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Literature for peptidase C01.034: cathepsin S

Summary Gene structure Alignment Tree Sequences Sequence features Distribution Structure Literature Substrates Pharma

(References are filtered for relevance to Inhibitor. To remove the filter click here. See explanation.)

    2025
  1. Bentley,D., Mannino,M., Manchester,M., Teixeira,P.C., Reis,B., Boyce,M. and Nagel,S.
    A randomized, double-blind, placebo-controlled, multiple dose, parallel study to investigate the effects of a cathepsin S inhibitor in celiac disease
    Clin Transl Sci18, e13901-e13901. PubMed  Europe PubMed DOI  I
    2. 2024
  2. Zhang,Y., Yang,L., Gan,Y., Zhao,C., Zhou,C., Chen,J., Yin,Y., Xia,S., Yang,H., Bao,X., Zhang,M., Xu,Y. and Li,J.
    Benzydamine attenuates microglia-mediated neuroinflammation and ischemic brain injury by targeting cathepsin s
    Int Immunopharmacol146, 113824-113824. PubMed  Europe PubMed DOI  I
    3. 2023
  3. Abdoli,M., Krasniqi,V., Bonardi,A., Gutschow,M., Supuran,C.T. and Zalubovskis,R.
    4-Cyanamido-substituted benzenesulfonamides act as dual carbonic anhydrase and cathepsin inhibitors
    Bioorg Chem139, 106725-106725. PubMed  Europe PubMed DOI  I
  4. Fuchs,N., Meta,M., Lantzberg,B., Bros,M., Ling Kuan,S., Weil,T. and Schirmeister,T.
    Subnanomolar Cathepsin S Inhibitors with High Selectivity: Optimizing Covalent Reversible alpha-Fluorovinylsulfones and alpha-Sulfonates as Potential Immunomodulators in Cancer
    ChemMedChem18, e202300160-e202300160. PubMed  Europe PubMed DOI  I
  5. Huang,H., Zhang,Y., Xu,X., Liu,Y., Zhao,J., Ma,L., Lei,J., Ge,W., Li,N., Ma,E., Li,Y. and Yuan,L.
    Design and synthesis of dual cathepsin L and S inhibitors and antimetastatic activity evaluation in pancreatic cancer cells
    Bioorg Med Chem Lett80, 129087-129087. PubMed  Europe PubMed DOI  I
    6. 2021
  6. Oldak,L., Sankiewicz,A., Zelazowska-Rutkowska,B., Cylwik,B., Lukaszewski,Z., Skoczylas,M. and Gorodkiewicz,E.
    Two SPRi biosensors for the determination of cathepsin S in blood plasma
    Talanta225, 121900-121900. PubMed  Europe PubMed DOI  I
    7. 2020
  7. Ahmad,S., Bhagwati,S., Kumar,S., Banerjee,D. and Siddiqi,M.I.
    Molecular modeling assisted identification and biological evaluation of potent cathepsin S inhibitors
    J Mol Graph Model96, 107512-107512. PubMed  Europe PubMed DOI  I
  8. Cianni,L., Rocho,F.D.R., Rosini,F., Bonatto,V., Ribeiro,J.F.R., Lameira,J., Leitao,A., Shamim,A. and Montanari,C.A.
    Optimization strategy of single-digit nanomolar cross-class inhibitors of mammalian and protozoa cysteine proteases
    Bioorg Chem101, 104039-104039. PubMed  Europe PubMed DOI  I
  9. Lai,C.H., Chang,J.Y., Wang,K.C., Lee,F.T., Wu,H.L. and Cheng,T.L.
    Pharmacological inhibition of cathepsin S suppresses abdominal aortic aneurysm in mice
    Eur J Vasc Endovasc Surg PubMed  Europe PubMed DOI  U  I
  10. Lemke,C., Cianni,L., Feldmann,C., Gilberg,E., Yin,J., Dos Reis Rocho,F., De Vita,D., Bartz,U., Bajorath,J., Montanari,C.A. and Gutschow,M.
