NMR Biochemical Assay for Oxidosqualene Cyclase: Evaluation of Inhibitor Activities on Trypanosoma cruzi and Human Enzymes

Journal of Medicinal Chemistry
Osamu TaniKazuhiko Yamasaki

Abstract

Oxidosqualene cyclase (OSC), a membrane-associated protein, is a key enzyme of sterol biosynthesis. Here we report a novel assay for OSC, involving reaction in aqueous solution, NMR quantification in organic solvent, and factor analysis of spectra. We evaluated one known and three novel inhibitors on OSC of Trypanosoma cruzi, a parasite causative of Chagas disease, and compared their effects on human OSC for selectivity. Among them, one novel inhibitor showed a significant parasiticidal activity.

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Citations

Mar 30, 2019·Proceedings of the National Academy of Sciences of the United States of America·Richard E PhillipsC David Allis
Aug 15, 2019·Expert Opinion on Drug Discovery·Fernando Villalta, Girish Rachakonda
Sep 13, 2019·Expert Opinion on Drug Discovery·Miaomiao Liu, Ronald J Quinn

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