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Identification of Novel Chemical Scaffolds Inhibiting Trypanothione Synthetase from Pathogenic Trypanosomatids.

Résumé : BACKGROUND: The search for novel chemical entities targeting essential and parasite-specific pathways is considered a priority for neglected diseases such as trypanosomiasis and leishmaniasis. The thiol-dependent redox metabolism of trypanosomatids relies on bis-glutathionylspermidine [trypanothione, T(SH)2], a low molecular mass cosubstrate absent in the host. In pathogenic trypanosomatids, a single enzyme, trypanothione synthetase (TryS), catalyzes trypanothione biosynthesis, which is indispensable for parasite survival. Thus, TryS qualifies as an attractive drug target candidate.
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Submitted on : Tuesday, September 26, 2017 - 5:05:17 PM
Last modification on : Tuesday, January 18, 2022 - 2:50:08 PM

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Diego Benítez, Andrea Medeiros, Lucía Fiestas, Esteban A Panozzo-Zenere, Franziska Maiwald, et al.. Identification of Novel Chemical Scaffolds Inhibiting Trypanothione Synthetase from Pathogenic Trypanosomatids.. PLoS Neglected Tropical Diseases, Public Library of Science, 2016, 10 (4), pp.e0004617. ⟨10.1371/journal.pntd.0004617⟩. ⟨pasteur-01498320⟩

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