Literature for peptidase C01.063: falcipain-3

Summary Alignment Tree Sequences Sequence features Distribution Structure Literature Substrates

(Topics flags: S Structure, K Knockout, P Specificity, I Inhibitor, V Review. To select only the references relevant to a single topic, click the link above. See explanation.)

    2024
  1. Hernandez Gonzalez,J.E., Salas-Sarduy,E., Alvarez,L.H., Valiente,P.A., Arni,R.K. and Pascutti,P.G.
    Three decades targeting falcipains to develop antiplasmodial agents: what have we learned and what can be done next?
    Curr Med Chem31, 2234-2263. PubMed  Europe PubMed DOI
  2. Madhav,H., Reddy,G.S., Rizvi,Z., Jameel,E., Patel,T.S., Rahman,A., Yadav,V., Fatima,S., Heyat,F., Pal,K., Minju-Op,A., Subbarao,N., Bhattacharjee,S., Dixit,B.C., Sijwali,P.S. and Hoda,N.
    Reinvestigation of diphenylmethylpiperazine analogues of pyrazine as new class of Plasmodial cysteine protease inhibitors for the treatment of malaria
    RSC Med Chem15, 1022-1037. PubMed  Europe PubMed DOI  I
  3. 2023
  4. Patra,J., Rana,D., Arora,S., Pal,M. and Mahindroo,N.
    Falcipains: Biochemistry, target validation and structure-activity relationship studies of inhibitors as antimalarials
    Eur J Med Chem252, 115299-115299. PubMed  Europe PubMed DOI
  5. 2020
  6. Ettari,R., Previti,S., Di Chio,C. and Zappala,M.
    Falcipain-2 and falcipain-3 inhibitors as promising antimalarial agents
    Curr Med Chem PubMed  Europe PubMed DOI  V
  7. Mishra,M., Singh,V., Tellis,M.B., Joshi,R.S., Pandey,K.C. and Singh,S.
    Cyclic peptide engineered from phytocystatin inhibitory hairpin loop as an effective modulator of falcipains and potent antimalarial
    J Biomol Struct Dyn1-13. PubMed  Europe PubMed DOI
  8. Rosenthal,P.J.
    Falcipain cysteine proteases of malaria parasites: an update
    Biochim Biophys Acta Proteins Proteom1868, 140362-140362. PubMed  Europe PubMed DOI
  9. 2019
  10. Pasupureddy,R., Verma,S., Pant,A., Sharma,R., Seshadri,S., Pande,V., Saxena,A.K., Dixit,R. and Pandey,K.C.
    Crucial residues in falcipains that mediate hemoglobin hydrolysis
    Exp Parasitol197, 43-50. PubMed  Europe PubMed DOI
  11. Rana,D., Kalamuddin,M., Sundriyal,S., Jaiswal,V., Sharma,G., Das Sarma,K., Sijwali,P.S., Mohmmed,A., Malhotra,P. and Mahindroo,N.
    Identification of antimalarial leads with dual falcipain-2 and falcipain-3 inhibitory activity
    Bioorg Med Chem115155-115155. PubMed  Europe PubMed DOI  I
  12. Stoye,A., Juillard,A., Tang,A.H., Legac,J., Gut,J., White,K.L., Charman,S.A., Rosenthal,P.J., Grau,G.E.R., Hunt,N.H. and Payne,R.J.
    Falcipain inhibitors based on the natural product gallinamide A are potent in vitro and in vivo antimalarials
    J Med Chem62, 5562-5578. PubMed  Europe PubMed DOI  I
  13. 2018
  14. Bekono,B.D., Ntie-Kang,F., Owono Owono,L.C. and Megnassan,E.
    Targeting cysteine proteases from Plasmodium falciparum: a general overview, rational drug design and computational approaches for drug discovery
    Curr Drug Targets19, 501-526. PubMed  Europe PubMed DOI  I
  15. Saddala,M.S. and Adi,P.J.
    Discovery of small molecules through pharmacophore modeling, docking and molecular dynamics simulation against Plasmodium vivax vivapain-3 (VP-3)
