Discovery of Novel Inhibitors of Cruzain Cysteine Protease of Trypanosoma cruzi .

Autor:	Prates JLB; Department of Drugs and Medicine, School of Pharmaceutical Sciences, São Paulo State University (UNESP), Araraquara, SP, Brazil.; Chemistry Institute Araraquara, São Paulo State University (UNESP), SP, Brazil., Lopes JR; Department of Drugs and Medicine, School of Pharmaceutical Sciences, São Paulo State University (UNESP), Araraquara, SP, Brazil., Chin CM; Department of Drugs and Medicine, School of Pharmaceutical Sciences, São Paulo State University (UNESP), Araraquara, SP, Brazil.; Union of the Colleges of the Great Lakes (UNILAGO), School of Medicine, Advanced Research Center in Medicine, São José do Rio Preto, SP, Brazil., Ferreira EI; LAPEN-Laboratory of Design and Synthesis of Chemotherapeutic Agents Potentially Active on Neglected Diseases, Department of Pharmacy, School of Pharmaceutical Sciences, University of São Paulo (USP), São Paulo, SP, Brazil., Dos Santos JL; Department of Drugs and Medicine, School of Pharmaceutical Sciences, São Paulo State University (UNESP), Araraquara, SP, Brazil.; Chemistry Institute Araraquara, São Paulo State University (UNESP), SP, Brazil., Scarim CB; Department of Drugs and Medicine, School of Pharmaceutical Sciences, São Paulo State University (UNESP), Araraquara, SP, Brazil.
Jazyk:	angličtina
Zdroj:	Current medicinal chemistry [Curr Med Chem] 2024; Vol. 31 (16), pp. 2285-2308.
DOI:	10.2174/0109298673254864230921090519
Abstrakt:	Chagas disease (CD) is a parasitic disease endemic in several developing countries. According to the World Health Organization, approximately 6-8 million people worldwide are inflicted by CD. The scarcity of new drugs, mainly for the chronic phase, is the main reason for treatment limitation in CD. Therefore, there is an urgent need to discover new targets for which new therapeutical agents could be developed. Cruzain cysteine protease (CCP) is a promising alternative because this enzyme exhibits pleiotropic effects by acting as a virulence factor, modulating host immune cells, and interacting with host cells. This systematic review was conducted to discover new compounds that act as cruzain inhibitors, and their effects in vitro were studied through enzymatic assays and molecular docking. Additionally, the advances and perspectives of these inhibitors are discussed. These findings are expected to contribute to medicinal chemistry in view of the design of new, safe, and efficacious inhibitors against Trypanosoma cruzi CCP detected in the last decade (2013-2022) to provide scaffolds for further optimization, aiming toward the discovery of new drugs. (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)
Databáze:	MEDLINE
Externí odkaz:	Zobrazit plný text záznamu