Literature for peptidase C01.075: cruzipain

Summary Alignment Sequences Sequence features Distribution Structure Literature Substrates Inhibitors Pharma

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

    2025
  1. Cerutti,J.P., Diniz,L.A., Correa Santos,V., Vilchez Larrea,S.C., Alonso,G.D., Ferreira,R.S., Quevedo,M.A. and Dehaen,W.
    Discovery of a Potent Triazole-Based Reversible Targeted Covalent Inhibitor of Cruzipain
    ACS Med Chem Lett (2025) 16, 72-79. PubMed  Europe PubMed DOI  PMC  EPMC  I
  2. Cerutti,J.P., Estrada Canepa,J.I., Diniz,L.A., Vilchez Larrea,S.C., Santos,V.C., Alonso,G.D., Ferreira,R.S., Dehaen,W. and Quevedo,M.A.
    Structure-Based Discovery of Non-Covalent Triazole-Based Cruzipain Inhibitors with Improved Bioactivity Translation
    J Chem Inf Model (2025) PubMed  Europe PubMed DOI  I
  3. Sheu-Idrees,R., Marques,G.V.L., Santana,P.A.L., Diniz,L.A., Resende,D.M., Odoma,S., Olorunshola,O., Ferreira,R.S., Murta,S.M.F., Maltarollo,V.G. and de Oliveira,R.B.
    Investigation of the activity of 4-aminoquinolines as cysteine protease inhibitors with application in the treatment of Chagas disease
    Mem Inst Oswaldo Cruz (2025) 120, e240161-e240161. PubMed  Europe PubMed DOI  PMC  EPMC  I
  4. 2023
  5. Santos,V.C., Leite,P.G., Santos,L.H., Pascutti,P.G., Kolb,P., Machado,F.S. and Ferreira,R.S.
    Structure-based discovery of novel cruzain inhibitors with distinct trypanocidal activity profiles
    Eur J Med Chem (2023) 257, 115498-115498. PubMed  Europe PubMed DOI  I
  6. 2022
  7. de Oliveira,A.S., Valli,M., Ferreira,L.L., Souza,J.M., Krogh,R., Meier,L., Abreu,H.R., Voltolini,B.G., Llanes,L.C., Nunes,R.J., Braga,A.L. and Andricopulo,A.D.
    Novel trypanocidal thiophen-chalcone cruzain inhibitors: structure- and ligand-based studies
    Future Med Chem (2022) 14, 795-808. PubMed  Europe PubMed DOI  I
  8. 2021
  9. Barbosa da Silva,E., Rocha,D.A., Fortes,I.S., Yang,W., Monti,L., Siqueira-Neto,J.L., Caffrey,C.R., McKerrow,J., Andrade,S.F. and Ferreira,R.S.
    Structure-Based Optimization of Quinazolines as Cruzain and TbrCATL Inhibitors
    J Med Chem (2021) 64, 13054-13071. PubMed  Europe PubMed DOI  I
  10. 2020
  11. Arafet,K., Gonzalez,F.V. and Moliner,V.
    Quantum mechanics/molecular mechanics studies of the mechanism of cysteine proteases inhibition by dipeptidyl nitroalkenes
    Chemistry (2020) 26, 2002-2012. PubMed  Europe PubMed DOI  I
  12. Bonatto,V., Batista,P.H.J., Cianni,L., De Vita,D., Silva,D.G., Cedron,R., Tezuka,D.Y., de Albuquerque,S., Moraes,C.B., Franco,C.H., Lameira,J., Leitao,A. and Montanari,C.A.
    On the intrinsic reactivity of highly potent trypanocidal cruzain inhibitors
    RSC Med Chem (2020) 11, 1275-1284. PubMed  Europe PubMed DOI  PMC  EPMC  I
  13. Chenna,B.C., Li,L., Mellott,D.M., Zhai,X., Siqueira-Neto,J.L., Calvet Alvarez,C., Bernatchez,J.A., Desormeaux,E., Alvarez Hernandez,E., Gomez,J., McKerrow,J.H., Cruz-Reyes,J. and Meek,T.D.
    Peptidomimetic vinyl heterocyclic inhibitors of cruzain effect anti-trypanosomal activity
    J Med Chem (2020) 63, 3298-3316. PubMed  Europe PubMed DOI  I
  14. Cianni,L., Lemke,C., Gilberg,E., Feldmann,C., Rosini,F., Rocho,F.D.R., Ribeiro,J.F.R., Tezuka,D.Y., Lopes,C.D., de Albuquerque,S., Bajorath,J., Laufer,S., Leitao,A., Gutschow,M. and Montanari,C.A.
    Mapping the S1 and S1' subsites of cysteine proteases with new dipeptidyl nitrile inhibitors as trypanocidal agents
    PLoS Negl Trop Dis (2020) 14, e0007755-e0007755. PubMed  Europe PubMed DOI  I
  15. 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 Chem (2020) 101, 104039-104039. PubMed  Europe PubMed DOI  I
  16. de Souza,M.L., de Oliveira Rezende Junior,C., Ferreira,R.S., Espinoza Chavez,R.M., Ferreira,L.L.G., Slafer,B.W., Magalhaes,L.G., Krogh,R., Oliva,G., Cruz,F.C., Dias,L.C. and Andricopulo,A.D.
    Discovery of potent, reversible and competitive cruzain inhibitors with trypanocidal activity: a structure-based drug design approach
    J Chem Inf Model (2020) 60, 1028-1041. PubMed  Europe PubMed DOI  I
  17. Ribeiro,J.F.R., Cianni,L., Li,C., Warwick,T.G., De Vita,D., Rosini,F., Dos Reis Rocho,F., Martins,F.C.P., Kenny,P.W., Lameira,J., Leitao,A., Emsley,J. and Montanari,C.A.
