Results 11 to 20 of about 1,018 (177)

Chemoinformatics Studies on a Series of Imidazoles as Cruzain Inhibitors [PDF]

Biomolecules, 2021
Natural products based on imidazole scaffolds have inspired the discovery of a wide variety of bioactive compounds. Herein, a series of imidazoles that act as competitive and potent cruzain inhibitors was investigated using a combination of ligand- and ...
Leonardo L G Ferreira, Mariana Laureano De Souza, Celso De Oliveira Rezende Júnior   +2 more
exaly   +9 more sources

The Trypanosoma cruzi protease cruzain mediates immune evasion. [PDF]

PLoS Pathogens, 2011
Trypanosoma cruzi is the causative agent of Chagas' disease. Novel chemotherapy with the drug K11777 targets the major cysteine protease cruzain and disrupts amastigote intracellular development.
Patricia S Doyle, Yuan M Zhou, Ivy Hsieh, Doron C Greenbaum, James H McKerrow, Juan C Engel   +5 more
doaj   +5 more sources

Screening the Pathogen Box to Discover and Characterize New Cruzain and TbrCatL Inhibitors [PDF]

Pathogens, 2023
Chagas disease and Human African Trypanosomiasis, caused by Trypanosoma cruzi and T. brucei, respectively, pose relevant health challenges throughout the world, placing 65 to 70 million people at risk each.
Thales do Valle Moreira, Luan Carvalho Martins, Lucas Abreu Diniz, Talita Cristina Diniz Bernardes, Renata Barbosa de Oliveira, Rafaela Salgado Ferreira   +5 more
doaj   +4 more sources

Computational identification of uncharacterized cruzain binding sites. [PDF]

PLoS Neglected Tropical Diseases, 2010
Chagas disease, caused by the unicellular parasite Trypanosoma cruzi, claims 50,000 lives annually and is the leading cause of infectious myocarditis in the world.
Jacob D Durrant, Henrik Keränen, Benjamin A Wilson, J Andrew McCammon   +3 more
doaj   +7 more sources

Cystatin from Austrelaps superbus snake venom as a model for identifying potential inhibitors of Trypanosoma cruzi cruzain [PDF]

Journal of Venomous Animals and Toxins including Tropical Diseases
Background: Chagas disease (CD), caused by Trypanosoma cruzi, affects approximately seven million individuals worldwide, with the highest number of cases in Latin America. CD has two phases, of which the chronic phase is characterized by reduced efficacy
Jorge Javier Alfonso Ruiz Díaz, Ana Fidelina Gómez Garay, Anderson Makoto Kayano, Rudson Holanda, Aleff Ferreira Francisco, Christian Collins Kuehn, Andreimar Martins Soares, Celeste Vega, Leonardo de Azevedo Calderon   +8 more
doaj   +3 more sources

Multiparameter Optimization of Trypanocidal Cruzain Inhibitors With In Vivo Activity and Favorable Pharmacokinetics [PDF]

Frontiers in Pharmacology, 2022
Cruzain, the main cysteine protease of Trypanosoma cruzi, plays key roles in all stages of the parasite’s life cycle, including nutrition acquisition, differentiation, evasion of the host immune system, and invasion of host cells.
Ivani Pauli, Celso de O. Rezende Jr., Brian W. Slafer, Marco A. Dessoy, Mariana L. de Souza, Leonardo L. G. Ferreira, Abraham L. M. Adjanohun, Rafaela S. Ferreira, Luma G. Magalhães, Renata Krogh, Simone Michelan-Duarte, Ricardo Vaz Del Pintor, Fernando B. R. da Silva, Fabio C. Cruz, Luiz C. Dias, Adriano D. Andricopulo   +15 more
doaj   +5 more sources

Convergent QSAR Models for the Prediction of Cruzain Inhibitors [PDF]

ACS Omega, 2023
Chagas disease is a parasitosis caused by Trypanosoma cruzi. Cruzain, the major cysteine protease from T. cruzi, is an excellent therapeutic target in the search for antichagasic drugs. It is important in the role of cell invasion, replication, differentiation, and metabolism of the parasite.
Rafael Bello Gonçalves, Witor Ribeiro Ferraz, Raisa Ludmila Calil, Marcus Tullius Scotti, Gustavo Henrique Goulart Trossini   +4 more
doaj   +4 more sources

Peptidomimetic Vinyl Heterocyclic Inhibitors of Cruzain Effect Antitrypanosomal Activity [PDF]

Journal of Medicinal Chemistry, 2020
Cruzain, an essential cysteine protease of the parasitic protozoan, Trypanosoma cruzi, is an important drug target for Chagas disease. We describe here a new series of reversible but time-dependent inhibitors of cruzain, composed of a dipeptide scaffold appended to vinyl heterocycles meant to provide replacements for the irreversible reactive "warheads"
Bala C. Chenna, Linfeng Li, Drake M. Mellott, Xiang Zhai, Jair L. Siqueira-Neto, Claudia Calvet Alvarez, Jean A. Bernatchez, Emily Desormeaux, Elizabeth Alvarez Hernandez, Jana Gomez, James H. McKerrow, Jorge Cruz-Reyes, Thomas D. Meek   +12 more
core   +6 more sources

In Silico Studies and Biological Evaluation of Thiosemicarbazones as Cruzain-Targeting Trypanocidal Agents for Chagas Disease [PDF]

Pharmaceutics
Background/Objectives: Chagas disease remains a major unmet medical need due to the limited efficacy and safety of current therapies. Here, we investigated sixteen thiosemicarbazone (TSC) derivatives as cruzain inhibitors using an integrated in silico/in
Lidiane Meier, Milena F. C. V. de Melo, Heitor R. Abreu, Isabella M. e Oliveira, Larissa Sens, Thiago H. Doring, Renata Krogh, Adilson Beatriz, Adriano D. Andricopulo, Sumbal Saba, Aldo S. de Oliveira, Jamal Rafique   +11 more
doaj   +2 more sources

Pharmacophore Model of Cruzain Inhibitors

QSAR & Combinatorial Science, 2009
AbstractChagas disease, caused by the protozoan Trypanosoma cruzi, is one of the most serious amongst the so‐called neglected diseases in Latin America, specially in Brazil. So far there has been no effective treatment for the chronic phase of this disease. Cruzain is a major cysteine protease of T.
Alberto Malvezzi, Leandro de Rezende, Antonia T.‐do Amaral   +2 more
openaire   +2 more sources