    Heliyon4, e00612-e00612. PubMed  Europe PubMed DOI  I
  16. 2016
  17. Musyoka,T.M., Kanzi,A.M., Lobb,K.A. and Tastan Bishop,O.
    Structure based docking and molecular dynamic studies of plasmodial cysteine proteases against a South African natural compound and its analogs
    Sci Rep6, 23690-23690. PubMed  Europe PubMed DOI  I
  18. Musyoka,T.M., Kanzi,A.M., Lobb,K.A. and Tastan Bishop,O.
    Analysis of non-peptidic compounds as potential malarial inhibitors against plasmodial cysteine proteases via integrated virtual screening workflow
    J Biomol Struct Dyn34, 2084-2101. PubMed  Europe PubMed DOI  I
  19. Ponsuwanna,P., Kochakarn,T., Bunditvorapoom,D., Kumpornsin,K., Otto,T.D., Ridenour,C., Chotivanich,K., Wilairat,P., White,N.J., Miotto,O. and Chookajorn,T.
    Comparative genome-wide analysis and evolutionary history of haemoglobin-processing and haem detoxification enzymes in malarial parasites
    Malar J15, 51-51. PubMed  Europe PubMed DOI
  20. Poongavanam,V. and Kongsted,J.
    Binding affinity models for falcipain inhibition based on the linear interaction energy method
    J Mol Graph Model70, 236-245. PubMed  Europe PubMed DOI  I
  21. 2015
  22. Kolla,V.K., Prasad,R., Sayyad,Z., Atul, Shah,A.Y., Allanki,A.D., Navale,R., Singhal,N., Tanneru,N., Sudhakar,R., Venkatesan,V., Deshmukh,M.V. and Sijwali,P.S.
    Independent amino acid residues in the S2 pocket of falcipain-3 determine its specificity for P2 residues in substrates
    Mol Biochem Parasitol202, 11-22. PubMed  Europe PubMed DOI
  23. 2014
  24. Conroy,T., Guo,J.T., Elias,N., Cergol,K.M., Gut,J., Legac,J., Khatoon,L., Liu,Y., McGowan,S., Rosenthal,P.J., Hunt,N.H. and Payne,R.J.
    Synthesis of gallinamide A analogues as potent falcipain inhibitors and antimalarials
    J Med Chem57, 10557-10563. PubMed  Europe PubMed DOI  I
  25. Weldon,D.J., Shah,F., Chittiboyina,A.G., Sheri,A., Chada,R.R., Gut,J., Rosenthal,P.J., Shivakumar,D., Sherman,W., Desai,P., Jung,J.C. and Avery,M.A.
    Synthesis, biological evaluation, hydration site thermodynamics, and chemical reactivity analysis of alpha-keto substituted peptidomimetics for the inhibition of Plasmodium falciparum
    Bioorg Med Chem Lett24, 1274-1279. PubMed  Europe PubMed DOI  I
  26. 2013
  27. Cotrin,S.S., Gouvea,I.E., Melo,P.M., Bagnaresi,P., Assis,D.M., Araujo,M.S., Juliano,M.A., Gazarini,M.L., Rosenthal,P.J., Juliano,L. and Carmona,A.K.
    Substrate specificity studies of the cysteine peptidases falcipain-2 and falcipain-3 from Plasmodium falciparum and demonstration of their kininogenase activity
    Mol Biochem Parasitol187, 111-116. PubMed  Europe PubMed DOI  P
  28. Kesharwani,R.K., Singh,D.V. and Misra,K.
    Computation-based virtual screening for designing novel antimalarial drugs by targeting falcipain-III: A structure-based drug designing approach
    J Vector Borne Dis50, 93-102. PubMed  Europe PubMed  I
  29. Mane,U.R., Gupta,R.C., Nadkarni,S.S., Giridhar,R.R., Naik,P.P. and Yadav,M.R.
    Falcipain inhibitors as potential therapeutics for resistant strains of malaria: a patent review
    Expert Opin Ther Pat23, 165-187. PubMed  Europe PubMed DOI  V  I
  30. Rathi,B., Singh,A.K., Kishan,R., Singh,N., Latha,N., Srinivasan,S., Pandey,K.C., Tiwari,H.K. and Singh,B.K.
    Functionalized hydroxyethylamine based peptide nanostructures as potential inhibitors of falcipain-3, an essential proteases of Plasmodium falciparum
    Bioorg Med Chem21, 5503-5509. PubMed  Europe PubMed DOI  I
  31. Wang,J., Li,F., Li,Y., Yang,Y., Zhang,S. and Yang,L.
    Structural features of falcipain-3 inhibitors: an in silico study
    Mol Biosyst9, 2296-2310. PubMed  Europe PubMed DOI  I
  32. 2012
  33. Bagnaresi,P., de Barros,N.M., Assis,D.M., Melo,P.M., Fonseca,R.G., Juliano,M.A., Pesquero,J.B., Juliano,L., Rosenthal,P.J., Carmona,A.K. and Gazarini,M.L.