    Crystal structure of Leishmania mexicana cysteine protease B in complex with a high-affinity azadipeptide nitrile inhibitor
    Bioorg Med Chem (2020) 28, 115743-115743. PubMed  Europe PubMed DOI  I
  18. Silva,J.R.A., Cianni,L., Araujo,D., Batista,P.H.J., De Vita,D., Rosini,F., Leitao,A., Lameira,J. and Montanari,C.A.
    Assessment of the cruzain cysteine protease reversible and irreversible covalent inhibition mechanism
    J Chem Inf Model (2020) 60, 1666-1677. PubMed  Europe PubMed DOI  I
  19. 2019
  20. Bhowmick,S., Chorge,R.D., Jangam,C.S., Bharatrao,L.D., Patil,P.C., Chikhale,R.V. and Islam,M.A.
    Identification of potential cruzain inhibitors using de novo design, molecular docking and dynamics simulations studies
    J Biomol Struct Dyn (2019) , 1-11. PubMed  Europe PubMed DOI  I
  21. Boudreau,P.D., Miller,B.W., McCall,L.I., Almaliti,J., Reher,R., Hirata,K., Le,T., Siqueira-Neto,J.L., Hook,V. and Gerwick,W.H.
    Design of gallinamide A analogs as potent inhibitors of the cysteine proteases human cathepsin L and Trypanosoma cruzi cruzain
    J Med Chem (2019) 62, 9026-9044. PubMed  Europe PubMed DOI  I
  22. Cianni,L., Feldmann,C.W., Gilberg,E., Gutschow,M., Juliano,L., Leitao,A., Bajorath,J. and Montanari,C.A.
    Can cysteine protease cross-class inhibitors achieve selectivity?
    J Med Chem (2019) 62, 10497-10525. PubMed  Europe PubMed DOI  I
  23. Fabian,L., Martini,M.F., Sarduy,E.S., Estrin,D.A. and Moglioni,A.G.
    Evaluation of quinoxaline compounds as ligands of a site adjacent to S2 (AS2) of cruzain
    Bioorg Med Chem Lett (2019) 29, 2197-2202. PubMed  Europe PubMed DOI  I
  24. Ferreira,R.A.A., Pauli,I., Sampaio,T.S., de Souza,M.L., Ferreira,L.L.G., Magalhaes,L.G., Rezende CO Jr, Ferreira,R.S., Krogh,R., Dias,L.C. and Andricopulo,A.D.
    Structure-based and molecular modeling studies for the discovery of cyclic imides as reversible cruzain inhibitors with potent anti-Trypanosoma cruzi activity
    Front Chem (2019) 7, 798-798. PubMed  Europe PubMed DOI  PMC  EPMC  I
  25. Gomes,J.C., Cianni,L., Ribeiro,J., Dos Reis Rocho,F., da Costa Martins Silva,S., Batista,P.H.J., Moraes,C.B., Franco,C.H., Freitas-Junior,L.H.G., Kenny,P.W., Leitao,A., Burtoloso,A.C.B., De Vita,D. and Montanari,C.A.
    Synthesis and structure-activity relationship of nitrile-based cruzain inhibitors incorporating a trifluoroethylamine-based P2 amide replacement
    Bioorg Med Chem (2019) , 115083-115083. PubMed  Europe PubMed DOI  I
  26. Herrera-Mayorga,V., Lara-Ramirez,E.E., Chacon-Vargas,K.F., Aguirre-Alvarado,C., Rodriguez-Paez,L., Alcantara-Farfan,V., Cordero-Martinez,J., Nogueda-Torres,B., Reyes-Espinosa,F., Bocanegra-Garcia,V. and Rivera,G.
    Structure-based virtual screening and in vitro evaluation of new Trypanosoma cruzi cruzain inhibitors
    Int J Mol Sci (2019) 20 PubMed  Europe PubMed DOI  I
  27. Luchi,A.M., Villafane,R.N., Gomez Chavez,J.L., Bogado,M.L., Angelina,E.L. and Peruchena,N.M.
    Combining charge density analysis with machine learning tools to investigate the cruzain inhibition mechanism
    ACS Omega (2019) 4, 19582-19594. PubMed  Europe PubMed DOI  PMC  EPMC  I
  28. Monteiro,M.E., Lechuga,G., Lara,L.S., Souto,B.A., Vigano,M.G., Bourguignon,S.C., Calvet,C.M., Oliveira,F.O.R., Jr., Alves,C.R., Souza-Silva,F., Santos,M.S. and Pereira,M.C.S.
    Synthesis, structure-activity relationship and trypanocidal activity of pyrazole-imidazoline and new pyrazole-tetrahydropyrimidine hybrids as promising chemotherapeutic agents for Chagas disease
    Eur J Med Chem (2019) 182, 111610-111610. PubMed  Europe PubMed DOI  I
  29. Santos,L.H., Waldner,B.J., Fuchs,J.E., Pereira,G.A.N., Liedl,K.R., Caffarena,E.R. and Ferreira,R.S.
    Understanding structure-activity relationships for trypanosomal cysteine protease inhibitors by simulations and free energy calculations
    J Chem Inf Model (2019) 59, 137-148. PubMed  Europe PubMed DOI  I
  30. Sartori,G.R., Leitao,A., Montanari,C.A. and Laughton,C.A.
    Ligand-induced conformational selection predicts the selectivity of cysteine protease inhibitors
    PLoS ONE (2019) 14, e0222055-e0222055. PubMed  Europe PubMed DOI  I
  31. Vieira,R.P., Santos,V.C. and Ferreira,R.S.
    Structure-based approaches targeting parasite cysteine proteases
    Curr Med Chem (2019) 26, 4435-4453. PubMed  Europe PubMed DOI  I
  32. 2018
  33. Cianni,L., Sartori,G., Rosini,F., De Vita,D., Pires,G., Lopes,B.R., Leitao,A., Burtoloso,A.C.B. and Montanari,C.A.
    Leveraging the cruzain S3 subsite to increase affinity for reversible covalent inhibitors
    Bioorg Chem (2018) 79, 285-292. PubMed  Europe PubMed DOI  I
  34. da Silva-Junior,E.F., Barcellos Franca,P.H., Ribeiro,F.F., Bezerra Mendonca-Junior,F.J., Scotti,L., Scotti,M.T., de Aquino,T.M. and de Araujo-Junior,J.X.
