors of the hepatitis C virus NS3 protease: use of a novel P2 cyclopentane-derived template
    Bioorg Med Chem14, 5136-5151. PubMed  Europe PubMed DOI  I
  389. Johnson,R.J., Lin,S.R. and Raines,R.T.
    A ribonuclease zymogen activated by the NS3 protease of the hepatitis C virus
    FEBS J273, 5457-5465. PubMed  Europe PubMed DOI
  390. Lin,C., Kwong,A.D. and Perni,R.B.
    Discovery and development of VX-950, a novel, covalent, and reversible inhibitor of hepatitis C virus NS3.4A serine protease
    Infect Disord Drug Targets6, 3-16. PubMed  Europe PubMed  V  I
  391. Lin,K., Perni,R.B., Kwong,A.D. and Lin,C.
    VX-950, a novel hepatitis C virus (HCV) NS3-4A protease inhibitor, exhibits potent antiviral activities in HCV replicon cells
    Antimicrob Agents Chemother50, 1813-1822. PubMed  Europe PubMed DOI  I
  392. Lin,R., Lacoste,J., Nakhaei,P., Sun,Q., Yang,L., Paz,S., Wilkinson,P., Julkunen,I., Vitour,D., Meurs,E. and Hiscott,J.
    Dissociation of a MAVS/IPS-1/VISA/Cardif-IKKepsilon molecular complex from the mitochondrial outer membrane by hepatitis C virus NS3-4A proteolytic cleavage
    J Virol80, 6072-6083. PubMed  Europe PubMed DOI
  393. [YEAR:11-4-2006]Loo,Y.M., Owen,D.M., Li,K., Erickson,A.K., Johnson,C.L., Fish,P.M., Carney,D.S., Wang,T., Ishida,H., Yoneyama,M., Fujita,T., Saito,T., Lee,W.M., Hagedorn,C.H., Lau,D.T., Weinman,S.A., Lemon,S.M. and Gale,M., Jr.
    Viral and therapeutic control of IFN-beta promoter stimulator 1 during hepatitis C virus infection
    Proc Natl Acad Sci U S A103, 6001-6006. PubMed  Europe PubMed DOI
  394. Malcolm,B.A., Liu,R., Lahser,F., Agrawal,S., Belanger,B., Butkiewicz,N., Chase,R., Gheyas,F., Hart,A., Hesk,D., Ingravallo,P., Jiang,C., Kong,R., Lu,J., Pichardo,J., Prongay,A., Skelton,A., Tong,X., Venkatraman,S., Xia,E., Girijavallabhan,V. and Njoroge,F.G.
    SCH 503034, a mechanism-based inhibitor of hepatitis C virus NS3 protease, suppresses polyprotein maturation and enhances the antiviral activity of alpha interferon in replicon cells
    Antimicrob Agents Chemother50, 1013-1020. PubMed  Europe PubMed DOI  I
  395. Perni,R.B., Almquist,S.J., Byrn,R.A., Chandorkar,G., Chaturvedi,P.R., Courtney,L.F., Decker,C.J., Dinehart,K., Gates,C.A., Harbeson,S.L., Heiser,A., Kalkeri,G., Kolaczkowski,E., Lin,K., Luong,Y.P., Rao,B.G., Taylor,W.P., Thomson,J.A., Tung,R.D., Wei,Y., Kwong,A.D. and Lin,C.
    Preclinical profile of VX-950, a potent, selective, and orally bioavailable inhibitor of hepatitis C virus NS3-4A serine protease
    Antimicrob Agents Chemother50, 899-909. PubMed  Europe PubMed DOI  I
  396. [YEAR:3-10-2006]Ronn,R., Sabnis,Y.A., Gossas,T., Akerblom,E., Danielson,U.H., Hallberg,A. and Johansson,A.
    Exploration of acyl sulfonamides as carboxylic acid replacements in protease inhibitors of the hepatitis C virus full-length NS3
    Bioorg Med Chem14, 544-559. PubMed  Europe PubMed DOI  I
  397. [YEAR:15-12-2006]Soderholm,J. and Sallberg,M.
    A complete mutational fitness map of the hepatitis C virus nonstructural 3 protease: relation to recognition by cytotoxic T lymphocytes
    J Infect Dis194, 1724-1728. PubMed  Europe PubMed DOI
  398. Thomson,J.A. and Perni,R.B.
    Hepatitis C virus NS3-4A protease inhibitors: countering viral subversion in vitro and showing promise in the clinic
    Curr Opin Drug Discov Devel9, 606-617. PubMed  Europe PubMed  V  I
  399. [YEAR:7-2-2006]Tong,X., Guo,Z., Wright-Minogue,J., Xia,E., Prongay,A., Madison,V., Qiu,P., Venkatraman,S., Velazquez,F., Njoroge,F.G. and Malcolm,B.A.
    Impact of naturally occurring variants of HCV protease on the binding of different classes of protease inhibitors
    Biochemistry45, 1353-1361. PubMed  Europe PubMed DOI  S  I
  400. [YEAR:5-10-2006]Venkatraman,S., Bogen,S.L., Arasappan,A., Bennett,F., Chen,K., Jao,E., Liu,Y.T., Lovey,R., Hendrata,S., Huang,Y., Pan,W., Parekh,T., Pinto,P., Popov,V., Pike,R., Ruan,S., Santhanam,B., Vibulbhan,B., Wu,W., Yang,W., Kong,J., Liang,X., Wong,J., Liu,R., Butkiewicz,N., Chase,R., Hart,A., Agrawal,S., Ingravallo,P., Pichardo,J., Kong,R., Baroudy,B., Malcolm,B., Guo,Z., Prongay,A., Madison,V., Broske,L., Cui,X., Cheng,K.C., Hsieh,Y., Brisson,J.M., Prelusky,D., Korfmacher,W., White,R., Bogdanowich-Knipp,S., Pavlovsky,A., Bradley,P., Saksena,A.K., Ganguly,A., Piwinski,J., Girijavallabhan,V. and Njoroge,F.G.
    Discovery of (1R,5S)-N-[3-Amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]- 3-[2(S)-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobuty l]- 6,6-dimethyl-3-azabicyclo[3.1.0]hexan-2(S)-carboxamide (SCH 503034), a selective, potent, orally bioavailable hepatitis C virus NS3 protease inhibitor: a potential therapeutic agent for the treatment of hepatitis C infection
    J Med Chem49, 6074-6086. PubMed  Europe PubMed DOI  I
  401. [YEAR:11-1-2006]Venkatraman,S., Njoroge,F.G., Wu,W., Girijavallabhan,V., Prongay,A.J., Butkiewicz,N. and Pichardo,J.
    Novel inhibitors of hepatitis C NS3-NS4A serine protease derived from 2-aza-bicyclo[2.2.1]heptane-3-carboxylic acid
    Bioorg Med Chem Lett16, 1628-1632. PubMed  Europe PubMed DOI  I
  402. White,P.W., Llinas-Brunet,M. and Bos,M.
    Blunting the Swiss army knife of hepatitis C virus: inhibitors of NS3/4A protease
    Prog Med Chem44, 65-107. PubMed  Europe PubMed DOI  V  I
  403. Yang,Z.R.
    Predicting hepatitis C virus protease cleavage sites using generalized linear indicator regression models
    IEEE Trans Biomed Eng53, 2119-2123. PubMed  Europe PubMed DOI
  404. [YEAR:13-12-2006]Yi,M., Tong,X., Skelton,A., Chase,R., Chen,T., Prongay,A., Bogen,S.L., Saksena,A.K., Njoroge,F.G., Veselenak,R.L., Pyles,R.B., Bourne,N., Malcolm,B.A. and Lemon,S.M.