    Intracellular proteolysis of kininogen by malaria parasites promotes release of active kinins
    Malar J11, 156-156. PubMed  Europe PubMed DOI
  34. Chintakrindi,A.S., Shaikh,M.S. and Coutinho,E.C.
    De novo design of 7-aminocoumarin derivatives as novel falcipain-3 inhibitors
    J Mol Model18, 1481-1493. PubMed  Europe PubMed DOI  I
  35. Marco,M. and Coteron,J.M.
    Falcipain inhibition as a promising antimalarial target
    Curr Top Med Chem12, 408-444. PubMed  Europe PubMed DOI  I
  36. Pandey,K.C. and Dixit,R.
    Structure-function of falcipains: malarial cysteine proteases
    J Trop Med2012, 345195-345195. PubMed  Europe PubMed DOI  I
  37. Prasad,R., Atul, Soni,A., Puri,S.K. and Sijwali,P.S.
    Expression, characterization, and cellular localization of knowpains, papain-like cysteine proteases of the Plasmodium knowlesi malaria parasite
    PLoS ONE7, e51619-e51619. PubMed  Europe PubMed DOI
  38. Shah,F., Gut,J., Legac,J., Shivakumar,D., Sherman,W., Rosenthal,P.J. and Avery,M.A.
    Computer-aided drug design of falcipain inhibitors: virtual screening, structure-activity relationships, hydration site thermodynamics, and reactivity analysis
    J Chem Inf Model52, 696-710. PubMed  Europe PubMed DOI  I
  39. Sundararaj,S., Singh,D., Saxena,A.K., Vashisht,K., Sijwali,P.S., Dixit,R. and Pandey,K.C.
    The ionic and hydrophobic interactions are required for the auto activation of cysteine proteases of Plasmodium falciparum
    PLoS ONE7, e47227-e47227. PubMed  Europe PubMed DOI
  40. 2011
  41. Pandey,K.C.
    Centenary celebrations article: Cysteine proteases of human malaria parasites
    J Parasitic Dis35, 94-103. PubMed  Europe PubMed DOI
  42. Potshangbam,A.M., Tanneeru,K., Reddy,B.M. and Guruprasad,L.
    3D-QSAR and molecular docking studies of 2-pyrimidinecarbonitrile derivatives as inhibitors against falcipain-3
    Bioorg Med Chem Lett21, 7219-7223. PubMed  Europe PubMed DOI  I
  43. Rosenthal,P.J.
    Falcipains and other cysteine proteases of malaria parasites
    Adv Exp Med Biol712, 30-48. PubMed  Europe PubMed DOI
  44. Shah,F., Mukherjee,P., Gut,J., Legac,J., Rosenthal,P.J., Tekwani,B.L. and Avery,M.A.
    Identification of novel malarial cysteine protease inhibitors using structure-based virtual screening of a focused cysteine protease inhibitor library
    J Chem Inf Model51, 852-864. PubMed  Europe PubMed DOI  I
  45. 2010
  46. Breuning,A., Degel,B., Schulz,F., Buchold,C., Stempka,M., Machon,U., Heppner,S., Gelhaus,C., Leippe,M., Leyh,M., Kisker,C., Rath,J., Stich,A., Gut,J., Rosenthal,P.J., Schmuck,C. and Schirmeister,T.
    Michael acceptor based antiplasmodial and antitrypanosomal cysteine protease inhibitors with unusual amino acids
    J Med Chem53, 1951-1963. PubMed  Europe PubMed DOI  I
  47. Coteron,J.M., Catterick,D., Castro,J., Chaparro,M.J., Diaz,B., Fernandez,E., Ferrer,S., Gamo,F.J., Gordo,M., Gut,J., de Las Heras,L., Legac,J., Marco,M., Miguel,J., Munoz,V., Porras,E., de la Rosa,J.C., Ruiz,J.R., Sandoval,E., Ventosa,P., Rosenthal,P.J. and Fiandor,J.M.