    N-Sulfonyl dipeptide nitriles as inhibitors of human cathepsin S: In silico design, synthesis and biochemical characterization
    Bioorg Med Chem Lett30, 127420-127420. PubMed  Europe PubMed DOI  I
  11. van Dalen,F.J., Bakkum,T., Van Leeuwen,T., Groenewold,M., Deu,E., Koster,A.J., van Kasteren,S.I. and Verdoes,M.
    Application of a Highly Selective Cathepsin S Two-step Activity-Based Probe in Multicolor Bio-Orthogonal Correlative Light-Electron Microscopy
    Front Chem8, 628433-628433. PubMed  Europe PubMed DOI  I
    12. 2019
  12. Chaput,L., Selwa,E., Elisee,E. and Iorga,B.I.
    Blinded evaluation of cathepsin S inhibitors from the D3RGC3 dataset using molecular docking and free energy calculations
    J Comput Aided Mol Des33, 93-103. PubMed  Europe PubMed DOI  I
  13. He,X., Man,V.H., Ji,B., Xie,X.Q. and Wang,J.
    Calculate protein-ligand binding affinities with the extended linear interaction energy method: application on the cathepsin S set in the D3R Grand Challenge 3
    J Comput Aided Mol Des33, 105-117. PubMed  Europe PubMed DOI  I
  14. Klinngam,W., Janga,S.R., Lee,C., Ju,Y., Yarber,F., Shah,M., Guo,H., Wang,D., MacKay,J.A., Edman,M.C. and Hamm-Alvarez,S.F.
    Inhibition of cathepsin S reduces lacrimal gland inflammation and increases tear flow in a mouse model of Sjogren's syndrome
    Sci Rep9, 9559-9559. PubMed  Europe PubMed DOI  I
  15. Shockey,W.A., Kieslich,C.A., Wilder,C.L., Watson,V. and Platt,M.O.
    Dynamic model of protease state and inhibitor trafficking to predict protease activity in breast cancer cells
    Cell Mol Bioeng12, 275-288. PubMed  Europe PubMed DOI  I
  16. Small,D.M., Brown,R.R., Doherty,D.F., Abladey,A., Zhou-Suckow,Z., Delaney,R.J., Kerrigan,L., Dougan,C.M., Borensztajn,K.S., Holsinger,L., Booth,R., Scott,C.J., Lopez-Campos,G., Elborn,J.S., Mall,M.A., Weldon,S. and Taggart,C.C.
    Targeting of cathepsin S reduces cystic fibrosis-like lung disease
    Eur Respir J53, 1801523-1801523. PubMed  Europe PubMed DOI  K  I
    17. 2018
  17. Chen,C.Y., Chen,C.Y., Liu,C.C. and Chen,C.P.
    Omega-3 polyunsaturated fatty acids reduce preterm labor by inhibiting trophoblast cathepsin S and inflammasome activation
    Clin Sci (Lond)132, 2221-2239. PubMed  Europe PubMed DOI  I
  18. Kubo,K., Kawato,Y., Nakamura,K., Nakajima,Y., Nakagawa,T.Y., Hanaoka,K., Oshima,S., Fukahori,H., Inami,M., Morokata,T. and Higashi,Y.
    Effective suppression of donor specific antibody production by cathepsin S inhibitors in a mouse transplantation model
    Eur J Pharmacol838, 145-152. PubMed  Europe PubMed DOI  I
  19. Tber,Z., Wartenberg,M., Jacques,J.E., Roy,V., Lecaille,F., Warszycki,D., Bojarski,A.J., Lalmanach,G. and Agrofoglio,L.A.
    Selective inhibition of human cathepsin S by 2,4,6-trisubstituted 1,3,5-triazine analogs
    Bioorg Med Chem26, 4310-4319. PubMed  Europe PubMed DOI  I
  20. Yuan,L., Sheng,L., He,W., Zou,C., Hu,B., Liu,J., Ge,W., Liu,Y., Wang,J. and Ma,E.
    Discovery of novel cathepsin inhibitors with potent anti-metastatic effects in breast cancer cells
    Bioorg Chem81, 672-680. PubMed  Europe PubMed DOI  I
    21. 2017
  21. Ahmad,S. and Siddiqi,M.I.
    Insights from molecular modeling into the selective inhibition of cathepsin S by its inhibitor
    J Mol Model23, 92-92. PubMed  Europe PubMed DOI  I
  22. Galibert,M., Wartenberg,M., Lecaille,F., Saidi,A., Mavel,S., Joulin-Giet,A., Korkmaz,B., Bromme,D., Aucagne,V., Delmas,A.F. and Lalmanach,G.
