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

N-Myristoyltransferases as antileishmanial targets: a piggyback approach with benzoheterocyclic analogues

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Author(s):
Luis Otávio Junqueira [1] ; Marcela Oliveira Legramanti da Costa [2] ; Daniela Gonçales Galasse Rando [3]
Total Authors: 3
Affiliation:
[1] Universidade Federal de São Paulo. Instituto de Ciências Ambientais, Químicas e Farmacêuticas. Departamento de Ciências Farmacêuticas - Brasil
[2] Universidade Federal de São Paulo. Instituto de Ciências Ambientais, Químicas e Farmacêuticas. Departamento de Ciências Farmacêuticas - Brasil
[3] Universidade Federal de São Paulo. Instituto de Ciências Ambientais, Químicas e Farmacêuticas. Departamento de Ciências Farmacêuticas - Brasil
Total Affiliations: 3
Document type: Journal article
Source: Brazilian Journal of Pharmaceutical Sciences; v. 55, 2019-10-24.
Abstract

Leishmaniasis is one of the neglected diseases that remain in need for pharmacological alternatives. In this context, N-Myristoyltransferases (NMT) arise as interesting targets to explore since they are involved in the co/post-translational processing of peptides which are responsible for host cell invasion. Studies that consider these enzymes as targets point out the potential of benzoheterocyclic compounds as inhibitors of Candida albicans’s N-myristoyltransferase. Here we applied a combination of comparative binding site analysis and molecular docking studies based on a Piggyback approach in the search for new Leishmania major NMT ligands. Our results revealed that NMT enzymes from both pathogens present enough structural similarity to allow extrapolation of the knowledge available from C. albicans studies to develop new L. major NMT inhibitors. Molecular docking studies with benzoheterocyclic analogues indicate the potential of benzothiazole derivatives as L. major NMT ligands, giving rise to a completely new class of chemical compounds to be explored in the development of antileishmanial drugs. (AU)

FAPESP's process: 13/01875-0 - Parallel synthesis, in vitro screening and SAR studies of a nitroderivatives compounds library active against macrophage's pathogens: Mycobacterium tuberculosis NRP forms and Leishmania sp
Grantee:Daniela Goncales Galasse Rando
Support Opportunities: Regular Research Grants