    Falcipain inhibitors: optimization studies of the 2-pyrimidinecarbonitrile lead series
    J Med Chem53, 6129-6152. PubMed  Europe PubMed DOI  I
  48. Gibbons,P., Verissimo,E., Araujo,N.C., Barton,V., Nixon,G.L., Amewu,R.K., Chadwick,J., Stocks,P.A., Biagini,G.A., Srivastava,A., Rosenthal,P.J., Gut,J., Guedes,R.C., Moreira,R., Sharma,R., Berry,N., Cristiano,M.L., Shone,A.E., Ward,S.A. and O'Neill,P.M.
    Endoperoxide carbonyl falcipain 2/3 inhibitor hybrids: toward combination chemotherapy of malaria through a single chemical entity
    J Med Chem53, 8202-8206. PubMed  Europe PubMed DOI  I
  49. Loser,R., Gut,J., Rosenthal,P.J., Frizler,M., Gutschow,M. and Andrews,K.T.
    Antimalarial activity of azadipeptide nitriles
    Bioorg Med Chem Lett20, 252-255. PubMed  Europe PubMed DOI  I
  50. 2009
  51. Dude,M.A., Kaeppler,U., Herb,M., Schiller,M., Schulz,F., Vedder,B., Heppner,S., Pradel,G., Gut,J., Rosenthal,P.J., Schirmeister,T., Leippe,M. and Gelhaus,C.
    Synthesis and evaluation of non-peptidic cysteine protease inhibitors of P. falciparum derived from etacrynic acid
    Molecules14, 19-35. PubMed  Europe PubMed DOI  I
  52. Kerr,I.D., Lee,J.H., Pandey,K.C., Harrison,A., Sajid,M., Rosenthal,P.J. and Brinen,L.S.
    Structures of falcipain-2 and falcipain-3 bound to small molecule inhibitors: implications for substrate specificity
    J Med Chem52, 852-857. PubMed  Europe PubMed DOI  S  I
  53. Kerr,I.D., Lee,J.H., Farady,C.J., Marion,R., Rickert,M., Sajid,M., Pandey,K.C., Caffrey,C.R., Legac,J., Hansell,E., McKerrow,J.H., Craik,C.S., Rosenthal,P.J. and Brinen,L.S.
    Vinyl sulfones as antiparasitic agents and a structural basis for drug design
    J Biol Chem284, 25697-25703. PubMed  Europe PubMed DOI  S  I
  54. Subramanian,S., Hardt,M., Choe,Y., Niles,R.K., Johansen,E.B., Legac,J., Gut,J., Kerr,I.D., Craik,C.S. and Rosenthal,P.J.
    Hemoglobin cleavage site-specificity of the Plasmodium falciparum cysteine proteases falcipain-2 and falcipain-3
    PLoS ONE4, e5156-e5156. PubMed  Europe PubMed DOI  P
  55. 2008
  56. Drew,M.E., Banerjee,R., Uffman,E.W., Gilbertson,S., Rosenthal,P.J. and Goldberg,D.E.
    Plasmodium food vacuole plasmepsins are activated by falcipains
    J Biol Chem283, 12870-12876. PubMed  Europe PubMed DOI
  57. Verissimo,E., Berry,N., Gibbons,P., Cristiano,M.L., Rosenthal,P.J., Gut,J., Ward,S.A. and O'Neill,P.M.
    Design and synthesis of novel 2-pyridone peptidomimetic falcipain 2/3 inhibitors
    Bioorg Med Chem Lett18, 4210-4214. PubMed  Europe PubMed DOI  I
  58. 2007
  59. Schulz,F., Gelhaus,C., Degel,B., Vicik,R., Heppner,S., Breuning,A., Leippe,M., Gut,J., Rosenthal,P.J. and Schirmeister,T.
    Screening of protease inhibitors as antiplasmodial agents. Part I: aziridines and epoxides
    ChemMedChem2, 1214-1224. PubMed  Europe PubMed DOI  I
  60. Subramanian,S., Sijwali,P.S. and Rosenthal,P.J.
    Falcipain cysteine proteases require bipartite motifs for trafficking to the Plasmodium falciparum food vacuole
    J Biol Chem282, 24961-24969. PubMed  Europe PubMed DOI
  61. 2006
  62. [YEAR:15-6-2006]Ramjee,M.K., Flinn,N.S., Pemberton,T.P., Quibell,M., Wang,Y. and Watts,J.P.