    Substrate-derived triazolo- and azapeptides as inhibitors of cathepsins K and S
    Eur J Med Chem144, 201-210. PubMed  Europe PubMed DOI  I
  23. Hsieh,M.J., Lin,C.W., Chen,M.K., Chien,S.Y., Lo,Y.S., Chuang,Y.C., Hsi,Y.T., Lin,C.C., Chen,J.C. and Yang,S.F.
    Inhibition of cathepsin S confers sensitivity to methyl protodioscin in oral cancer cells via activation of p38 MAPK/JNK signaling pathways
    Sci Rep7, 45039-45039. PubMed  Europe PubMed DOI  I
  24. Tato,M., Kumar,S.V., Liu,Y., Mulay,S.R., Moll,S., Popper,B., Eberhard,J.N., Thomasova,D., Rufer,A.C., Gruner,S., Haap,W., Hartmann,G. and Anders,H.J.
    Cathepsin S inhibition combines control of systemic and peripheral pathomechanisms of autoimmune tissue injury
    Sci Rep7, 2775-2775. PubMed  Europe PubMed DOI  I
  25. Thanei,S., Theron,M., Silva,A.P., Reis,B., Branco,L., Schirmbeck,L., Kolb,F.A., Haap,W., Schindler,T. and Trendelenburg,M.
    Cathepsin S inhibition suppresses autoimmune-triggered inflammatory responses in macrophages
    Biochem Pharmacol146, 151-164. PubMed  Europe PubMed DOI  I
  26. Yan,X., Wu,C., Chen,T., Santos,M.M., Liu,C.L., Yang,C., Zhang,L., Ren,J., Liao,S., Guo,H., Sukhova,G.K. and Shi,G.P.
    Cathepsin S inhibition changes regulatory T-cell activity in regulating bladder cancer and immune cell proliferation and apoptosis
    Mol Immunol82, 66-74. PubMed  Europe PubMed DOI  I
    27. 2016
  27. Hewitt,E., Pitcher,T., Rizoska,B., Tunblad,K., Henderson,I., Sahlberg,B.L., Grabowska,U., Classon,B., Edenius,C., Malcangio,M. and Lindstrom,E.
    Selective cathepsin S inhibition with MIV-247 attenuates mechanical allodynia and enhances the antiallodynic effects of gabapentin and pregabalin in a mouse model of neuropathic pain
    J Pharmacol Exp Ther358, 387-396. PubMed  Europe PubMed DOI  I
  28. Huang,C.C., Lee,C.C., Lin,H.H. and Chang,J.Y.
    Cathepsin S attenuates endosomal EGFR signalling: a mechanical rationale for the combination of cathepsin S and EGFR tyrosine kinase inhibitors
    Sci Rep6, 29256-29256. PubMed  Europe PubMed DOI  I
  29. Ihmaid,S.K., Ahmed,H.E., Zayed,M.F. and Abadleh,M.M.
    Self organizing map-based classification of cathepsin K and S inhibitors with different selectivity profiles using different structural molecular fingerprints: design and application for discovery of novel hits
    Molecules21, 175-175. PubMed  Europe PubMed DOI  I
  30. Plebanek,E., Chevrier,F., Roy,V., Garenne,T., Lecaille,F., Warszycki,D., Bojarski,A.J., Lalmanach,G. and Agrofoglio,L.A.
    Straightforward synthesis of 2,4,6-trisubstituted 1,3,5-triazine compounds targeting cysteine cathepsins K and S
    Eur J Med Chem121, 12-20. PubMed  Europe PubMed DOI  I
  31. Wilkinson,R.D., Young,A., Burden,R.E., Williams,R. and Scott,C.J.
    A bioavailable cathepsin S nitrile inhibitor abrogates tumor development
    Mol Cancer15, 29-29. PubMed  Europe PubMed DOI  I
    32. 2015
  32. Barlow,N., Nasser,Y., Zhao,P., Sharma,N., Guerrero-Alba,R., Edgington-Mitchell,L.E., Lieu,T., Veldhuis,N.A., Poole,D.P., Conner,J.W., Lindstrom,E., Craig,A.W., Graham,B., Vanner,S.J. and Bunnett,N.W.