    Molecular docking studies applied to a dataset of cruzain inhibitors
    Curr Comput Aided Drug Des (2018) 14, 68-78. PubMed  Europe PubMed DOI  I
  35. Dos Santos,A.M., Cianni,L., De Vita,D., Rosini,F., Leitao,A., Laughton,C.A., Lameira,J. and Montanari,C.A.
    Experimental study and computational modelling of cruzain cysteine protease inhibition by dipeptidyl nitriles
    Phys Chem Chem Phys (2018) 20, 24317-24328. PubMed  Europe PubMed DOI  I
  36. Giroud,M., Dietzel,U., Anselm,L., Banner,D., Kuglstatter,A., Benz,J., Blanc,J.B., Gaufreteau,D., Liu,H., Lin,X., Stich,A., Kuhn,B., Schuler,F., Kaiser,M., Brun,R., Schirmeister,T., Kisker,C., Diederich,F. and Haap,W.
    Repurposing a library of human cathepsin L ligands: identification of macrocyclic lactams as potent rhodesain and Trypanosoma brucei inhibitors
    J Med Chem (2018) 61, 3350-3369. PubMed  Europe PubMed DOI  S  I
  37. Martins,L.C., Torres,P.H.M., de Oliveira,R.B., Pascutti,P.G., Cino,E.A. and Ferreira,R.S.
    Investigation of the binding mode of a novel cruzain inhibitor by docking, molecular dynamics, ab initio and MM/PBSA calculations
    J Comput Aided Mol Des (2018) 32, 591-605. PubMed  Europe PubMed DOI  I
  38. Rocha,D.A., Silva,E.B., Fortes,I.S., Lopes,M.S., Ferreira,R.S. and Andrade,S.F.
    Synthesis and structure-activity relationship studies of cruzain and rhodesain inhibitors
    Eur J Med Chem (2018) 157, 1426-1459. PubMed  Europe PubMed DOI  I
  39. Royo,S., Schirmeister,T., Kaiser,M., Jung,S., Rodriguez,S., Bautista,J.M. and Gonzalez,F.V.
    Antiprotozoal and cysteine proteases inhibitory activity of dipeptidyl enoates
    Bioorg Med Chem (2018) 26, 4624-4634. PubMed  Europe PubMed DOI  I
  40. Salas-Sarduy,E., Landaburu,L.U., Karpiak,J., Madauss,K.P., Cazzulo,J.J., Aguero,F. and Alvarez,V.E.
    Author Correction: Novel scaffolds for inhibition of cruzipain identified from high-throughput screening of anti-kinetoplastid chemical boxes
    Sci Rep (2018) 8, 8743-8743. PubMed  Europe PubMed DOI  PMC  EPMC  I
  41. Saraiva,A.P.B., Miranda,R.M., Valente,R.P.P., Araujo,J.O., Souza,R.N.B., Costa,C.H.S., Oliveira,A.R.S., Almeida,M.O., Figueiredo,A.F., Ferreira,J.E.V., Alves,C.N. and Honorio,K.M.
    Molecular description of alpha-keto-based inhibitors of cruzain with activity against Chagas disease combining 3D-QSAR studies and molecular dynamics
    Chem Biol Drug Des (2018) 92, 1475-1487. PubMed  Europe PubMed DOI  I
  42. 2017
  43. Braga,S.F., Martins,L.C., da Silva,E.B., Sales Junior,P.A., Murta,S.M., Romanha,A.J., Soh,W.T., Brandstetter,H., Ferreira,R.S. and de Oliveira,R.B.
    Synthesis and biological evaluation of potential inhibitors of the cysteine proteases cruzain and rhodesain designed by molecular simplification
    Bioorg Med Chem (2017) 25, 1889-1900. PubMed  Europe PubMed DOI  I
  44. Burtoloso,A.C., de Albuquerque,S., Furber,M., Gomes,J.C., Goncalez,C., Kenny,P.W., Leitao,A., Montanari,C.A., Quilles JC Junior, Ribeiro,J.F. and Rocha,J.R.
    Anti-trypanosomal activity of non-peptidic nitrile-based cysteine protease inhibitors
    PLoS Negl Trop Dis (2017) 11, e0005343-e0005343. PubMed  Europe PubMed DOI  I
  45. de Souza,A.S., de Oliveira,M.T. and Andricopulo,A.D.
    Development of a pharmacophore for cruzain using oxadiazoles as virtual molecular probes: quantitative structure-activity relationship studies
    J Comput Aided Mol Des (2017) 31, 801-816. PubMed  Europe PubMed DOI  I
  46. Palos,I., Lara-Ramirez,E.E., Lopez-Cedillo,J.C., Garcia-Perez,C., Kashif,M., Bocanegra-Garcia,V., Nogueda-Torres,B. and Rivera,G.