    Substrate mapping and inhibitor profiling of falcipain-2, falcipain-3 and berghepain-2: implications for peptidase anti-malarial drug discovery
    Biochem J399, 47-57. PubMed  Europe PubMed DOI  P
  63. [YEAR:20-7-2006]Sijwali,P.S., Koo,J., Singh,N. and Rosenthal,P.J.
    Gene disruptions demonstrate independent roles for the four falcipain cysteine proteases of Plasmodium falciparum
    Mol Biochem Parasitol150, 96-106. PubMed  Europe PubMed DOI  K
  64. 2005
  65. Dahl,E.L. and Rosenthal,P.J.
    Biosynthesis, localization, and processing of falcipain cysteine proteases of Plasmodium falciparum
    Mol Biochem Parasitol139, 205-212. PubMed  Europe PubMed DOI
  66. Florent,I., Lecaille,F., Montagne,J.J., Gauthier,F., Schrevel,J. and Lalmanach,G.
    Labelling of four distinct trophozoite falcipains of Plasmodium falciparum by a cystatin-derived probe
    Biol Chem386, 401-406. PubMed  Europe PubMed DOI
  67. 2004
  68. Desai,P.V., Patny,A., Sabnis,Y., Tekwani,B., Gut,J., Rosenthal,P., Srivastava,A. and Avery,M.
    Identification of novel parasitic cysteine protease inhibitors using virtual screening. 1. The ChemBridge database
    J Med Chem47, 6609-6615. PubMed  Europe PubMed DOI  I
  69. Desai,P.V. and Avery,M.A.
    Structural characterization of vivapain-2 and vivapain-3, cysteine proteases from Plasmodium vivax: comparative protein modeling and docking studies
    J Biomol Struct Dyn21, 781-790. PubMed  Europe PubMed DOI
  70. [YEAR:20-11-2004]Na,B.K., Shenai,B.R., Sijwali,P.S., Choe,Y., Pandey,K.C., Singh,A., Craik,C.S. and Rosenthal,P.J.
    Identification and biochemical characterization of vivapains, cysteine proteases of the malaria parasite Plasmodium vivax
    Biochem J378, 529-538. PubMed  Europe PubMed DOI
  71. [YEAR:15-9-2004]Na,B.K., Kim,T.S., Rosenthal,P.J., Lee,J.K. and Kong,Y.
    Evaluation of cysteine proteases of Plasmodium vivax as antimalarial drug targets: sequence analysis and sensitivity to cysteine protease inhibitors
    Parasitol Res94, 312-317. PubMed  Europe PubMed DOI  I
  72. Rosenthal,P.J.
    Falcipains
    [ISSN:0-12-079610-4]2, 1157-1160.  V
  73. 2003
  74. Lee,B.J., Singh,A., Chiang,P., Kemp,S.J., Goldman,E.A., Weinhouse,M.I., Vlasuk,G.P. and Rosenthal,P.J.
    Antimalarial activities of novel synthetic cysteine protease inhibitors
    Antimicrobial Agents Chemother47, 3810-3814. PubMed  Europe PubMed DOI  I
  75. Shenai,B.R., Lee,B.J., Alvarez-Hernandez,A., Chong,P.Y., Emal,C.D., Neitz,R.J., Roush,W.R. and Rosenthal,P.J.
    Structure-activity relationships for inhibition of cysteine protease activity and development of Plasmodium falciparum by peptidyl vinyl sulfones
    Antimicrobial Agents Chemother47, 154-160. PubMed  Europe PubMed DOI  I
  76. 2001
  77. [YEAR:1-12-2001]Sijwali,P.S., Shenai,B.R., Gut,J., Singh,A. and Rosenthal,P.J.
    Expression and characterization of the Plasmodium falciparum haemoglobinase falcipain-3
    Biochem J360, 481-489. PubMed  Europe PubMed DOI
  78. 1987
  79. [YEAR:1-9-1987]Rosenthal,P.J., Kim,K., McKerrow,J.H. and Leech,J.H.
    Identification of three stage-specific proteinases of Plasmodium falciparum
    J Exp Med166, 816-821. PubMed  Europe PubMed