    Demonstration of elevated levels of active cathepsin S in dextran sulfate sodium colitis using a new activatable probe
    Neurogastroenterol Motil27, 1675-1680. PubMed  Europe PubMed DOI  L  I
  33. Figueiredo,J.L., Aikawa,M., Zheng,C., Aaron,J., Lax,L., Libby,P., de Lima Filho,J.L., Gruener,S., Fingerle,J., Haap,W., Hartmann,G. and Aikawa,E.
    Selective cathepsin S inhibition attenuates atherosclerosis in apolipoprotein E-deficient mice with chronic renal disease
    Am J Pathol185, 1156-1166. PubMed  Europe PubMed DOI  I
  34. Kohl,F., Schmitz,J., Furtmann,N., Schulz-Fincke,A.C., Mertens,M.D., Kuppers,J., Benkhoff,M., Tobiasch,E., Bartz,U., Bajorath,J., Stirnberg,M. and Gutschow,M.
    Design, characterization and cellular uptake studies of fluorescence-labeled prototypic cathepsin inhibitors
    Org Biomol Chem13, 10310-10323. PubMed  Europe PubMed DOI  I
  35. Rupanagudi,K.V., Kulkarni,O.P., Lichtnekert,J., Darisipudi,M.N., Mulay,S.R., Schott,B., Gruner,S., Haap,W., Hartmann,G. and Anders,H.J.
    Cathepsin S inhibition suppresses systemic lupus erythematosus and lupus nephritis because cathepsin S is essential for MHC class II-mediated CD4 T cell and B cell priming
    Ann Rheum Dis74, 452-463. PubMed  Europe PubMed DOI  I
    36. 2014
  36. Battu,M.B., Chandra,A.M., Sriram,D. and Yogeeswari,P.
    Pharmacophore-based 3DQSAR and molecular docking studies to identify new non-peptidic inhibitors of cathepsin S
    Curr Med Chem21, 1910-1921. PubMed  Europe PubMed  I
  37. Bernard,N.J.
    Connective tissue diseases. Inhibiting cathepsin S to treat SLE and lupus nephritis
    Nat Rev Rheumatol10, 66-66. PubMed  Europe PubMed DOI  I
  38. Chua,K.C., Pietsch,M., Zhang,X., Hautmann,S., Chan,H.Y., Bruning,J.B., Gutschow,M. and Abell,A.D.
    Macrocyclic protease inhibitors with reduced peptide character
    Angew Chem Int Ed Engl53, 7828-7831. PubMed  Europe PubMed DOI  I
  39. Jadhav,P.K., Schiffler,M.A., Gavardinas,K., Kim,E.J., Matthews,D.P., Staszak,M.A., Coffey,D.S., Shaw,B.W., Cassidy,K.C., Brier,R.A., Zhang,Y., Christie,R.M., Matter,W.F., Qing,K., Durbin,J.D., Wang,Y. and Deng,G.G.
    Discovery of cathepsin S inhibitor LY3000328 for the treatment of abdominal aortic aneurysm
    ACS Med Chem Lett5, 1138-1142. PubMed  Europe PubMed DOI  I
  40. Kim,M., Jeon,J., Baek,J., Choi,J., Park,E.J., Song,J., Bang,H., Suh,K.H., Kim,Y.H., Kim,J., Kim,D., Min,K.H. and Lee,K.-O.
    Synthesis of vinyl sulfone-tethered proline derivatives as highly selective cathepsin S inhibitors
    Bull Korean Chem Soc35, 345-346. DOI  I
  41. Lafarge,J.C., Pini,M., Pelloux,V., Orasanu,G., Hartmann,G., Venteclef,N., Sulpice,T., Shi,G.P., Clement,K. and Guerre-Millo,M.