    Repositioning FDA drugs as potential cruzain inhibitors from Trypanosoma cruzi: virtual screening, In vitro and in vivo studies
    Molecules (2017) 22 PubMed  Europe PubMed DOI  I
  47. Pauli,I., Ferreira,L.G., de Souza,M.L., Oliva,G., Ferreira,R.S., Dessoy,M.A., Slafer,B.W., Dias,L.C. and Andricopulo,A.D.
    Molecular modeling and structure-activity relationships for a series of benzimidazole derivatives as cruzain inhibitors
    Future Med Chem (2017) 9, 641-657. PubMed  Europe PubMed DOI  I
  48. Salas-Sarduy,E., Landaburu,L.U., Karpiak,J.X., Madauss,K.P., Cazzulo,J.J., Aguero,F. and Alvarez,V.E.
    Novel scaffolds for inhibition of cruzipain identified from high-throughput screening of anti-kinetoplastid chemical boxes
    Sci Rep (2017) 7, 12073-12073. PubMed  Europe PubMed DOI  I
  49. Silva,D.G., Ribeiro,J.F.R., De Vita,D., Cianni,L., Franco,C.H., Freitas-Junior,L.H., Moraes,C.B., Rocha,J.R., Burtoloso,A.C.B., Kenny,P.W., Leitao,A. and Montanari,C.A.
    A comparative study of warheads for design of cysteine protease inhibitors
    Bioorg Med Chem Lett (2017) 27, 5031-5035. PubMed  Europe PubMed DOI  I
  50. Silva,D.G., Rocha,J.R., Sartori,G.R. and Montanari,C.A.
    Highly predictive hologram QSAR models of nitrile-containing cruzain inhibitors
    J Biomol Struct Dyn (2017) 35, 3232-3249. PubMed  Europe PubMed DOI  I
  51. 2016
  52. de Moraes Gomes,P.A., de Oliveira Barbosa,M., Farias Santiago,E., de Oliveira Cardoso,M.V., Capistrano Costa,N.T., Hernandes,M.Z., Moreira,D.R., Da Silva,A.C., Dos Santos,T.A., Pereira,V.R., Brayner Dos Santosd,F.A., do Nascimento Pereira,G.A., Ferreira,R.S. and Leite,A.C.
    New 1,3-thiazole derivatives and their biological and ultrastructural effects on Trypanosoma cruzi
    Eur J Med Chem (2016) 121, 387-398. PubMed  Europe PubMed DOI  I
  53. Jefferson,T., McShan,D., Warfield,J. and Ogungbe,I.V.
    Screening and identification of inhibitors of Trypanosoma brucei cathepsin L with antitrypanosomal activity
    Chem Biol Drug Des (2016) 87, 154-158. PubMed  Europe PubMed DOI  I
  54. Latorre,A., Schirmeister,T., Kesselring,J., Jung,S., Johe,P., Hellmich,U.A., Heilos,A., Engels,B., Krauth-Siegel,R.L., Dirdjaja,N., Bou-Iserte,L., Rodriguez,S. and Gonzalez,F.V.
    Dipeptidyl nitroalkenes as potent reversible inhibitors of cysteine proteases rhodesain and cruzain
    ACS Med Chem Lett (2016) 7, 1073-1076. PubMed  Europe PubMed DOI  PMC  EPMC  I
  55. Sbaraglini,M.L., Bellera,C.L., Fraccaroli,L., Larocca,L., Carrillo,C., Talevi,A. and Alba Soto,C.D.
    Novel cruzipain inhibitors for the chemotherapy of chronic Chagas disease
    Int J Antimicrob Agents (2016) 48, 91-95. PubMed  Europe PubMed DOI  I
  56. Silva-Junior,E.F., Silva,E.P., Franca,P.H., Silva,J.P., Barreto,E.O., Silva,E.B., Ferreira,R.S., Gatto,C.C., Moreira,D.R., Siqueira-Neto,J.L., Mendonca-Junior,F.J., Lima,M.C., Bortoluzzi,J.H., Scotti,M.T., Scotti,L., Meneghetti,M.R., Aquino,T.M. and Araujo-Junior,J.X.
    Design, synthesis, molecular docking and biological evaluation of thiophen-2-iminothiazolidine derivatives for use against Trypanosoma cruzi
    Bioorg Med Chem (2016) 24, 4228-4240. PubMed  Europe PubMed DOI  I
  57. 2015
  58. Arafet,K., Ferrer,S. and Moliner,V.
    First quantum mechanics/molecular mechanics studies of the inhibition mechanism of cruzain by peptidyl halomethyl ketones
    Biochemistry (2015) 54, 3381-3391. PubMed  Europe PubMed DOI  I
  59. Avelar,L.A., Camilo,C.D., de Albuquerque,S., Fernandes,W.B., Goncalez,C., Kenny,P.W., Leitao,A., McKerrow,J.H., Montanari,C.A., Orozco,E.V., Ribeiro,J.F., Rocha,J.R., Rosini,F. and Saidel,M.E.
    Molecular design, synthesis and trypanocidal activity of dipeptidyl nitriles as cruzain inhibitors
    PLoS Negl Trop Dis (2015) 9, e0003916-e0003916. PubMed  Europe PubMed DOI  PMC  EPMC  I
  60. de Almeida,L., Alves,K.F., Maciel-Rezende,C.M., Jesus Lde,O., Pires,F.R., Junior,C.V., Izidoro,M.A., Judice,W.A., Dos Santos,M.H. and Marques,M.J.
    Benzophenone derivatives as cysteine protease inhibitors and biological activity against Leishmania(L.) amazonensis amastigotes
    Biomed Pharmacother (2015) 75, 93-99. PubMed  Europe PubMed DOI  I
  61. Espindola,J.W., Cardoso,M.V., Filho,G.B., Oliveira E Silva,D.A., Moreira,D.R., Bastos,T.M., Simone,C.A., Soares,M.B., Villela,F.S., Ferreira,R.S., Castro,M.C., Pereira,V.R., Murta,S.M., Sales Junior,P.A., Romanha,A.J. and Leite,A.C.
