Design of Gallinamide A Analogs as Potent Inhibitors of the Cysteine Proteases Human Cathepsin L and Trypanosoma cruzi Cruzain
Gallinamide A, originally isolated with a modest antimalarial activity, was subsequently
reisolated and characterized as a potent, selective, and irreversible inhibitor of the human …
reisolated and characterized as a potent, selective, and irreversible inhibitor of the human …
Intramolecular Interactions Enhance the Potency of Gallinamide A Analogues against Trypanosoma cruzi
E Barbosa Da Silva, V Sharma… - Journal of Medicinal …, 2022 - ACS Publications
Gallinamide A, a metabolite of the marine cyanobacterium Schizothrix sp., selectively
inhibits cathepsin L-like cysteine proteases. We evaluated the potency of gallinamide A and …
inhibits cathepsin L-like cysteine proteases. We evaluated the potency of gallinamide A and …
Identification and optimization of inhibitors of trypanosomal cysteine proteases: cruzain, rhodesain, and TbCatB
BT Mott, RS Ferreira, A Simeonov… - Journal of medicinal …, 2010 - ACS Publications
Trypanosoma cruzi and Trypanosoma brucei are parasites that cause Chagas' disease and
African sleeping sickness, respectively. Both parasites rely on essential cysteine proteases …
African sleeping sickness, respectively. Both parasites rely on essential cysteine proteases …
Targeting cysteine proteases in trypanosomatid disease drug discovery
LG Ferreira, AD Andricopulo - Pharmacology & therapeutics, 2017 - Elsevier
Chagas disease and human African trypanosomiasis are endemic conditions in Latin
America and Africa, respectively, for which no effective and safe therapy is available. Efforts …
America and Africa, respectively, for which no effective and safe therapy is available. Efforts …
Discovery and characterization of trypanocidal cysteine protease inhibitors from the 'malaria box'
GAN Pereira, EB da Silva, SFP Braga, PG Leite… - European journal of …, 2019 - Elsevier
Abstract Chagas disease, Human African Trypanosomiasis, and schistosomiasis are
neglected parasitic diseases for which new treatments are urgently needed. To identify new …
neglected parasitic diseases for which new treatments are urgently needed. To identify new …
The propeptide of cruzipain− a potent selective inhibitor of the trypanosomal enzymes cruzipain and brucipain, and of the human enzyme cathepsin F
FCG Reis, TFR Costa, T Sulea, A Mezzetti… - The FEBS …, 2007 - Wiley Online Library
Papain‐like cysteine proteases of pathogenic protozoa play important roles in parasite
growth, differentiation and host cell invasion. The main cysteine proteases of Trypanosoma …
growth, differentiation and host cell invasion. The main cysteine proteases of Trypanosoma …
The major cysteine proteinase of Trypanosoma cruzi: a valid target for chemotherapy of Chagas disease
J Cazzulo, V Stoka, V Turk - Current pharmaceutical design, 2001 - ingentaconnect.com
Trypanosoma cruzi, the causative agent of the American Trypanosomiasis, Chagas disease,
contains a major cysteine proteinase (CP), cruzipain (also known as cruzain, or GP57/51) …
contains a major cysteine proteinase (CP), cruzipain (also known as cruzain, or GP57/51) …
[HTML][HTML] Anti-trypanosomal activity of non-peptidic nitrile-based cysteine protease inhibitors
ACB Burtoloso, S De Albuquerque… - PLoS Neglected …, 2017 - journals.plos.org
The cysteine protease cruzipain is considered to be a validated target for therapeutic
intervention in the treatment of Chagas disease. Anti-trypanosomal activity against the CL …
intervention in the treatment of Chagas disease. Anti-trypanosomal activity against the CL …
Identification of a new class of nonpeptidic inhibitors of cruzain
K Brak, PS Doyle, JH McKerrow… - Journal of the American …, 2008 - ACS Publications
Cruzain is the major cysteine protease of Trypanosoma cruzi, which is the causative agent of
Chagas disease and is a promising target for the development of new chemotherapy. With …
Chagas disease and is a promising target for the development of new chemotherapy. With …
Structure-Based Optimization of Quinazolines as Cruzain and TbrCATL Inhibitors
E Barbosa da Silva, DA Rocha, IS Fortes… - Journal of Medicinal …, 2021 - ACS Publications
The cysteine proteases, cruzain and Tbr CATL (rhodesain), are therapeutic targets for
Chagas disease and Human African Trypanosomiasis, respectively. Among the known …
Chagas disease and Human African Trypanosomiasis, respectively. Among the known …