    Mutations conferring resistance to SCH6, a novel hepatitis C virus NS3/4A protease inhibitor. Reduced RNA replication fitness and partial rescue by second-site mutations
    J Biol Chem281, 8205-8215. PubMed  Europe PubMed DOI  I
  405. Zhu,Q., Oei,Y., Mendel,D.B., Garrett,E.N., Patawaran,M.B., Hollenbach,P.W., Aukerman,S.L. and Weiner,A.J.
    Novel robust hepatitis C virus mouse efficacy model
    Antimicrob Agents Chemother50, 3260-3268. PubMed  Europe PubMed DOI  I
  406. 2005
  407. [YEAR:5-8-2005]Arasappan,A., Njoroge,F.G., Chan,T.Y., Bennett,F., Bogen,S.L., Chen,K., Gu,H., Hong,L., Jao,E., Liu,Y.T., Lovey,R.G., Parekh,T., Pike,R.E., Pinto,P., Santhanam,B., Venkatraman,S., Vaccaro,H., Wang,H., Yang,X., Zhu,Z., McKittrick,B., Saksena,A.K., Girijavallabhan,V., Pichardo,J., Butkiewicz,N., Ingram,R., Malcolm,B., Prongay,A., Yao,N., Marten,B., Madison,V., Kemp,S., Levy,O., Lim-Wilby,M., Tamura,S. and Ganguly,A.K.
    Hepatitis C virus NS3-4A serine protease inhibitors: SAR of P2' moiety with improved potency
    Bioorg Med Chem Lett15, 4180-4184. PubMed  Europe PubMed DOI  I
  408. [YEAR:18-8-2005]Bogen,S., Saksena,A.K., Arasappan,A., Gu,H., Njoroge,F.G., Girijavallabhan,V., Pichardo,J., Butkiewicz,N., Prongay,A. and Madison,V.
    Hepatitis C virus NS3-4A serine protease inhibitors: use of a P2-P1 cyclopropyl alanine combination for improved potency
    Bioorg Med Chem Lett15, 4515-4519. PubMed  Europe PubMed DOI  S  I
  409. [YEAR:6-10-2005]Chen,K.X., Njoroge,F.G., Pichardo,J., Prongay,A., Butkiewicz,N., Yao,N., Madison,V. and Girijavallabhan,V.
    Design, synthesis, and biological activity of m-tyrosine-based 16- and 17-membered macrocyclic inhibitors of hepatitis C virus NS3 serine protease
    J Med Chem48, 6229-6235. PubMed  Europe PubMed DOI  S  I
  410. [YEAR:18-8-2005]Chen,K.X., Njoroge,F.G., Prongay,A., Pichardo,J., Madison,V. and Girijavallabhan,V.
    Synthesis and biological activity of macrocyclic inhibitors of hepatitis C virus (HCV) NS3 protease
    Bioorg Med Chem Lett15, 4475-4478. PubMed  Europe PubMed DOI  I
  411. Chen,S.H. and Tan,S.L.
    Discovery of small-molecule inhibitors of HCV NS3-4A protease as potential therapeutic agents against HCV infection
    Curr Med Chem12, 2317-2342. PubMed  Europe PubMed DOI  V  I
  412. Chung,V., Carroll,A.R., Gray,N.M., Parry,N.R., Thommes,P.A., Viner,K.C. and D'Souza,E.A.
    Development of cell-based assays for in vitro characterization of hepatitis C virus NS3/4A protease inhibitors
    Antimicrob Agents Chemother49, 1381-1390. PubMed  Europe PubMed DOI  A
  413. da Silveira,N.J., Arcuri,H.A., Bonalumi,C.E., de Souza,F.P., Mello,I.M., Rahal,P., Pinho,J.R. and de Azevedo,W.F., Jr.
    Molecular models of NS3 protease variants of the hepatitis C virus
    BMC Struct Biol5, 1-1. PubMed  Europe PubMed DOI
  414. Goudreau,N. and Llinas-Brunet,M.
    The therapeutic potential of NS3 protease inhibitors in HCV infection
    Expert Opin Investig Drugs14, 1129-1144. PubMed  Europe PubMed DOI  I
  415. Gu,B., Pruss,C.M., Gates,A.T. and Khandekar,S.S.
    The RNA-unwinding activity of hepatitis C virus non-structural protein 3 (NS3) is positively modulated by its protease domain
    Protein Pept Lett12, 315-321. PubMed  Europe PubMed DOI
  416. [YEAR:12-8-2005]Karayiannis,P.
    The hepatitis C virus NS3/4A protease complex interferes with pathways of the innate immune response
    J Hepatol43, 743-745. PubMed  Europe PubMed DOI
  417. Latli,B., Hrapchak,M., Gorys,V., Busacca,C.A. and Senanayake,C.
    Synthesis of deuterium-, tritium-, and carbon-14-labeled BILN2061, a potent hepatitis C virus protease inhibitor
    J Labelled Comp Radiopharm48, 447-455.  I
  418. Lee,J.C., Yu,M.C., Lien,T.W., Chang,C.F. and Hsu,J.T.
    High-throughput cell-based screening for hepatitis C virus NS3/4A protease inhibitors
    Assay Drug Dev Technol3, 385-392. PubMed  Europe PubMed DOI  I
  419. [YEAR:22-2-2005]Li,K., Foy,E., Ferreon,J.C., Nakamura,M., Ferreon,A.C., Ikeda,M., Ray,S.C., Gale,M., Jr. and Lemon,S.M.
    Immune evasion by hepatitis C virus NS3/4A protease-mediated cleavage of the Toll-like receptor 3 adaptor protein TRIF
    Proc Natl Acad Sci U S A102, 2992-2997. PubMed  Europe PubMed DOI  I
  420. [YEAR:21-11-2005]Li,X.D., Sun,L., Seth,R.B., Pineda,G. and Chen,Z.J.
    Hepatitis C virus protease NS3/4A cleaves mitochondrial antiviral signaling protein off the mitochondria to evade innate immunity
    Proc Natl Acad Sci U S A102, 17717-17722. PubMed  Europe PubMed DOI
  421. [YEAR:8-8-2005]Lin,C., Gates,C.A., Rao,B.G., Brennan,D.L., Fulghum,J.R., Luong,Y.P., Frantz,J.D., Lin,K., Ma,S., Wei,Y.Y., Perni,R.B. and Kwong,A.D.
    In vitro studies of cross-resistance mutations against two hepatitis C virus serine protease inhibitors, VX-950 and BILN 2061
    J Biol Chem280, 36784-36791. PubMed  Europe PubMed DOI  I
  422. [YEAR:24-2-2005]Reiser,M., Hinrichsen,H., Benhamou,Y., Reesink,H.W., Wedemeyer,H., Avendano,C., Riba,N., Yong,C.L., Nehmiz,G. and Steinmann,G.G.
    Antiviral efficacy of NS3-serine protease inhibitor BILN-2061 in patients with chronic genotype 2 and 3 hepatitis C
    Hepatology41, 832-835. PubMed  Europe PubMed DOI  I
  423. Summa,V.
    VX-950 (Vertex/Mitsubishi)
    Curr Opin Investig Drugs6, 831-837. PubMed  Europe PubMed  I
  424. Vallet,S., Gouriou,S., Nousbaum,J.B., Legrand-Quillien,M.C., Goudeau,A. and Picard,B.
    Genetic heterogeneity of the NS3 protease gene in hepatitis C virus genotype 1 from untreated infected patients
    J Med Virol75, 528-537. PubMed  Europe PubMed DOI
  425. [YEAR:11-8-2005]Venkatraman,S., Njoroge,F.G., Girijavallabhan,V.M., Madison,V.S., Yao,N.H., Prongay,A.J., Butkiewicz,N. and Pichardo,J.
    Design and synthesis of depeptidized macrocyclic inhibitors of hepatitis C NS3-4A protease using structure-based drug design
    J Med Chem48, 5088-5091. PubMed  Europe PubMed DOI  I
  426. 2004
  427. [YEAR:6-12-2004]Arasappan,A., Njoroge,F.G., Parekh,T.N., Yang,X., Pichardo,J., Butkiewicz,N., Prongay,A., Yao,N. and Girijavallabhan,V.