    Synthesis and structure-activity relationship study of a new series of antiparasitic aryloxyl thiosemicarbazones inhibiting Trypanosoma cruzi cruzain
    Eur J Med Chem (2015) 101, 818-835. PubMed  Europe PubMed DOI  I
  62. Ferrao,P.M., D'Avila-Levy,C.M., Araujo-Jorge,T.C., Degrave,W.M., Goncalves,A.S., Garzoni,L.R., Lima,A.P., Feige,J.J., Bailly,S., Mendonca-Lima,L. and Waghabi,M.C.
    Cruzipain activates latent TGF-beta from host cells during T. cruzi invasion
    PLoS ONE (2015) 10, e0124832- PubMed  Europe PubMed DOI  PMC  EPMC  I
  63. Fonseca,N.C., da Cruz,L.F., da Silva Villela,F., do Nascimento Pereira,G.A., de Siqueira-Neto,J.L., Kellar,D., Suzuki,B.M., Ray,D., de Souza,T.B., Alves,R.J., Junior,P.A., Romanha,A.J., Murta,S.M., McKerrow,J.H., Caffrey,C.R., de Oliveira,R.B. and Ferreira,R.S.
    Synthesis of a sugar-based thiosemicarbazone series and structure-activity relationship versus the parasite cysteine proteases rhodesain, cruzain, and Schistosoma mansoni cathepsin B1
    Antimicrob Agents Chemother (2015) 59, 2666-2677. PubMed  Europe PubMed DOI  I
  64. Martinez-Mayorga,K., Byler,K.G., Ramirez-Hernandez,A.I. and Terrazas-Alvares,D.E.
    Cruzain inhibitors: efforts made, current leads and a structural outlook of new hits
    Drug Discov Today (2015) 20, 890-898. PubMed  Europe PubMed DOI  I
  65. Neitz,R.J., Bryant,C., Chen,S., Gut,J., Hugo Caselli,E., Ponce,S., Chowdhury,S., Xu,H., Arkin,M.R., Ellman,J.A. and Renslo,A.R.
    Tetrafluorophenoxymethyl ketone cruzain inhibitors with improved pharmacokinetic properties as therapeutic leads for Chagas' disease
    Bioorg Med Chem Lett (2015) 25, 4834-4837. PubMed  Europe PubMed DOI  I
  66. 2014
  67. Ferreira,R.S., Dessoy,M.A., Pauli,I., Souza,M.L., Krogh,R., Sales,A.I., Oliva,G., Dias,L.C. and Andricopulo,A.D.
    Synthesis, biological evaluation, and structure-activity relationships of potent noncovalent and nonpeptidic cruzain inhibitors as anti-Trypanosoma cruzi agents
    J Med Chem (2014) 57, 2380-2392. PubMed  Europe PubMed DOI  I
  68. Ndao,M., Beaulieu,C., Black,W.C., Isabel,E., Vasquez-Camargo,F., Nath-Chowdhury,M., Masse,F., Mellon,C., Methot,N. and Nicoll-Griffith,D.A.
    Reversible cysteine protease inhibitors show promise for a Chagas disease cure
    Antimicrob Agents Chemother (2014) 58, 1167-1178. PubMed  Europe PubMed DOI  I
  69. 2013
  70. Assis,D.M., Gontijo,V.S., de Oliveira Pereira,I., Santos,J.A., Camps,I., Nagem,T.J., Ellena,J., Izidoro,M.A., Dos Santos Tersariol,I.L., de Barros,N.M., Doriguetto,A.C., Dos Santos,M.H. and Juliano,M.A.
    Inhibition of cysteine proteases by a natural biflavone: behavioral evaluation of fukugetin as papain and cruzain inhibitor
    J Enzyme Inhib Med Chem (2013) 28, 661-670. PubMed  Europe PubMed DOI  S  I
  71. Bellera,C.L., Balcazar,D.E., Alberca,L., Labriola,C.A., Talevi,A. and Carrillo,C.
    Application of computer-aided drug repurposing in the search of new cruzipain inhibitors: discovery of amiodarone and bromocriptine inhibitory effects
    J Chem Inf Model (2013) 53, 2402-2408. PubMed  Europe PubMed DOI  I
  72. Wiggers,H.J., Rocha,J.R., Fernandes,W.B., Sesti-Costa,R., Carneiro,Z.A., Cheleski,J., Da Silva,A.B., Juliano,L., Cezari,M.H., Silva,J.S., McKerrow,J.H. and Montanari,C.A.
    Non-peptidic cruzain inhibitors with trypanocidal activity discovered by virtual screening and in vitro assay
    PLoS Negl Trop Dis (2013) 7, e2370-e2370. PubMed  Europe PubMed DOI  PMC  EPMC  I
  73. 2012
  74. Lavrado,J., Mackey,Z., Hansell,E., McKerrow,J.H., Paulo,A. and Moreira,R.
    Antitrypanosomal and cysteine protease inhibitory activities of alkyldiamine cryptolepine derivatives