    Cathepsin S inhibition lowers blood glucose levels in mice
    Diabetologia57, 1674-1683. PubMed  Europe PubMed DOI  I
  42. Payne,C.D., Deeg,M.A., Chan,M., Tan,L.H., LaBell,E.S., Shen,T. and DeBrota,D.J.
    Pharmacokinetics and pharmacodynamics of the cathepsin S inhibitor, LY3000328, in healthy subjects
    Br J Clin Pharmacol78, 1334-1342. PubMed  Europe PubMed DOI  I
  43. Tsai,J.Y., Lee,M.J., Chang,M.D., Wang,H.C., Lin,C.C. and Huang,H.
    Effects of novel human cathepsin S inhibitors on cell migration in human cancer cells
    J Enzyme Inhib Med Chem29, 538-546. PubMed  Europe PubMed DOI  I
    44. 2013
  44. Feth,M.P., Heyse,W., Baumgartner,B., Nagel,N., Tappertzhofen,C., Olpp,T., Jurascheck,J., Ulrich,J., Helmdach,L. and Petzoldt,C.
    From laboratory to pilot plant: the solid-state process development of a highly potent cathepsin S/K inhibitor
    Eur J Pharm Biopharm83, 436-448. PubMed  Europe PubMed DOI  I
  45. Hilpert,H., Mauser,H., Humm,R., Anselm,L., Kuehne,H., Hartmann,G., Gruener,S., Banner,D.W., Benz,J., Gsell,B., Kuglstatter,A., Stihle,M., Thoma,R., Sanchez,R.A., Iding,H., Wirz,B. and Haap,W.
    Identification of potent and selective cathepsin S inhibitors containing different central cyclic scaffolds
    J Med Chem56, 9789-9801. PubMed  Europe PubMed DOI  I
  46. Huang,C.C., Chen,K.L., Cheung,C.H. and Chang,J.Y.
    Autophagy induced by cathepsin S inhibition induces early ROS production, oxidative DNA damage, and cell death via xanthine oxidase
    Free Radic Biol Med65, 1473-1486. PubMed  Europe PubMed DOI  I
  47. Kim,M., Jeon,J., Song,J., Suh,K.H., Kim,Y.H., Min,K.H. and Lee,K.O.
    Synthesis of proline analogues as potent and selective cathepsin S inhibitors
    Bioorg Med Chem Lett23, 3140-3144. PubMed  Europe PubMed DOI  I
  48. Pehere,A.D., Pietsch,M., Gutschow,M., Neilsen,P.M., Pedersen,D.S., Nguyen,S., Zvarec,O., Sykes,M.J., Callen,D.F. and Abell,A.D.
    Synthesis and extended activity of triazole-containing macrocyclic protease inhibitors
    Chemistry19, 7975-7981. PubMed  Europe PubMed DOI  I
  49. Wiener,J.J., Wickboldt,A.T., Nguyen,S., Sun,S., Rynberg,R., Rizzolio,M., Karlsson,L., Edwards,J.P. and Grice,C.A.
    Pyrazole-based arylalkyne cathepsin S inhibitors. Part III: modification of P4 region
    Bioorg Med Chem Lett23, 1070-1074. PubMed  Europe PubMed DOI  I
  50. Xu,J., Wang,H., Ding,K., Lu,X., Li,T., Wang,J., Wang,C. and Wang,J.
    Inhibition of cathepsin S produces neuroprotective effects after traumatic brain injury in mice
    Mediators Inflamm2013, 187873-187873. PubMed  Europe PubMed DOI  I
    51. 2012
  51. Chen,K.L., Chang,W.S., Cheung,C.H., Lin,C.C., Huang,C.C., Yang,Y.N., Kuo,C.P., Kuo,C.C., Chang,Y.H., Liu,K.J., Wu,C.M. and Chang,J.Y.