    Novel 2-oxoimidazolidine-4-carboxylic acid derivatives as hepatitis C virus NS3-4A serine protease inhibitors: synthesis, activity, and X-ray crystal structure of an enzyme inhibitor complex
    Bioorg Med Chem Lett14, 5751-5755. PubMed  Europe PubMed DOI  S  I
  428. [YEAR:15-7-2004]Bailey,M.D., Halmos,T., Goudreau,N., Lescop,E. and Llinas-Brunet,M.
    Novel azapeptide inhibitors of hepatitis C virus serine protease
    J Med Chem47, 3788-3799. PubMed  Europe PubMed DOI  I
  429. Brass,V., Blum,H.E. and Moradpour,D.
    Recent developments in target identification against hepatitis C virus
    Expert Opin Ther Targets8, 295-307. PubMed  Europe PubMed DOI
  430. [YEAR:19-8-2004]Faucher,A.M., Bailey,M.D., Beaulieu,P.L., Brochu,C., Duceppe,J.S., Ferland,J.M., Ghiro,E., Gorys,V., Halmos,T., Kawai,S.H., Poirier,M., Simoneau,B., Tsantrizos,Y.S. and Llinas-Brunet,M.
    Synthesis of BILN 2061, an HCV NS3 protease inhibitor with proven antiviral effect in humans
    Org Lett6, 2901-2904. PubMed  Europe PubMed DOI  I
  431. Frecer,V., Kabelac,M., De Nardi,P., Pricl,S. and Miertus,S.
    Structure-based design of inhibitors of NS3 serine protease of hepatitis C virus
    J Mol Graph Model22, 209-220. PubMed  Europe PubMed DOI  I
  432. Frick,D.N., Rypma,R.S., Lam,A.M. and Gu,B.
    The nonstructural protein 3 protease/helicase requires an intact protease domain to unwind duplex RNA efficiently
    J Biol Chem279, 1269-1280. PubMed  Europe PubMed DOI
  433. [YEAR:17-12-2004]Fukuda,K., Umehara,T., Sekiya,S., Kunio,K., Hasegawa,T. and Nishikawa,S.
    An RNA ligand inhibits hepatitis C virus NS3 protease and helicase activities
    Biochem Biophys Res Commun325, 670-675. PubMed  Europe PubMed DOI
  434. [YEAR:1-1-2004]Goudreau,N., Cameron,D.R., Bonneau,P., Gorys,V., Plouffe,C., Poirier,M., Lamarre,D. and Llinas-Brunet,M.
    NMR structural characterization of peptide inhibitors bound to the hepatitis C virus NS3 protease: design of a new P2 substituent
    J Med Chem47, 123-132. PubMed  Europe PubMed DOI  I
  435. [YEAR:17-9-2004]Goudreau,N., Brochu,C., Cameron,D.R., Duceppe,J.S., Faucher,A.M., Ferland,J.M., Grand-Maitre,C., Poirier,M., Simoneau,B. and Tsantrizos,Y.S.
    Potent inhibitors of the hepatitis C virus NS3 protease: design and synthesis of macrocyclic substrate-based beta-strand mimics
    J Org Chem69, 6185-6201. PubMed  Europe PubMed DOI  I
  436. [YEAR:10-8-2004]Khu,Y.L., Tan,Y.J., Lim,S.G., Hong,W. and Goh,P.Y.
    Hepatitis C virus non-structural protein NS3 interacts with LMP7, a component of the immunoproteasome, and affects its proteasome activity
    Biochem J384, 401-409. PubMed  Europe PubMed DOI
  437. [YEAR:5-1-2004]Lamar,J., Victor,F., Snyder,N., Johnson,R.B., Wang,Q.M., Glass,J.I. and Chen,S.H.
    Novel P4 truncated tripeptidyl alpha-ketoamides as HCV protease inhibitors
    Bioorg Med Chem Lett14, 263-266. PubMed  Europe PubMed DOI  I
  438. [YEAR:1-3-2004]Lee,J.C., Chang,C.F., Chi,Y.H., Hwang,D.R. and Hsu,J.T.
    A reporter-based assay for identifying hepatitis C virus inhibitors based on subgenomic replicon cells
    J Virol Methods116, 27-33. PubMed  Europe PubMed DOI
  439. [YEAR:6-2-2004]Lin,C., Lin,K., Luong,Y.P., Rao,B.G., Wei,Y.Y., Brennan,D.L., Fulghum,J.R., Hsiao,H.M., Ma,S., Maxwell,J.P., Cottrell,K.M., Perni,R.B., Gates,C.A. and Kwong,A.D.
    In vitro resistance studies of hepatitis C virus serine protease inhibitors, VX-950 and BILN 2061: structural analysis indicates different resistance mechanisms
    J Biol Chem279, 17508-17514. PubMed  Europe PubMed DOI  I
  440. Lin,K., Kwong,A.D. and Lin,C.
    Combination of a hepatitis C virus NS3-NS4A protease inhibitor and alpha interferon synergistically inhibits viral RNA replication and facilitates viral RNA clearance in replicon cells
    Antimicrob Agents Chemother48, 4784-4792. PubMed  Europe PubMed DOI  I
  441. [YEAR:15-1-2004]Liu,Y., Stoll,V.S., Richardson,P.L., Saldivar,A., Klaus,J.L., Molla,A., Kohlbrenner,W. and Kati,W.M.
    Hepatitis C NS3 protease inhibition by peptidyl-alpha-ketoamide inhibitors: kinetic mechanism and structure
    Arch Biochem Biophys421, 207-216. PubMed  Europe PubMed DOI  I
  442. [YEAR:16-12-2004]Llinas-Brunet,M., Bailey,M.D., Ghiro,E., Gorys,V., Halmos,T., Poirier,M., Rancourt,J. and Goudreau,N.
    A systematic approach to the optimization of substrate-based inhibitors of the hepatitis C virus NS3 protease: discovery of potent and specific tripeptide inhibitors
    J Med Chem47, 6584-6594. PubMed  Europe PubMed DOI  I
  443. [YEAR:25-3-2004]Llinas-Brunet,M., Bailey,M.D., Bolger,G., Brochu,C., Faucher,A.M., Ferland,J.M., Garneau,M., Ghiro,E., Gorys,V., Grand-Maitre,C., Halmos,T., Lapeyre-Paquette,N., Liard,F., Poirier,M., Rheaume,M., Tsantrizos,Y.S. and Lamarre,D.
    Structure-activity study on a novel series of macrocyclic inhibitors of the hepatitis C virus NS3 protease leading to the discovery of BILN 2061
    J Med Chem47, 1605-1608. PubMed  Europe PubMed DOI  I
  444. Lu,L., Pilot-Matias,T.J., Stewart,K.D., Randolph,J.T., Pithawalla,R., He,W., Huang,P.P., Klein,L.L., Mo,H. and Molla,A.
    Mutations conferring resistance to a potent hepatitis C virus serine protease inhibitor in vitro
    Antimicrobial Agents Chemother48, 2260-2266. PubMed  Europe PubMed DOI  I
  445. [YEAR:16-12-2004]Ontoria,J.M., Di Marco,S., Conte,I., Di Francesco,M.E., Gardelli,C., Koch,U., Matassa,V.G., Poma,M., Steinkuhler,C., Volpari,C. and Harper,S.
    The design and enzyme-bound crystal structure of indoline based peptidomimetic inhibitors of hepatitis C virus NS3 protease
    J Med Chem47, 6443-6446. PubMed  Europe PubMed DOI  I
  446. [YEAR:22-3-2004]Perni,R.B., Pitlik,J., Britt,S.D., Court,J.J., Courtney,L.F., Deininger,D.D., Farmer,L.J., Gates,C.A., Harbeson,S.L., Levin,R.B., Lin,C., Lin,K., Moon,Y.C., Luong,Y.P., O'Malley,E.T., Rao,B.G., Thomson,J.A., Tung,R.D., Van Drie,J.H. and Wei,Y.