    Bioorg Med Chem Lett (2012) 22, 6256-6260. PubMed  Europe PubMed DOI  I
  75. Lee,G.M., Balouch,E., Goetz,D.H., Lazic,A., McKerrow,J.H. and Craik,C.S.
    Mapping inhibitor binding modes on an active cysteine protease via nuclear magnetic resonance spectroscopy
    Biochemistry (2012) 51, 10087-10098. PubMed  Europe PubMed DOI  E  S  I
  76. Lozano,N.B., Maltarollo,V.G., Weber,K.C., Honorio,K.M., Guido,R.V., Andricopulo,A.D. and Da Silva,A.B.
    Molecular features for antitrypanosomal activity of thiosemicarbazones revealed by OPS-PLS QSAR studies
    Med Chem (2012) 8, 1045-1056. PubMed  Europe PubMed  I
  77. Mendez-Lucio,O., Romo-Mancillas,A., Medina-Franco,J.L. and Castillo,R.
    Computational study on the inhibition mechanism of cruzain by nitrile-containing molecules
    J Mol Graph Model (2012) 35, 28-35. PubMed  Europe PubMed DOI  I
  78. Rogers,K.E., Keranen,H., Durrant,J.D., Ratnam,J., Doak,A., Arkin,M.R. and McCammon,J.A.
    Novel cruzain inhibitors for the treatment of Chagas' disease
    Chem Biol Drug Des (2012) 80, 398-405. PubMed  Europe PubMed DOI  I
  79. Yang,P.Y., Wang,M., Li,L., Wu,H., He,C.Y. and Yao,S.Q.
    Design, synthesis and biological evaluation of potent azadipeptide nitrile inhibitors and activity-based probes as promising anti-Trypanosoma brucei agents
    Chemistry (2012) 18, 6528-6541. PubMed  Europe PubMed DOI  I
  80. 2011
  81. Caputto,M.E., Fabian,L.E., Benitez,D., Merlino,A., Rios,N., Cerecetto,H., Moltrasio,G.Y., Moglioni,A.G., Gonzalez,M. and Finkielsztein,L.M.
    Thiosemicarbazones derived from 1-indanones as new anti-Trypanosoma cruzi agents
    Bioorg Med Chem (2011) 19, 6818-6826. PubMed  Europe PubMed DOI  I
  82. 2010
  83. Beaulieu,C., Isabel,E., Fortier,A., Masse,F., Mellon,C., Methot,N., Ndao,M., Nicoll-Griffith,D., Lee,D., Park,H. and Black,W.C.
    Identification of potent and reversible cruzipain inhibitors for the treatment of Chagas disease
    Bioorg Med Chem Lett (2010) 20, 7444-7449. PubMed  Europe PubMed DOI  I
  84. Brak,K., Kerr,I.D., Barrett,K.T., Fuchi,N., Debnath,M., Ang,K., Engel,J.C., McKerrow,J.H., Doyle,P.S., Brinen,L.S. and Ellman,J.A.
    Nonpeptidic tetrafluorophenoxymethyl ketone cruzain inhibitors as promising new leads for Chagas disease chemotherapy
    J Med Chem (2010) 53, 1763-1773. PubMed  Europe PubMed DOI  I
  85. Ferreira,R.S., Simeonov,A., Jadhav,A., Eidam,O., Mott,B.T., Keiser,M.J., McKerrow,J.H., Maloney,D.J., Irwin,J.J. and Shoichet,B.K.
    Complementarity between a docking and a high-throughput screen in discovering new cruzain inhibitors
    J Med Chem (2010) 53, 4891-4905. PubMed  Europe PubMed DOI  I
  86. Luci,D., Lea,W., Ferreira,R., Shoichet,B., Simeonov,A., Rodriguez,A., Jadhav,A. and Maloney,D.J.
    Reversible and non-covalent benzimidazole-based in vivo lead for Chagas disease
    [ISSN:NBK133417] (2010) PubMed  Europe PubMed  I
  87. Mott,B.T., Ferreira,R.S., Simeonov,A., Jadhav,A., Ang,K.K., Leister,W., Shen,M., Silveira,J.T., Doyle,P.S., Arkin,M.R., McKerrow,J.H., Inglese,J., Austin,C.P., Thomas,C.J., Shoichet,B.K. and Maloney,D.J.
    Identification and optimization of inhibitors of trypanosomal cysteine proteases: cruzain, rhodesain, and TbCatB
    J Med Chem (2010) 53, 52-60. PubMed  Europe PubMed DOI  S  I
  88. Rodrigues,G.C., Aguiar,A.P., da Silva Goncalves Vianez Jr., Macrae,A., De Melo,A.C.N. and Vermelho,A.B.
    Peptidase inhibitors as a possible therapeutic strategy for Chagas disease
    Curr Enzyme Inhib (2010) 6, 183-194. DOI  I
  89. 2009
  90. Bryant,C., Kerr,I.D., Debnath,M., Ang,K.K., Ratnam,J., Ferreira,R.S., Jaishankar,P., Zhao,D., Arkin,M.R., McKerrow,J.H., Brinen,L.S. and Renslo,A.R.
    Novel non-peptidic vinylsulfones targeting the S2 and S3 subsites of parasite cysteine proteases
    Bioorg Med Chem Lett (2009) 19, 6218-6221. PubMed  Europe PubMed DOI  S  I
  91. Caffrey,C.R. and Steverding,D.
    Kinetoplastid papain-like cysteine peptidases
    Mol Biochem Parasitol (2009) 167, 12-19. PubMed  Europe PubMed DOI  I
  92. dos Santos Filho,J.M., Leite,A.C., de Oliveira,B.G., Moreira,D.R., Lima,M.S., Soares,M.B. and Leite,L.F.
