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https://www.arca.fiocruz.br/handle/icict/50552
TRYPANOSOMATIDAE DISEASES: FROM THE CURRENT THERAPY TO THE EFFICACIOUS ROLE OF TRYPANOTHIONE REDUCTASE IN DRUG DISCOVERY
trypanosomatidae diseases
trypanothione reductase
trypanothione reductase inhibitors
Affilliation
Universidade Federal de Santa Catarina. Departamento de Ciencias Farmaceuticas. Florianopolis, SC, Brazil
Fundação Oswaldo Cruz. Centro de Pesquisa Rene Rachou. Belo Horizonte, MG, Brazil
Universidade de São Paulo. Faculdade de Ciências Farmacêuticas. Ribeirão Preto, SP, Brazil
Fundação Oswaldo Cruz. Centro de Pesquisa Rene Rachou. Belo Horizonte, MG, Brazil
Universidade de São Paulo. Faculdade de Ciências Farmacêuticas. Ribeirão Preto, SP, Brazil
Abstract
According to World Health Organization (WHO), trypanosomiasis and leishmaniasis are the most challenging among the neglected tropical diseases. Comparative studies between Leishmania spp and Trypanosoma cruzi have been conducted aiming to find a broad spectrum antiprotozoal agent acting against both parasites. Among the potential molecular target, Trypanothione reductase (TR) is considered an ideal enzyme since it is involved in the unique thiol-based metabolism observed in the Trypanosomatidae family and is a validated target for the search of antitrypanosomatidae drugs. In this review we intend to describe the currently available therapy to treat trypanosomatidae diseases and to highlight important aspects of trypanothione reductase as a target for the search of new and selective inhibitors, such as tricyclic, diphenylsulfide, bicyclic and heterocyclic, polyamine, natural product, N-oxide and nitroheterocyclic, aryl beta-aminocarbonyl and, alpha,beta-unsaturated carbonyl derivatives
Keywords
Antitrypanosomatidae drugstrypanosomatidae diseases
trypanothione reductase
trypanothione reductase inhibitors
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