    Inhibitors of hepatitis C virus NS3.4A protease 2. Warhead SAR and optimization
    Bioorg Med Chem Lett14, 1441-1446. PubMed  Europe PubMed DOI  I
  447. [YEAR:19-4-2004]Perni,R.B., Farmer,L.J., Cottrell,K.M., Court,J.J., Courtney,L.F., Deininger,D.D., Gates,C.A., Harbeson,S.L., Kim,J.L., Lin,C., Lin,K., Luong,Y.P., Maxwell,J.P., Murcko,M.A., Pitlik,J., Rao,B.G., Schairer,W.C., Tung,R.D., Van Drie,J.H., Wilson,K. and Thomson,J.A.
    Inhibitors of hepatitis C virus NS3.4A protease. Part 3: P2 proline variants
    Bioorg Med Chem Lett14, 1939-1942. PubMed  Europe PubMed DOI  I
  448. [YEAR:7-4-2004]Poliakov,A., Johansson,A., Akerblom,E., Oscarsson,K., Samuelsson,B., Hallberg,A. and Danielson,U.H.
    Structure-activity relationships for the selectivity of hepatitis C virus NS3 protease inhibitors
    Biochim Biophys Acta1672, 51-59. PubMed  Europe PubMed DOI  I
  449. [YEAR:6-5-2004]Rancourt,J., Cameron,D.R., Gorys,V., Lamarre,D., Poirier,M., Thibeault,D. and Llinas-Brunet,M.
    Peptide-based inhibitors of the hepatitis C virus NS3 protease: structure-activity relationship at the C-terminal position
    J Med Chem47, 2511-2522. PubMed  Europe PubMed DOI  I
  450. [YEAR:1-5-2004]Shokhen,M. and Albeck,A.
    Identification of protons position in acid-base enzyme catalyzed reactions: the hepatitis C viral NS3 protease
    Proteins55, 245-250. PubMed  Europe PubMed DOI
  451. Steinkuhler,C.
    Hepacivirin
    [ISSN:0-12-079610-4]2, 1773-1779.  V
  452. [YEAR:16-8-2004]Sun,D.X., Liu,L., Heinz,B., Kolykhalov,A., Lamar,J., Johnson,R.B., Wang,Q.M., Yip,Y. and Chen,S.H.
    P4 cap modified tetrapeptidyl alpha-ketoamides as potent HCV NS3 protease inhibitors
    Bioorg Med Chem Lett14, 4333-4338. PubMed  Europe PubMed DOI  I
  453. Thibeault,D., Bousquet,C., Gingras,R., Lagace,L., Maurice,R., White,P.W. and Lamarre,D.
    Sensitivity of NS3 serine proteases from hepatitis C virus genotypes 2 and 3 to the inhibitor BILN 2061
    J Virol78, 7352-7359. PubMed  Europe PubMed DOI  I
  454. Tsantrizos,Y.S.
    The design of a potent inhibitor of the hepatitis C virus NS3 protease: BILN 2061 - from the NMR tube to the clinic
    Biopolymers76, 309-323. PubMed  Europe PubMed DOI  I
  455. [YEAR:5-1-2004]Victor,F., Lamar,J., Snyder,N., Yip,Y., Guo,D., Yumibe,N., Johnson,R.B., Wang,Q.M., Glass,J.I. and Chen,S.H.
    P1 and P3 optimization of novel bicycloproline P2 bearing tetrapeptidyl alpha-ketoamide based HCV protease inhibitors
    Bioorg Med Chem Lett14, 257-261. PubMed  Europe PubMed DOI  I
  456. Wang,W., Lahser,F.C., Yi,M., Wright-Minogue,J., Xia,E., Weber,P.C., Lemon,S.M. and Malcolm,B.A.
    Conserved C-terminal threonine of hepatitis C virus NS3 regulates autoproteolysis and prevents product inhibition
    J Virol78, 700-709. PubMed  Europe PubMed DOI
  457. [YEAR:6-5-2004]Wyss,D.F., Arasappan,A., Senior,M.M., Wang,Y.S., Beyer,B.M., Njoroge,F.G. and McCoy,M.A.
    Non-peptidic small-molecule inhibitors of the single-chain hepatitis C virus NS3 protease/NS4A cofactor complex discovered by structure-based NMR screening
    J Med Chem47, 2486-2498. PubMed  Europe PubMed DOI  I
  458. [YEAR:5-1-2004]Yip,Y., Victor,F., Lamar,J., Johnson,R., Wang,Q.M., Barket,D., Glass,J., Jin,L., Liu,L., Venable,D., Wakulchik,M., Xie,C., Heinz,B., Villarreal,E., Colacino,J., Yumibe,N., Tebbe,M., Munroe,J. and Chen,S.H.
    Discovery of a novel bicycloproline P2 bearing peptidyl alpha-ketoamide LY514962 as HCV protease inhibitor
    Bioorg Med Chem Lett14, 251-256. PubMed  Europe PubMed DOI  I
  459. [YEAR:4-10-2004]Yip,Y., Victor,F., Lamar,J., Johnson,R., Wang,Q.M., Glass,J.I., Yumibe,N., Wakulchik,M., Munroe,J. and Chen,S.H.
    P4 and P1' optimization of bicycloproline P2 bearing tetrapeptidyl alpha-ketoamides as HCV protease inhibitors
    Bioorg Med Chem Lett14, 5007-5011. PubMed  Europe PubMed DOI  I
  460. 2003
  461. Andrews,D.M., Chaignot,H.M., Coomber,B.A., Dowle,M.D., Hind,S.L., Johnson,M.R., Jones,P.S., Mills,G., Patikis,A., Pateman,T.J., Robinson,J.E., Slater,M.J. and Trivedi,N.
    The design of potent, non-peptidic inhibitors of hepatitis C protease
    Eur J Med Chem38, 339-343. PubMed  Europe PubMed DOI  I
  462. De Francesco,R., Tomei,L., Altamura,S., Summa,V. and Migliaccio,G.
    Approaching a new era for hepatitis C virus therapy: inhibitors of the NS3-4A serine protease and the NS5B RNA-dependent RNA polymerase
    Antiviral Res58, 1-16. PubMed  Europe PubMed DOI  I
  463. [YEAR:16-5-2003]Foy,E., Li,K., Wang,C., Sumpter,R., Jr., Ikeda,M., Lemon,S.M. and Gale,M., Jr.
    Regulation of interferon regulatory factor-3 by the hepatitis C virus serine protease
    Science300, 1145-1148. PubMed  Europe PubMed DOI  I
  464. [YEAR:24-3-2003]Han,W., Hu,Z., Jiang,X., Wasserman,Z.R. and Decicco,C.P.
    Glycine alpha-ketoamides as HCV NS3 protease inhibitors
    Bioorg Med Chem Lett13, 1111-1114. PubMed  Europe PubMed DOI  I
  465. [YEAR:13-11-2003]Lamarre,D., Anderson,P.C., Bailey,M., Beaulieu,P., Bolger,G., Bonneau,P., Bos,M., Cameron,D.R., Cartier,M., Cordingley,M.G., Faucher,A.M., Goudreau,N., Kawai,S.H., Kukolj,G., Lagace,L., LaPlante,S.R., Narjes,H., Poupart,M.A., Rancourt,J., Sentjens,R.E., St George,R., Simoneau,B., Steinmann,G., Thibeault,D., Tsantrizos,Y.S., Weldon,S.M., Yong,C.L. and Llinas-Brunet,M.
    An NS3 protease inhibitor with antiviral effects in humans infected with hepatitis C virus
    Nature426, 186-189. PubMed  Europe PubMed DOI  I
  466. [YEAR:15-5-2003]Lee,J.C., Shih,Y.F., Hsu,S.P., Chang,T.Y., Chen,L.H. and Hsu,J.T.
    Development of a cell-based assay for monitoring specific hepatitis C virus NS3/4A protease activity in mammalian cells
    Anal Biochem316, 162-170. PubMed  Europe PubMed DOI  A
  467. [YEAR:29-7-2003]Liu,Y., Saldivar,A., Bess,J., Solomon,L., Chen,C.M., Tripathi,R., Barrett,L., Richardson,P.L., Molla,A., Kohlbrenner,W. and Kati,W.