    Targeting cathepsin S induces tumor cell autophagy via the EGFR-Erk signaling pathway
    Cancer Lett317, 89-98. PubMed  Europe PubMed DOI  I
  52. Frizler,M., Schmitz,J., Schulz-Fincke,A.C. and Gutschow,M.
    Selective nitrile inhibitors to modulate the proteolytic synergism of cathepsins S and F
    J Med Chem55, 5982-5986. PubMed  Europe PubMed DOI  I
  53. Fujii,H., Ivison,S.M., Shimizu,H., Kajiwara,R., Kariminia,A., Yan,M., Dutz,J.P. and Schultz,K.R.
    Inhibition of cathepsin S reduces allogeneic T cell priming but not graft-versus-host disease against minor histocompatibility antigens
    Biol Blood Marrow Transplant18, 546-556. PubMed  Europe PubMed DOI  I
  54. Moss,N., Xiong,Z., Burke,M., Cogan,D., Gao,D.A., Haverty,K., Heim-Riether,A., Hickey,E.R., Nagaraja,R., Netherton,M., O'Shea,K., Ramsden,P., Schwartz,R., Shih,D.T., Ward,Y., Young,E. and Zhang,Q.
    Exploration of cathepsin S inhibitors characterized by a triazole P1-P2 amide replacement
    Bioorg Med Chem Lett22, 7189-7193. PubMed  Europe PubMed DOI  I
    55. 2011
  55. Baugh,M., Black,D., Westwood,P., Kinghorn,E., McGregor,K., Bruin,J., Hamilton,W., Dempster,M., Claxton,C., Cai,J., Bennett,J., Long,C., McKinnon,H., Vink,P., Hoed,L., Gorecka,M., Vora,K., Grant,E., Percival,M.D., Boots,A.M. and van Lierop,M.J.
    Therapeutic dosing of an orally active, selective cathepsin S inhibitor suppresses disease in models of autoimmunity
    J Autoimmun36, 201-209. PubMed  Europe PubMed DOI  I
  56. Deschamps,K., Cromlish,W., Weicker,S., Lamontagne,S., Huszar,S.L., Gauthier,J.Y., Mudgett,J.S., Guimond,A., Romand,R., Frossard,N., Percival,M.D., Slipetz,D. and Tan,C.M.
    Genetic and pharmacological evaluation of cathepsin S in a mouse model of asthma
    Am J Respir Cell Mol Biol45, 81-87. PubMed  Europe PubMed DOI  K  I
  57. Jiang,C., Sun,W., Zhou,X.P. and Yang,X.H.
    Cathepsin S inhibitors and the structure-activity relationship: research advances
    J Int Pharm Res38, 182-188.  I
  58. Kerns,J.K., Nie,H., Bondinell,W., Widdowson,K.L., Yamashita,D.S., Rahman,A., Podolin,P.L., Carpenter,D.C., Jin,Q., Riflade,B., Dong,X., Nevins,N., Keller,P.M., Mitchell,L. and Tomaszek,T.
    Azepanone-based inhibitors of human cathepsin S: optimization of selectivity via the P2 substituent
    Bioorg Med Chem Lett21, 4409-4415. PubMed  Europe PubMed DOI  I
  59. Lee-Dutra,A., Wiener,D.K. and Sun,S.
    Cathepsin S inhibitors: 2004 - 2010
    Expert Opin Ther Pat21, 311-337. PubMed  Europe PubMed DOI  V  I
  60. Loser,R.
    Cathepsin S inhibitors: WO2010070615
    Expert Opin Ther Pat21, 585-591. PubMed  Europe PubMed DOI  I
  61. Veilleux,A., Black,W.C., Gauthier,J.Y., Mellon,C., Percival,M.D., Tawa,P. and Falgueyret,J.P.
    Probing cathepsin S activity in whole blood by the activity-based probe BIL-DMK: cellular distribution in human leukocyte populations and evidence of diurnal modulation
    Anal Biochem411, 43-49. PubMed  Europe PubMed DOI  I
    62. 2010
  62. Ameriks,M.K., Bembenek,S.D., Burdett,M.T., Choong,I.C., Edwards,J.P., Gebauer,D., Gu,Y., Karlsson,L., Purkey,H.E., Staker,B.L., Sun,S., Thurmond,R.L. and Zhu,J.
