Mechanistic and biological characterisation of novel N5-substituted paullones targeting the biosynthesis of trypanothione in Leishmania

Mechanistic and biological characterisation of novel N5-substituted paullones targeting the biosynthesis of trypanothione in Leishmania

Trypanothione synthetase (TryS) produces N1,N8-bis(glutathionyl)spermidine (or trypanothione) at the expense of ATP. Trypanothione is a metabolite unique and essential for survival and drug-resistance of trypanosomatid parasites. In this study, we report the mechanistic and biological characterisati...

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Bibliographic Details
Main Authors: Andrea Medeiros, Diego Benítez, Ricarda S. Korn, Vinicius C. Ferreira, Exequiel Barrera, Federico Carrión, Otto Pritsch, Sergio Pantano, Conrad Kunick, Camila I. de Oliveira, Oliver C. F. Orban, Marcelo A. Comini
Format: Article
Language:English
Published: Taylor & Francis Group 2020-01-01
Series:Journal of Enzyme Inhibition and Medicinal Chemistry
Subjects:
paullone
trypanothione synthetase
leishmania
thiol
inhibition mode
Online Access:http://dx.doi.org/10.1080/14756366.2020.1780227

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