    Investigating the origin of the slow-binding inhibition of HCV NS3 serine protease by a novel substrate based inhibitor
    Biochemistry42, 8862-8869. PubMed  Europe PubMed DOI  I
  468. Lodrini,S., Bagaglio,S., Canducci,F., De Mitri,M.S., Andreone,P., Loggi,E., Lazzarin,A., Clementi,M. and Morsica,G.
    Sequence analysis of NS3 protease gene in clinical strains of hepatitis C virus
    J Biol Regul Homeost Agents17, 198-204. PubMed  Europe PubMed
  469. Martinez,M.A. and Clotet,B.
    Genetic screen for monitoring hepatitis C virus NS3 serine protease activity
    Antimicrobial Agents Chemother47, 1760-1765. PubMed  Europe PubMed DOI
  470. [YEAR:1-4-2003]Nishikawa,F., Kakiuchi,N., Funaji,K., Fukuda,K., Sekiya,S. and Nishikawa,S.
    Inhibition of HCV NS3 protease by RNA aptamers in cells
    Nucleic Acids Res31, 1935-1943. PubMed  Europe PubMed DOI
  471. [YEAR:18-8-2003]Orvieto,F., Koch,U., Matassa,V.G. and Muraglia,E.
    Novel, potent phenethylamide inhibitors of the hepatitis C virus (HCV) NS3 protease: probing the role of P2 aryloxyprolines with hybrid structures
    Bioorg Med Chem Lett13, 2745-2748. PubMed  Europe PubMed DOI  I
  472. [YEAR:30-5-2003]Pause,A., Kukolj,G., Bailey,M., Brault,M., Do,F., Halmos,T., Lagace,L., Maurice,R., Marquis,M., McKercher,G., Pellerin,C., Pilote,L., Thibeault,D. and Lamarre,D.
    An NS3 serine protease inhibitor abrogates replication of subgenomic hepatitis C virus RNA
    J Biol Chem278, 20374-20380. PubMed  Europe PubMed DOI  I
  473. [YEAR:13-11-2003]Rice,C.M.
    Virology: fresh assault on hepatitis C
    Nature426, 129-131. PubMed  Europe PubMed DOI  I
  474. Sekiya,S., Nishikawa,F., Fukuda,K. and Nishikawa,S.
    Structure/function analysis of an RNA aptamer for hepatitis C virus NS3 protease
    J Biochem133, 351-359. PubMed  Europe PubMed DOI
  475. Slater,M.J., Amphlett,E.M., Andrews,D.M., Bamborough,P., Carey,S.J., Johnson,M.R., Jones,P.S., Mills,G., Parry,N.R., Somers,D.O., Stewart,A.J. and Skarzynski,T.
    Pyrrolidine-5,5-trans-lactams. 4. Incorporation of a P3/P4 urea leads to potent intracellular inhibitors of hepatitis C virus NS3/4A protease
    Org Lett5, 4627-4630. PubMed  Europe PubMed DOI  S  I
  476. Trozzi,C., Bartholomew,L., Ceccacci,A., Biasiol,G., Pacini,L., Altamura,S., Narjes,F., Muraglia,E., Paonessa,G., Koch,U., De Francesco,R., Steinkuhler,C. and Migliaccio,G.
    In vitro selection and characterization of hepatitis C virus serine protease variants resistant to an active-site peptide inhibitor
    J Virol77, 3669-3679. PubMed  Europe PubMed DOI  I
  477. [YEAR:24-3-2003]Zhang,X., Schmitt,A.C., Jiang,W., Wasserman,Z. and Decicco,C.P.
    Design and synthesis of potent, non-peptide inhibitors of HCVNS3 protease
    Bioorg Med Chem Lett13, 1157-1160. PubMed  Europe PubMed DOI  I
  478. 2002
  479. Andrews,D.M., Chaignot,H., Coomber,B.A., Good,A.C., Hind,S.L., Johnson,M.R., Jones,P.S., Mills,G., Robinson,J.E., Skarzynski,T., Slater,M.J. and Somers,D.O.
    Pyrrolidine-5,5-trans-lactams. 2. The use of X-ray crystal structure data in the optimization of P3 and P4 substituents
    Org Lett4, 4479-4482. PubMed  Europe PubMed DOI  S  I
  480. [YEAR:25-2-2002]Beevers,R., Carr,M.G., Jones,P.S., Jordan,S., Kay,P.B., Lazell,R.C. and Raynham,T.M.
    Solution and solid-phase synthesis of potent inhibitors of hepatitis C Virus NS3 proteinase
    Bioorg Med Chem Lett12, 641-643. PubMed  Europe PubMed DOI  I
  481. Bianchi,E. and Pessi,A.
    Inhibiting viral proteases: Challenges and opportunities
    Biopolymers66, 101-114. PubMed  Europe PubMed DOI
  482. Casbarra,A., Piaz,F.D., Ingallinella,P., Orru,S., Pucci,P., Pessi,A. and Bianchi,E.
    The effect of prime-site occupancy on the hepatitis C virus NS3 protease structure
    Protein Sci11, 2102-2112. PubMed  Europe PubMed DOI
  483. Holland-Staley,C.A., Kovari,L.C., Golenberg,E.M., Pobursky,K.J. and Mayers,D.L.
    Genetic diversity and response to IFN of the NS3 protease gene from clinical strains of the hepatitis C virus
    Arch Virol147, 1385-1406. PubMed  Europe PubMed DOI
  484. [YEAR:30-4-2002]Ingallinella,P., Fattori,D., Altamura,S., Steinkuhler,C., Koch,U., Cicero,D., Bazzo,R., Cortese,R., Bianchi,E. and Pessi,A.
    Prime site binding inhibitors of a serine protease: NS3/4A of hepatitis C virus
    Biochemistry41, 5483-5492. PubMed  Europe PubMed DOI  I
  485. [YEAR:25-2-2002]Narjes,F., Koehler,K.F., Koch,U., Gerlach,B., Colarusso,S., Steinkuhler,C., Brunetti,M., Altamura,S., De Francesco,R. and Matassa,V.G.
    A designed P1 cysteine mimetic for covalent and non-covalent inhibitors of HCVNS3 protease
    Bioorg Med Chem Lett12, 701-704. PubMed  Europe PubMed DOI  I
  486. Poliakov,A., Hubatsch,I., Shuman,C.F., Stenberg,G. and Danielson,U.H.
    Expression and purification of recombinant full-length NS3 protease-helicase from a new variant of hepatitis C virus
    Protein Expr Purif25, 363-371. PubMed  Europe PubMed DOI
  487. [YEAR:4-11-2002]Priestley,E.S., De Lucca,I., Ghavimi,B., Erickson-Viitanen,S. and Decicco,C.P.
    P1 Phenethyl peptide boronic acid inhibitors of HCV NS3 protease
    Bioorg Med Chem Lett12, 3199-3202. PubMed  Europe PubMed DOI  I
  488. [YEAR:4-11-2002]Sperandio,D., Gangloff,A.R., Litvak,J., Goldsmith,R., Hataye,J.M., Wang,V.R., Shelton,E.J., Elrod,K., Janc,J.W., Clark,J.M., Rice,K., Weinheimer,S., Yeung,K.S., Meanwell,N.A., Hernandez,D., Staab,A.J., Venables,B.L. and Spencer,J.R.
    Highly potent non-peptidic inhibitors of the HCV NS3/NS4A serine protease
    Bioorg Med Chem Lett12, 3129-3133. PubMed  Europe PubMed DOI  I
  489. [YEAR:1-8-2002]Steinkuhler,C., Biasiol,G., Cerretani,M., Di Renzo,L., Brunetti,M., Ingallinella,P., De Francesco,R. and Altamura,S.
