Identification of novel chemical scaffolds Inhibiting trypanothione synthetase from pathogenic trypanosomatids

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],...

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Detalles Bibliográficos
Autores principales: Benítez, Diego, Medeiros, Andrea, Fiestas, Lucía, Panozzo Zénere, Esteban Andrés, Maiwald, Franziska, Prousis, Kyriakos C., Roussaki, Marina, Calogeropoulou, Theodora, Detsi, Anastasia, Jaeger, Timo, Šarlauskas, Jonas, Peterlin Mašič, Lucíja, Kunick, Conrad, Labadie, Guillermo Roberto, Flohé, Leopold, Comini, Marcelo A.
Formato: article artículo publishedVersion
Lenguaje:Inglés
Publicado: Public Library of Science (PLOS) 2020
Materias:
Neglected Diseases
Trypanothione Synthetase Inhibitors
Pathogenic Trypanosomatids
Leishmania
Trypanosoma
Acceso en línea:http://hdl.handle.net/2133/19536
http://hdl.handle.net/2133/19536
Aporte de:
Repositorio Hipermedial de la Universidad Nacional de Rosario (UNR) de Universidad Nacional de Rosario
Descripción
Sumario: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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