    Design, synthesis and cruzain docking of 3-(4-substituted-aryl)-1,2,4-oxadiazole-N-acylhydrazones as anti-Trypanosoma cruzi agents
    Bioorg Med Chem (2009) 17, 6682-6691. PubMed  Europe PubMed DOI  I
  93. Ferreira,R.S., Bryant,C., Ang,K.K., McKerrow,J.H., Shoichet,B.K. and Renslo,A.R.
    Divergent modes of enzyme inhibition in a homologous structure-activity series
    J Med Chem (2009) 52, 5005-5008. PubMed  Europe PubMed DOI  I
  94. 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 Chem (2009) 284, 25697-25703. PubMed  Europe PubMed DOI  PMC  EPMC  S  I
  95. Romeiro,N.C., Aguirre,G., Hernandez,P., Gonzalez,M., Cerecetto,H., Aldana,I., Perez-Silanes,S., Monge,A., Barreiro,E.J. and Lima,L.M.
    Synthesis, trypanocidal activity and docking studies of novel quinoxaline-N-acylhydrazones, designed as cruzain inhibitors candidates
    Bioorg Med Chem (2009) 17, 641-652. PubMed  Europe PubMed DOI  I
  96. 2008
  97. Brak,K., Doyle,P.S., McKerrow,J.H. and Ellman,J.A.
    Identification of a new class of nonpeptidic inhibitors of cruzain
    J Am Chem Soc (2008) 130, 6404-6410. PubMed  Europe PubMed DOI  PMC  EPMC  I
  98. Chen,Y.T., Lira,R., Hansell,E., McKerrow,J.H. and Roush,W.R.
    Synthesis of macrocyclic trypanosomal cysteine protease inhibitors
    Bioorg Med Chem Lett (2008) 18, 5860-5863. PubMed  Europe PubMed DOI  PMC  EPMC  I
  99. Freitas,R.F., Oprea,T.I. and Montanari,C.A.
    2D QSAR and similarity studies on cruzain inhibitors aimed at improving selectivity over cathepsin L
    Bioorg Med Chem (2008) 16, 838-853. PubMed  Europe PubMed DOI  I
  100. Guido,R.V., Trossini,G.H., Castilho,M.S., Oliva,G., Ferreira,E.I. and Andricopulo,A.D.
    Structure-activity relationships for a class of selective inhibitors of the major cysteine protease from Trypanosoma cruzi
    J Enzyme Inhib Med Chem (2008) 23, 964-973. PubMed  Europe PubMed DOI  I
  101. Jaishankar,P., Hansell,E., Zhao,D.M., Doyle,P.S., McKerrow,J.H. and Renslo,A.R.
    Potency and selectivity of P2/P3-modified inhibitors of cysteine proteases from trypanosomes
    Bioorg Med Chem Lett (2008) 18, 624-628. PubMed  Europe PubMed DOI  I
  102. Zanatta,N., Amaral,S.S., Dos Santos,J.M., de Mello,D.L., Fernandes,L., Bonacorso,H.G., Martins,M.A., Andricopulo,A.D. and Borchhardt,D.M.
    Convergent synthesis and cruzain inhibitory activity of novel 2-(N'-benzylidenehydrazino)-4-trifluoromethyl-pyrimidines
    Bioorg Med Chem (2008) 16, 10236-10243. PubMed  Europe PubMed DOI  I
  103. 2007
  104. Doyle,P.S., Zhou,Y.M., Engel,J.C. and McKerrow,J.H.
    A cysteine protease inhibitor cures Chagas' disease in an immunodeficient-mouse model of infection
    Antimicrob Agents Chemother (2007) 51, 3932-3939. PubMed  Europe PubMed DOI  PMC  EPMC  I
  105. Gonzalez,F.V., Izquierdo,J., Rodriguez,S., McKerrow,J.H. and Hansell,E.
    Dipeptidyl-alpha,beta-epoxyesters as potent irreversible inhibitors of the cysteine proteases cruzain and rhodesain
    Bioorg Med Chem Lett (2007) 17, 6697-6700. PubMed  Europe PubMed DOI  I
  106. Leite,A.C., Moreira,D.R., Cardoso,M.V., Hernandes,M.Z., Alves Pereira,V.R., Silva,R.O., Kiperstok,A.C., Lima,M. and Soares,M.B.
    Synthesis, cruzain docking, and in vitro studies of aryl-4-oxothiazolylhydrazones against Trypanosoma cruzi
    ChemMedChem (2007) 2, 1339-1345. PubMed  Europe PubMed DOI  I
  107. 2005
  108. Barr,S.C., Warner,K.L., Kornreic,B.G., Piscitelli,J., Wolfe,A., Benet,L. and McKerrow,J.H.
    A cysteine protease inhibitor protects dogs from cardiac damage during infection by Trypanosoma cruzi
    Antimicrob Agents Chemother (2005) 49, 5160-5161. PubMed  Europe PubMed DOI  PMC  EPMC  I
  109. [YEAR:15-3-2005]Choe,Y., Brinen,L.S., Price,M.S., Engel,J.C., Lange,M., Grisostomi,C., Weston,S.G., Pallai,P.V., Cheng,H., Hardy,L.W., Hartsough,D.S., McMakin,M., Tilton,R.F., Baldino,C.M. and Craik,C.S.
    Development of alpha-keto-based inhibitors of cruzain, a cysteine protease implicated in Chagas disease
    Bioorg Med Chem (15-3-2005) 13, 2141-2156. PubMed  Europe PubMed DOI  S  I
  110. [YEAR:3-1-2005]Fujii,N., Mallari,J.P., Hansell,E.J., Mackey,Z., Doyle,P., Zhou,Y.M., Gut,J., Rosenthal,P.J., McKerrow,J.H. and Guy,R.K.