    A scintillation proximity active site binding assay for the hepatitis C virus serine protease
    Anal Biochem307, 99-104. PubMed  Europe PubMed DOI  A
  490. Tong,L.
    Viral proteases
    Chem Rev102, 4609-4626. PubMed  Europe PubMed DOI  V
  491. [YEAR:14-8-2002]Tsumoto,K., Misawa,S., Ohba,Y., Ueno,T., Hayashi,H., Kasai,N., Watanabe,H., Asano,R. and Kumagai,I.
    Inhibition of hepatitis C virus NS3 protease by peptides derived from complementarity-determining regions (CDRs) of the monoclonal antibody 8D4: tolerance of a CDR peptide to conformational changes of a target
    FEBS Lett525, 77-82. PubMed  Europe PubMed DOI
  492. [YEAR:8-4-2002]Zhang,R., Durkin,J.P. and Windsor,W.T.
    Azapeptides as inhibitors of the hepatitis C virus NS3 serine protease
    Bioorg Med Chem Lett12, 1005-1008. PubMed  Europe PubMed DOI  I
  493. 2001
  494. [YEAR:12-2-2001]Bennett,J.M., Campbell,A.D., Campbell,A.J., Carr,M.G., Dunsdon,R.M., Greening,J.R., Hurst,D.N., Jennings,N.S., Jones,P.S., Jordan,S., Kay,P.B., O'Brien,M.A., King-Underwood,J., Raynham,T.M., Wilkinson,C.S., Wilkinson,T.C. and Wilson,F.X.
    The identification of alpha-ketoamides as potent inhibitors of hepatitis C virus NS3-4A proteinase
    Bioorg Med Chem Lett11, 355-357. PubMed  Europe PubMed DOI  I
  495. [YEAR:1-5-2001]Beyer,B.M., Zhang,R., Hong,Z., Madison,V. and Malcolm,B.A.
    Effect of naturally occurring active site mutations on hepatitis C virus NS3 protease specificity
    Proteins43, 82-88. PubMed  Europe PubMed DOI
  496. [YEAR:23-1-2001]Koch,U., Biasiol,G., Brunetti,M., Fattori,D., Pallaoro,M. and Steinkuhler,C.
    Role of charged residues in the catalytic mechanism of hepatitis C virus NS3 protease: Electrostatic precollision guidance and transition-state stabilization
    Biochemistry40, 631-640. PubMed  Europe PubMed DOI
  497. [YEAR:10-8-2001]Mak,P., Palant,O., Labonte,P. and Plotch,S.
    Reconstitution of hepatitis C virus protease activities in yeast
    FEBS Lett503, 13-18. PubMed  Europe PubMed DOI
  498. [YEAR:13-7-2001]Poupart,M.A., Cameron,D.R., Chabot,C., Ghiro,E., Goudreau,N., Goulet,S., Poirier,M. and Tsantrizos,Y.S.
    Solid-phase synthesis of peptidomimetic inhibitors for the hepatitis C virus NS3 protease
    J Org Chem66, 4743-4751. PubMed  Europe PubMed DOI  I
  499. Steinkuhler,C., Koch,U., Narjes,F. and Matassa,V.G.
    Hepatitis C virus protease inhibitors: current progress and future challenges
    Curr Med Chem8, 919-932. PubMed  Europe PubMed  I
  500. [YEAR:3-9-2001]Yeung,K.S., Meanwell,N.A., Qiu,Z., Hernandez,D., Zhang,S., McPhee,F., Weinheimer,S., Clark,J.M. and Janc,J.W.
    Structure-activity relationship studies of a bisbenzimidazole-based, Zn(2+)-dependent inhibitor of HCVNS3 serine protease
    Bioorg Med Chem Lett11, 2355-2359. PubMed  Europe PubMed DOI  I
  501. 2000
  502. [YEAR:15-3-2000]Barbato,G., Cicero,D.O., Cordier,F., Narjes,F., Gerlach,B., Sambucini,S., Grzesiek,S., Matassa,V.G., De Francesco,R. and Bazzo,R.
    Inhibitor binding induces active site stabilization of the HCVNS3 protein serine protease domain
    EMBO J19, 1195-1206. PubMed  Europe PubMed DOI  S
  503. De Francesco,R. and Steinkuhler,C.
    Structure and function of the hepatitis C virus NS3-NS4A serine proteinase
    Curr Top Microbiol Immunol242, 149-169. PubMed  Europe PubMed
  504. [YEAR:10-3-2000]Di Marco,S., Rizzi,M., Volpari,C., Walsh,M.A., Narjes,F., Colarusso,S., De Francesco,R., Matassa,V.G. and Sollazzo,M.
    Inhibition of the hepatitis C virus NS3/4A protease. The crystal structures of two protease-inhibitor complexes
    J Biol Chem275, 7152-7157. PubMed  Europe PubMed DOI  S  I
  505. Fattori,D., Urbani,A., Brunetti,M., Ingenito,R., Pessi,A., Prendergast,K., Narjes,F., Matassa,V.G., De Francesco,R. and Steinkuhler,C.
    Probing the active site of the hepatitis C virus serine protease by fluorescence resonance energy transfer
    J Biol Chem275, 15106-15113. PubMed  Europe PubMed DOI
  506. Fukuda,K., Vishnuvardhan,D., Sekiya,S., Hwang,J., Kakiuchi,N., Taira,K., Shimotohno,K., Kumar,P.K. and Nishikawa,S.
    Isolation and characterization of RNA aptamers specific for the hepatitis C virus nonstructural protein 3 protease
    Eur J Biochem267, 3685-3694. PubMed  Europe PubMed DOI
  507. [YEAR:17-4-2000]Han,W., Hu,Z.L., Jiang,X.J. and Decicco,C.P.
    alpha-Ketoamides, alpha-ketoesters and alpha-diketones as HCVNS3 protease inhibitors
    Bioorg Med Chem Lett10, 711-713. PubMed  Europe PubMed DOI  I
  508. [YEAR:20-12-2000]Hwang,J., Fauzi,H., Fukuda,K., Sekiya,S., Kakiuchi,N., Shimotohno,K., Taira,K., Kusakabe,I. and Nishikawa,S.
    The RNA aptamer-binding site of hepatitis C virus NS3 protease
    Biochem Biophys Res Commun279, 557-562. PubMed  Europe PubMed DOI
  509. [YEAR:24-10-2000]Ingallinella,P., Bianchi,E., Ingenito,R., Koch,U., Steinkuhler,C., Altamura,S. and Pessi,A.
    Optimization of the P'-region of peptide inhibitors of hepatitis C virus NS3/4A protease
    Biochemistry39, 12898-12906. PubMed  Europe PubMed DOI  I
  510. [YEAR:15-8-2000]Kim,S.Y., Park,K.W., Lee,Y.J., Back,S.H., Goo,J.H., Park,O.K., Jang,S.K. and Park,W.J.
    In vivo determination of substrate specificity of hepatitis C virus NS3 protease: genetic assay for site-specific proteolysis
    Anal Biochem284, 42-48. PubMed  Europe PubMed DOI  A  P
  511. Kolykhalov,A.A., Mihalik,K., Feinstone,S.M. and Rice,C.M.
    Hepatitis C virus-encoded enzymatic activities and conserved RNA elements in the 3' nontranslated region are essential for virus replication in vivo
    J Virol74, 2046-2051. PubMed  Europe PubMed DOI
  512. [YEAR:16-10-2000]Llinas-Brunet,M., Bailey,M., Fazal,G., Ghiro,E., Gorys,V., Goulet,S., Halmos,T., Maurice,R., Poirier,M., Poupart,M.A., Rancourt,J., Thibeault,D., Wernic,D. and Lamarre,D.