    Diazinones as P2 replacements for pyrazole-based cathepsin S inhibitors
    Bioorg Med Chem Lett20, 4060-4064. PubMed  Europe PubMed DOI  I
  63. Cai,J., Bennett,D.J., Rankovic,Z., Dempster,M., Fradera,X., Gillespie,J., Cumming,I., Finlay,W., Baugh,M., Boucharens,S., Bruin,J., Cameron,K.S., Hamilton,W., Kerr,J., Kinghorn,E., McGarry,G., Robinson,J., Scullion,P., Uitdehaag,J.C., van Zeeland,M., Potin,D., Saniere,L., Fouquet,A., Chevallier,F., Deronzier,H., Dorleans,C. and Nicolai,E.
    2-Phenyl-9H-purine-6-carbonitrile derivatives as selective cathepsin S inhibitors
    Bioorg Med Chem Lett20, 4447-4450. PubMed  Europe PubMed DOI  I
  64. Cai,J., Baugh,M., Black,D., Long,C., Jonathan Bennett,D., Dempster,M., Fradera,X., Gillespie,J., Andrews,F., Boucharens,S., Bruin,J., Cameron,K.S., Cumming,I., Hamilton,W., Jones,P.S., Kaptein,A., Kinghorn,E., Maidment,M., Martin,I., Mitchell,A., Rankovic,Z., Robinson,J., Scullion,P., Uitdehaag,J.C., Vink,P., Westwood,P., van Zeeland,M., van Berkom,L., Bastiani,M. and Meulemans,T.
    6-Phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile as cathepsin S inhibitors
    Bioorg Med Chem Lett20, 4350-4354. PubMed  Europe PubMed DOI  I
  65. Cai,J., Robinson,J., Belshaw,S., Everett,K., Fradera,X., van Zeeland,M., van Berkom,L., van Rijnsbergen,P., Popplestone,L., Baugh,M., Dempster,M., Bruin,J., Hamilton,W., Kinghorn,E., Westwood,P., Kerr,J., Rankovic,Z., Arbuckle,W., Bennett,D.J., Jones,P.S., Long,C., Martin,I., Uitdehaag,J.C. and Meulemans,T.
    Trifluoromethylphenyl as P2 for ketoamide-based cathepsin S inhibitors
    Bioorg Med Chem Lett20, 6890-6894. PubMed  Europe PubMed DOI  I
  66. Cai,J., Fradera,X., van Zeeland,M., Dempster,M., Cameron,K.S., Bennett,D.J., Robinson,J., Popplestone,L., Baugh,M., Westwood,P., Bruin,J., Hamilton,W., Kinghorn,E., Long,C. and Uitdehaag,J.C.
    4-(3-Trifluoromethylphenyl)-pyrimidine-2-carbonitrile as cathepsin S inhibitors: N3, not N1 is critically important
    Bioorg Med Chem Lett20, 4507-4510. PubMed  Europe PubMed DOI  I
  67. Chen,J.C., Uang,B.J., Lyu,P.C., Chang,J.Y., Liu,K.J., Kuo,C.C., Hsieh,H.P., Wang,H.C., Cheng,C.S., Chang,Y.H., Chang,M.D., Chang,W.S. and Lin,C.C.
    Design and synthesis of alpha-ketoamides as cathepsin S inhibitors with potential applications against tumor invasion and angiogenesis
    J Med Chem53, 4545-4549. PubMed  Europe PubMed DOI  I
  68. Frizler,M., Stirnberg,M., Sisay,M.T. and Gutschow,M.
    Development of nitrile-based peptidic inhibitors of cysteine cathepsins
    Curr Top Med Chem10, 294-322. PubMed  Europe PubMed DOI  T  I
  69. Isabel,E., Bateman,K.P., Chauret,N., Cromlish,W., Desmarais,S., Duong,l.T., Falgueyret,J.P., Gauthier,J.Y., Lamontagne,S., Lau,C.K., Leger,S., LeRiche,T., Levesque,J.F., Li,C.S., Masse,F., McKay,D.J., Mellon,C., Nicoll-Griffith,D.A., Oballa,R.M., Percival,M.D., Riendeau,D., Robichaud,J., Rodan,G.A., Rodan,S.B., Seto,C., Therien,M., Truong,V.L., Wesolowski,G., Young,R.N., Zamboni,R. and Black,W.C.
    The discovery of MK-0674, an orally bioavailable cathepsin K inhibitor
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