Drug-like molecules with anti-trypanothione synthetase activity identified by high throughput screening
Diego Benítez, Jaime Franco, Florencia Sardi, Alejandro Leyva, Rosario Durán, Gahee Choi, Gyongseon Yang, Tae Hee Kim, Namyoul Kim, Jinyeong Heo, Kideok Kim, Honggun Lee, Inhee Choi, Constantin Radu, David Shum, Joo Hwan No, Marcelo A. Comini
Abstract
TryS inhibitor (a singleton containing an adamantine moiety) exerted a non-covalent, non-competitive (with any of the substrates) inhibition of the enzyme. These data feed the drug discovery pipeline for trypanosomatids with novel and valuable information on chemical entities with drug potential.
Topics & Concepts
Trypanosoma bruceiChemistryBiochemistrySerine hydrolaseATP-binding cassette transporterStereochemistryEnzymeTransporterSerineGeneResearch on Leishmaniasis StudiesTrypanosoma species research and implicationsSynthesis and Biological Evaluation