    Highly potent and selective peptide-based inhibitors of the hepatitis C virus serine protease: towards smaller inhibitors
    Bioorg Med Chem Lett10, 2267-2270. PubMed  Europe PubMed DOI  I
  513. [YEAR:22-2-2000]Narjes,F., Brunetti,M., Colarusso,S., Gerlach,B., Koch,U., Biasiol,G., Fattori,D., De Francesco,R., Matassa,V.G. and Steinkuhler,C.
    alpha-Ketoacids are potent slow binding inhibitors of the hepatitis C virus NS3 protease
    Biochemistry39, 1849-1861. PubMed  Europe PubMed DOI  I
  514. Wright-Minogue,J., Yao,N., Zhang,R., Butkiewicz,N.J., Baroudy,B.M., Lau,J.Y. and Hong,Z.
    Cross-genotypic interaction between hepatitis C virus NS3 protease domains and NS4A cofactors
    J Hepatol32, 497-504. PubMed  Europe PubMed DOI
  515. [YEAR:1-3-2000]Yang,S.H., Lee,C.G., Song,M.K. and Sung,Y.C.
    Internal cleavage of hepatitis C virus NS3 protein is dependent on the activity of NS34A protease
    Virology268, 132-140. PubMed  Europe PubMed DOI
  516. 1999
  517. [YEAR:4-6-1999]Barbato,G., Cicero,D.O., Nardi,M.C., Steinkuhler,C., Cortese,R., De Francesco,R. and Bazzo,R.
    The solution structure of the N-terminal proteinase domain of the hepatitis C virus (HCV) NS3 protein provides new insights into its activation and catalytic mechanism
    J Mol Biol289, 371-384. PubMed  Europe PubMed DOI  S
  518. Sardana,V.V., Blue,J.T., Zugay-Murphy,J., Sardana,M.K. and Kuo,L.C.
    An uniquely purified HCV NS3 protease and NS4A(21-34) peptide form a highly active serine protease complex in peptide hydrolysis
    Protein Expr Purif16, 440-447. PubMed  Europe PubMed DOI
  519. [YEAR:15-11-1999]Yao,N., Reichert,P., Taremi,S.S., Prosise,W.W. and Weber,P.C.
    Molecular views of viral polyprotein processing revealed by the crystal structure of the hepatitis C virus bifunctional protease-helicase
    Structure7, 1353-1363. PubMed  Europe PubMed DOI  S
  520. [YEAR:1-6-1999]Zhang,R., Beyer,B.M., Durkin,J., Ingram,R., Njoroge,F.G., Windsor,W.T. and Malcolm,B.A.
    A continuous spectrophotometric assay for the hepatitis C virus serine protease
    Anal Biochem270, 268-275. PubMed  Europe PubMed DOI  A
  521. 1998
  522. Blight,K.J., Kolykhalov,A.A., Reed,K.E., Agapov,E.V. and Rice,C.M.
    Molecular virology of hepatitis C virus: an update with respect to potential antiviral targets
    Antivir Ther3, 71-81. PubMed  Europe PubMed  V
  523. [YEAR:23-6-1998]Ingallinella,P., Altamura,S., Bianchi,E., Taliani,M., Ingenito,R., Cortese,R., De Francesco,R., Steinkuhler,C. and Pessi,A.
    Potent peptide inhibitors of human hepatitis C virus NS3 protease are obtained by optimizing the cleavage products
    Biochemistry37, 8906-8914. PubMed  Europe PubMed DOI  I
  524. [YEAR:7-7-1998]Llinas-Brunet,M., Bailey,M., Fazal,G., Goulet,S., Halmos,T., Laplante,S., Maurice,R., Poirier,M., Poupart,M.A., Thibeault,D., Wernic,D. and Lamarre,D.
    Peptide-based inhibitors of the hepatitis C virus serine protease
    Bioorg Med Chem Lett8, 1713-1718. PubMed  Europe PubMed DOI  I
  525. [YEAR:6-10-1998]Llinas-Brunet,M., Bailey,M., Deziel,R., Fazal,G., Gorys,V., Goulet,S., Halmos,T., Maurice,R., Poirier,M., Poupart,M.A., Rancourt,J., Thibeault,D., Wernic,D. and Lamarre,D.
    Studies on the C-terminal of hexapeptide inhibitors of the hepatitis C virus serine protease
    Bioorg Med Chem Lett8, 2719-2724. PubMed  Europe PubMed DOI  I
  526. [YEAR:18-8-1998]Martin,F., Dimasi,N., Volpari,C., Perrera,C., Di Marco,S., Brunetti,M., Steinkuhler,C., De Francesco,R. and Sollazzo,M.
    Design of selective eglin inhibitors of HCV NS3 proteinase
    Biochemistry37, 11459-11468. PubMed  Europe PubMed DOI
  527. Pasquo,A., Nardi,M.C., Dimasi,N., Tomei,L., Steinkuhler,C., Delmastro,P., Tramontano,A. and De Francesco,R.
    Rational design and functional expression of a constitutively active single-chain NS4A-NS3 proteinase
    Fold Des3, 433-441. PubMed  Europe PubMed DOI
  528. Ryan,M.D., Monaghan,S. and Flint,M.
    Virus-encoded proteinases of the Flaviviridae
    J Gen Virol79, 947-959. PubMed  Europe PubMed
  529. Wu,Z., Yao,N., Le,H.V. and Weber,P.C.
    Mechanism of autoproteolysis at the NS2-NS3 junction of the hepatitis C virus polyprotein
    Trends Biochem Sci23, 92-94. PubMed  Europe PubMed DOI
  530. Yan,Y., Li,Y., Munshi,S., Sardana,V., Cole,J.L., Sardana,M., Steinkuehler,C., Tomei,L., De Francesco,R., Kuo,L.C. and Chen,Z.
    Complex of NS3 protease and NS4A peptide of BK strain hepatitis C virus: A 2.2 A resolution structure in a hexagonal crystal form
    Protein Sci7, 837-847. PubMed  Europe PubMed DOI  S
  531. 1997
  532. [YEAR:14-11-1997]Babe,L.M. and Craik,C.S.
    Viral proteases: evolution of diverse structural motifs to optimize function
    Cell91, 427-430. PubMed  Europe PubMed
  533. Neddermann,P., Tomei,L., Steinkuhler,C., Gallinari,P., Tramontano,A. and De Francesco,R.
    The nonstructural proteins of the hepatitis C virus: structure and functions
    Biol Chem Hoppe Seyler378, 469-476. PubMed  Europe PubMed
  534. [YEAR:4-4-1997]Urbani,A., Bianchi,E., Narjes,F., Tramontano,A., De Francesco,R., Steinkuhler,C. and Pessi,A.
    Substrate specificity of the hepatitis C virus serine protease NS3
    J Biol Chem272, 9204-9209. PubMed  Europe PubMed DOI
  535. Wilkinson,T.C., Bunyard,P.R., Quirk,K. and Wilkinson,C.S.
    Characterisation of an HCV NS3/NS4A proteinase fusion protein expressed in E.coli using synthetic peptide substrates
    Biochem Soc Trans25, S624-S624. PubMed  Europe PubMed  E
  536. 1996
  537. Bianchi,E., Steinkuhler,C., Taliani,M., Urbani,A., De Francesco,R. and Pessi,A.
    Synthetic depsipeptide substrates for the assay of human hepatitis C virus protease
    Anal Biochem237, 239-244. PubMed  Europe PubMed DOI  A
  538. De Francesco,R., Urbani,A., Nardi,M.C., Tomei,L., Steinkuhler,C. and Tramontano,A.
    A zinc binding site in viral serine proteinases
    Biochemistry35, 13282-13287. PubMed  Europe PubMed DOI
  539. Failla,C.M., Pizzi,E., De Francesco,R. and Tramontano,A.
    Redesigning the substrate specificity of the hepatitis C virus NS3 protease
    Fold Des1, 35-42. PubMed  Europe PubMed
  540. Hamatake,R., Wang,H.G., Butcher,J.A., Bifano,M., Clark,G., Hernandez,D., Zhang,S., Racela,J., Standring,D. and Colonno,R.