    Discovery of potent thiosemicarbazone inhibitors of rhodesain and cruzain
    Bioorg Med Chem Lett (3-1-2005) 15, 121-123. PubMed  Europe PubMed DOI  I
  111. 2003
  112. Chibale,K. and Musonda,C.C.
    The synthesis of parasitic cysteine protease and trypanothione reductase inhibitors
    Curr Med Chem (2003) 10, 1863-1889. PubMed  Europe PubMed DOI  I
  113. [YEAR:20-10-2003]Chiyanzu,I., Hansell,E., Gut,J., Rosenthal,P.J., McKerrow,J.H. and Chibale,K.
    Synthesis and evaluation of isatins and thiosemicarbazone derivatives against cruzain, falcipain-2 and rhodesain
    Bioorg Med Chem Lett (20-10-2003) 13, 3527-3530. PubMed  Europe PubMed DOI  I
  114. Huang,L., Brinen,L.S. and Ellman,J.A.
    Crystal structures of reversible ketone-based inhibitors of the cysteine protease cruzain
    Bioorg Med Chem (2003) 11, 21-29. PubMed  Europe PubMed DOI  S  I
  115. 2002
  116. [YEAR:20-6-2002]Du,X., Guo,C., Hansell,E., Doyle,P.S., Caffrey,C.R., Holler,T.P., McKerrow,J.H. and Cohen,F.E.
    Synthesis and structure-activity relationship study of potent trypanocidal thio semicarbazone inhibitors of the trypanosomal cysteine protease cruzain
    J Med Chem (20-6-2002) 45, 2695-2707. PubMed  Europe PubMed DOI  I
  117. [YEAR:21-10-2002]Huang,L. and Ellman,J.A.
    General solid-phase method to prepare novel cyclic ketone inhibitors of the cysteine protease cruzain
    Bioorg Med Chem Lett (21-10-2002) 12, 2993-2996. PubMed  Europe PubMed DOI  I
  118. [YEAR:31-1-2002]Huang,L., Lee,A. and Ellman,J.A.
    Identification of potent and selective mechanism-based inhibitors of the cysteine protease cruzain using solid-phase parallel synthesis
    J Med Chem (31-1-2002) 45, 676-684. PubMed  Europe PubMed DOI  I
  119. [YEAR:3-6-2002]Rodrigues,C.R., Flaherty,T.M., Springer,C., McKerrow,J.H. and Cohen,F.E.
    CoMFA and HQSAR of acylhydrazide cruzain inhibitors
    Bioorg Med Chem Lett (3-6-2002) 12, 1537-1541. PubMed  Europe PubMed DOI  I
  120. 2001
  121. [YEAR:25-4-2001]Lima,A.P., dos Reis,F.C., Serveau,C., Lalmanach,G., Juliano,L., Menard,R., Vernet,T., Thomas,D.Y., Storer,A.C. and Scharfstein,J.
    Cysteine protease isoforms from Trypanosoma cruzi, cruzipain 2 and cruzain, present different substrate preference and susceptibility to inhibitors
    Mol Biochem Parasitol (25-4-2001) 114, 41-52. PubMed  Europe PubMed DOI  I
  122. [YEAR:22-10-2001]Roush,W.R., Cheng,J., Knapp-Reed,B., Alvarez-Hernandez,A., McKerrow,J.H., Hansell,E. and Engel,J.C.
    Potent second generation vinyl sulfonamide inhibitors of the trypanosomal cysteine protease cruzain
    Bioorg Med Chem Lett (22-10-2001) 11, 2759-2762. PubMed  Europe PubMed DOI  I
  123. 2000
  124. Jacobsen,W., Christians,U. and Benet,L.Z.
    In vitro evaluation of the disposition of a novel cysteine protease inhibitor
    Drug Metab Dispos (2000) 28, 1343-1351. PubMed  Europe PubMed  I
  125. [YEAR:8-12-2000]Roush,W.R., Hernandez,A.A., McKerrow,J.H., Selzer,P.M., Hansell,E. and Engel,J.C.
    Design, synthesis and evaluation of D-homophenylalanyl epoxysuccinate inhibitors of the trypanosomal cysteine protease cruzain
    Tetrahedron (8-12-2000) 56, 9747-9762.  I
  126. 1998
  127. [YEAR:17-8-1998]Engel,J.C., Doyle,P.S., Hsieh,I. and McKerrow,J.H.
    Cysteine protease inhibitors cure an experimental Trypanosoma cruzi infection
    J Exp Med (17-8-1998) 188, 725-734. PubMed  Europe PubMed DOI  PMC  EPMC  I
  128. [YEAR:6-10-1998]Roush,W.R., Gonzalez,F.V., McKerrow,J.H. and Hansell,E.
    Design and synthesis of dipeptidyl alpha',beta'-epoxy ketones, potent irreversible inhibitors of the cysteine protease cruzain
    Bioorg Med Chem Lett (6-10-1998) 8, 2809-2812. PubMed  Europe PubMed DOI  I
  129. Scheidt,K.A., Roush,W.R., McKerrow,J.H., Selzer,P.M., Hansell,E. and Rosenthal,P.J.
    Structure-based design, synthesis and evaluation of conformationally constrained cysteine protease inhibitors
    Bioorg Med Chem (1998) 6, 2477-2494. PubMed  Europe PubMed DOI  I
  130. 1997
  131. Gillmor,S.A., Craik,C.S. and Fletterick,R.J.
    Structural determinants of specificity in the cysteine protease cruzain
    Protein Sci (1997) 6, 1603-1611. PubMed  Europe PubMed DOI  PMC  EPMC  S  I
  132. 1994
  133. [YEAR:15-11-1994]Franke de Cazzulo,B.M., Martinez,J., North,M.J., Coombs,G.H. and Cazzulo,J.J.
    Effects of proteinase inhibitors on the growth and differentiation of Trypanosoma cruzi
    FEMS Microbiol Lett (15-11-1994) 124, 81-86. PubMed  Europe PubMed DOI  I