Results 91 to 100 of about 1,018 (177)

Analysis of novel low nanomolar thiosemicarbazone inhibitors of cruzain

The FASEB Journal, 2010
Chagas’ disease, caused by the protozoan Trypanosoma cruzi, affects millions of people in Latin America where it is a major cause of heart disease.
Gustavo Edgardo Chavarria, Jacob A. Wiley, Kishore Kumar Gaddale Devanna, Wara M. Arispe, Weiyue Li, Lauren J. Adamson, Lindsay M. Jones, Matthew T. MacDonough, Kevin G. Pinney, Mary Lynn Trawick   +9 more
openaire   +1 more source

Identification and Optimization of Inhibitors of Trypanosomal Cysteine Proteases: Cruzain, Rhodesain, and TbCatB

, 2016
Trypanosoma cruzi and Trypanosoma brucei are parasites that cause Chagas’ disease and African sleeping sickness, respectively. Both parasites rely on essential cysteine proteases for survival: cruzain for T. cruzi and TbCatB/rhodesain for T. brucei.
Kenny Kean-Hooi Ang (2133721), David J. Maloney (126223), Ajit Jadhav (85100), Julia T. Silveira (2325715), Min Shen (68726), William Leister (1307844), Patricia S. Doyle (345076), Michelle R. Arkin (114394), Brian K. Shoichet (434829), Craig J. Thomas (17880), Christopher P. Austin (85106), Rafaela S. Ferreira (1271616), James H. McKerrow (113918), Bryan T. Mott (207629), James Inglese (85104), Anton Simeonov (85099)   +15 more
core   +1 more source

Inhibition of cysteine proteases by a natural biflavone: behavioral evaluation of fukugetin as papain and cruzain inhibitor

, 2012
Cruzain is the major cysteine protease of Trypanosoma cruzi, the infectious agent responsible for Chagas disease, and cruzain inhibitors display considerable antitrypanosomal activity. In the present work we elucidated crystallographic data of fukugetin,
Nagem, Tanus Jorge, Izidoro, Mario Augusto [UNIFESP], Juliano, Maria Aparecida, Camps, Ihosvany, Tersariol, Ivarne Luis dos Santos [UNIFESP], Juliano, Maria Aparecida [UNIFESP], Pereira, Ivan de Oliveira, Assis, Diego Magno [UNIFESP], Santos, Jorge Alexandre Nogueira [UNIFESP], Barros, Nilana Meza Tenório de, Tersariol, Ivarne Luis dos Santos, Barros, Nilana Meza Tenório de [UNIFESP], Santos, Marcelo Henrique dos, Doriguetto, Antonio Carlos, Izidoro, Mario Augusto, Assis, Diego Magno, Ellena, Javier, Gontijo, Vanessa Silva, Santos, Jorge Alexandre Nogueira   +18 more
core   +1 more source

Virtual screening models or cruzain inhibitors: development and Eexperimental validation

, 2016
Com o objetivo de buscar e identificar novo(s) inibidor(es) da cruzaína uma cisteíno-protease do Trypanosoma cruzi, o agente etiológico da doença de Chagas foram propostos, validados e, a seguir, aplicados sobre a biblioteca de compostos ZINC (3.294 ...
Malvezzi, Alberto
core   +1 more source

Small Molecule Inhibitors of Cruzain for Treatment of Chagas' Disease

, 2016
Chagas’ disease, a neglected tropical disease, affects millions worldwide. This zoonosis occurs as a result of parasitic invasion. The etiological organism, Trypanosoma cruzi (T. cruzi) enters mammalian host cells by triaatomine insects.
Ahmed, Hijab
core  

An active site affinity tag identifies processed active proteases of wild type and cruzain deficient T. cruzi.

, 2013
Iodinated DCGO4 (0.1, 1, 10, and-50 µM) was reacted with epimastigote extracts (105 epimastigotes/lane). Processed, active cruzain (47.5 kD) was identified as the major protease in wild type T. cruzi.
Ivy Hsieh (174545), James H. McKerrow (113918), Patricia S. Doyle (345076), Doron C. Greenbaum (345078), Juan C. Engel (145730), Yuan M. Zhou (345077)   +5 more
core   +1 more source

Experimental study and computational modelling of cruzain cysteine protease inhibition by dipeptidyl nitriles

, 2018
Chagas disease affects millions of people in Latin America. This disease is caused by the protozoan parasite Trypanossoma cruzi. The cysteine protease cruzain is a key enzyme for the survival and propagation of this parasite lifecycle.
Laughton, Charles A, Leitão, Andrei, Montanari, Carlos A., Rosini, Fabiana, Dos Santos, Alberto Monteiro, De Vita, Daniela, Lameira, Jerônimo, Cianni, Lorenzo, Laughton, Charles A., Montanari, Carlos A   +9 more
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RMSF and RMSD values of cruzain analyzed complexes.

, 2019
(A) RMSF profiles and (B) RMSD distribution calculated for analyzed systems of cruzain. Each parameter was calculated for backbone atoms and taking as reference structure the starting frame of productive MD simulations.
Lilian Hernández Alvarez (739728), Diego Enry Barreto Gomes (739732), Pedro Geraldo Pascutti (564220), Jorge Enrique Hernández González (739730)   +3 more
core   +1 more source

Inhibition of cruzain and cathepsins by nitrile-based cysteine protease inhibitors.

, 2017
Inhibition of cruzain and cathepsins by nitrile-based cysteine protease inhibitors.
Andrei Leitão (769676), Sérgio de Albuquerque (769673), Juliana C. Gomes (1883650), Carlos A. Montanari (449507), Jean F. R. Ribeiro (769678), Mark Furber (2465680), Cristiana Gonçalez (769674), Peter W. Kenny (769675), Antonio C. B. Burtoloso (1776874), José Carlos Quilles Júnior (3769651), Josmar R. Rocha (449500)   +10 more
core   +1 more source

Synthesis of 2��-Vinyl Heterocycles as Potential Electrophilic Components for Inhibitors of Cruzain and NMR Spectroscopic Analysis of Their Thia-��Michael Reactions with Thiols [PDF]

, 2017
Cruzain is an essential cysteine protease in Trypanosoma cruzi (T. cruzi), the causative agent of Chagas disease. Cruzain is an ideal target for development of potential trypanocidal drugs because of its critical role in the survival of T.
Luna Robles, Mireya
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