    Establishment of an in vitro assay to characterize hepatitis C virus NS3-4A protease trans-processing activity
    Intervirology39, 249-258. PubMed  Europe PubMed  A
  541. Kim,J.L., Morgenstern,K.A., Lin,C., Fox,T., Dwyer,M.D., Landro,J.A., Chambers,S.P., Markland,W., Lepre,C.A., O'Malley,E.T., Harbeson,S.L., Rice,C.M., Murcko,M.A., Caron,P.R. and Thomson,J.A.
    Crystal structure of the hepatitis C virus NS3 protease domain complexed with a synthetic NS4A cofactor peptide
    Cell87, 343-355. PubMed  Europe PubMed DOI  S
  542. Lohmann,V., Koch,J.O. and Bartenschlager,R.
    Processing pathways of the hepatitis C virus proteins
    J Hepatol24 Suppl 2, 11-19. PubMed  Europe PubMed  V
  543. Love,R.A., Parge,H.E., Wickersham,J.A., Hostomsky,Z., Habuka,N., Moomaw,E.W., Adachi,T. and Hostomska,Z.
    The crystal structure of hepatitis C virus NS3 proteinase reveals a trypsin-like fold and a structural zinc binding site
    Cell87, 331-342. PubMed  Europe PubMed DOI  S
  544. Rice,C.M.
    Flaviridae: the viruses and their replication
    3, 931-959.
  545. Shimizu,Y., Yamaji,K., Masuho,Y., Yokota,T., Inoue,H., Sudo,K., Satoh,S. and Shimotohno,K.
    Identification of the sequence on NS4A required for enhanced cleavage of the NS5A/5B site by hepatitis C virus NS3 protease
    J Virol70, 127-132. PubMed  Europe PubMed
  546. Song,O.K., Cho,O.H., Hahm,B. and Jang,S.K.
    Development of an in-vivo assay system suitable for screening inhibitors of hepatitis C viral protease
    Mol Cells6, 183-189.  A
  547. Steinkuhler,C., Tomei,L. and De Francesco,R.
    In vitro activity of hepatitis C virus protease NS3 purified from recombinant baculovirus-infected Sf9 cells
    J Biol Chem271, 6367-6373. PubMed  Europe PubMed DOI
  548. Sudo,K., Inoue,H., Shimizu,Y., Yamaji,K., Konno,K., Shigeta,S., Kaneko,T., Yokota,T. and Shimotohno,K.
    Establishment of an in vitro assay system for screening hepatitis C virus protease inhibitors using high performance liquid chromatography
    Antiviral Res32, 9-18. PubMed  Europe PubMed DOI  A
  549. Taliani,M., Bianchi,E., Narjes,F., Fossatelli,M., Urbani,A., Steinkuhler,C., De Francesco,R. and Pessi,A.
    A continuous assay of hepatitis C virus protease based on resonance energy transfer depsipeptide substrates
    Anal Biochem240, 60-67. PubMed  Europe PubMed DOI  A
  550. 1995
  551. Bartenschlager,R., Ahlborn-Laake,L., Yasargil,K., Mous,J. and Jacobsen,H.
    Substrate determinants for cleavage in cis and in trans by the hepatitis C virus NS3 proteinase
    J Virol69, 198-205. PubMed  Europe PubMed  P
  552. Bouffard,P., Bartenschlager,R., Ahlborn-Laake,L., Mous,J., Roberts,N. and Jacobsen,H.
    An in vitro assay for hepatitis C virus NS3 serine proteinase
    Virology209, 52-59. PubMed  Europe PubMed DOI  A
  553. Lin,C. and Rice,C.M.
    The hepatitis C virus NS3 serine proteinase and NS4A cofactor: establishment of a cell-free trans-processing assay
    Proc Natl Acad Sci U S A92, 7622-7626. PubMed  Europe PubMed DOI  A
  554. Overton,H., McMillan,D., Gillespie,F. and Mills,J.
    Recombinant baculovirus-expressed NS3 proteinase of hepatitis C virus shows activity in cell-based and in vitro assays
    J Gen Virol76, 3009-3019. PubMed  Europe PubMed  A
  555. 1994
  556. Failla,C., Tomei,L. and De Francesco,R.
    Both NS3 and NS4A are required for proteolytic processing of hepatitis C virus nonstructural proteins
    J Virol68, 3753-3760. PubMed  Europe PubMed
  557. Kolykhalov,A.A., Agapov,E.V. and Rice,C.M.
    Specificity of the hepatitis C virus NS3 serine protease: effects of substitutions at the 3/4a, 4a/4b, 4b/5a, and 5a/5b cleavage sites on polyprotein processing
    J Virol68, 7525-7533. PubMed  Europe PubMed
  558. Leinbach,S.S., Bhat,R.A., Xia,S.M., Hum,W.T., Stauffer,B., Davis,A.R., Hung,P.P. and Mizutani,S.
    Substrate specificity of the NS3 serine proteinase of hepatitis C virus as determined by mutagenesis at the NS3/NS4A junction
    Virology204, 163-169. PubMed  Europe PubMed DOI  P
  559. Lin,C., Pragai,B.M., Grakoui,A., Xu,J. and Rice,C.M.
    Hepatitis C virus NS3 serine proteinase: trans-cleavage requirements and processing kinetics
    J Virol68, 8147-8157. PubMed  Europe PubMed
  560. Pizzi,E., Tramontano,A., Tomei,L., La Monica,N., Failla,C., Sardana,M., Wood,T. and De Francesco,R.
    Molecular model of the specificity pocket of the hepatitis C virus protease: implications for substrate recognition
    Proc Natl Acad Sci U S A91, 888-892. PubMed  Europe PubMed
  561. Tanji,Y., Hijikata,M., Hirowatari,Y. and Shimotohno,K.
    Hepatitis C virus polyprotein processing: kinetics and mutagenic analysis of serine proteinase-dependent cleavage
    J Virol68, 8418-8422. PubMed  Europe PubMed
  562. 1993
  563. Bartenschlager,R., Ahlborn-Laake,L., Mous,J. and Jacobsen,H.
    Nonstructural protein 3 of the hepatitis C virus encodes a serine-type proteinase required for cleavage at the NS3/4 and NS4/5 junctions
    J Virol67, 3835-3844. PubMed  Europe PubMed
  564. Eckart,M.R., Selby,M., Masiarz,F., Lee,C., Berger,K., Crawford,K., Kuo,C., Kuo,G., Houghton,M. and Choo,Q.L.
    The hepatitis C virus encodes a serine protease involved in processing of the putative nonstructural proteins from the viral polyprotein precursor
    Biochem Biophys Res Commun192, 399-406. PubMed  Europe PubMed DOI
  565. [YEAR:15-11-1993]Grakoui,A., McCourt,D.W., Wychowski,C., Feinstone,S.M. and Rice,C.M.
    A second hepatitis C virus-encoded proteinase
    Proc Natl Acad Sci U S A90, 10583-10587. PubMed  Europe PubMed DOI
  566. Grakoui,A., McCourt,D.W., Wychowski,C., Feinstone,S.M. and Rice,C.M.
    Characterization of the hepatitis C virus-encoded serine proteinase: determination of proteinase-dependent polyprotein cleavage sites
    J Virol67, 2832-2843. PubMed  Europe PubMed
  567. Hijikata,M., Mizushima,H., Akagi,T., Mori,S., Kakiuchi,N., Kato,N., Tanaka,T., Kimura,K. and Shimotohno,K.
    Two distinct proteinase activities required for the processing of a putative nonstructural precursor protein of hepatitis C virus
    J Virol67, 4665-4675. PubMed  Europe PubMed
  568. Tomei,L., Failla,C., Santolini,E., De Francesco,R. and La Monica,N.
    NS3 is a serine protease required for processing of hepatitis C virus polyprotein
    J Virol67, 4017-4026. PubMed  Europe PubMed
  569. 1989
  570. [YEAR:21-4-1989]Choo,Q.L., Kuo,G., Weiner,A.J., Overby,L.R., Bradley,D.W. and Houghton,M.
    Isolation of a cDNA clone derived from a blood-borne non-A, non-B viral hepatitis genome
    Science244, 359-362. PubMed  Europe PubMed