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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

Targeting cysteine proteases in trypanosomatid disease drug discovery

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Author(s):
Ferreira, Leonardo G. [1] ; Andricopulo, Adriano D. [1]
Total Authors: 2
Affiliation:
[1] Univ Sao Paulo, Inst Fis Sao Carlos, Ctr Pesquisa & Inovacao Biodiversidade & Farmacos, Lab Quim Med & Computac, Ave Joao Dagnone 1100, BR-13563120 Sao Carlos, SP - Brazil
Total Affiliations: 1
Document type: Review article
Source: PHARMACOLOGY & THERAPEUTICS; v. 180, p. 49-61, DEC 2017.
Web of Science Citations: 14
Abstract

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 in drug discovery have focused on several enzymes from these protozoans, among which cysteine proteases have been validated as molecular targets for pharmacological intervention. These enzymes are expressed during the entire life cycle of trypanosomatid parasites and are essential to many biological processes, including infectivity to the human host. As a result of advances in the knowledge of the structural aspects of cysteine proteases and their role in disease physiopathology, inhibition of these enzymes by small molecules has been demonstrated to be a worthwhile approach to trypanosomatid drug research. This review provides an update on drug discovery strategies targeting the cysteine peptidases cruzain from Trypanosoma cruzi and rhodesain and cathepsin B from Trypanosoma brucei. Given that current chemotherapy for Chagas disease and human African trypanosomiasis has several drawbacks, cysteine proteases will continue to be actively pursued as valuable molecular targets in trypanosomatid disease drug discovery efforts. (C) 2017 Published by Elsevier Inc. (AU)

FAPESP's process: 13/07600-3 - CIBFar - Center for Innovation in Biodiversity and Drug Discovery
Grantee:Glaucius Oliva
Support Opportunities: Research Grants - Research, Innovation and Dissemination Centers - RIDC
FAPESP's process: 13/25658-9 - Design and Development of Drug Candidates for Chagas Disease
Grantee:Leonardo Luiz Gomes Ferreira
Support Opportunities: Scholarships in Brazil - Post-Doctoral