Trypanosoma cruzi Sirtuin 2 as a Relevant Druggable Target: New Inhibitors Developed by Computer-Aided Drug Design.
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ABSTRACT:
SUBMITTER: Ferreira GM
PROVIDER: S-EPMC10057528 | biostudies-literature | 2023 Mar
REPOSITORIES: biostudies-literature
Publications
<i>Trypanosoma cruzi</i> Sirtuin 2 as a Relevant Druggable Target: New Inhibitors Developed by Computer-Aided Drug Design.
Ferreira Glaucio Monteiro GM Kronenberger Thales T Maltarollo Vinicius Gonçalves VG Poso Antti A de Moura Gatti Fernando F Almeida Vitor Medeiros VM Marana Sandro Roberto SR Lopes Carla Duque CD Tezuka Daiane Yukie DY de Albuquerque Sérgio S da Silva Emery Flavio F Trossini Gustavo Henrique Goulart GHG
Pharmaceuticals (Basel, Switzerland) 20230310 3
<i>Trypanosoma cruzi</i>, the etiological agent of Chagas disease, relies on finely coordinated epigenetic regulation during the transition between hosts. Herein we targeted the silent information regulator 2 (Sir2) enzyme, a NAD<sup>+</sup>-dependent class III histone deacetylase, to interfere with the parasites' cell cycle. A combination of molecular modelling with on-target experimental validation was used to discover new inhibitors from commercially available compound libraries. We selected ...[more]
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