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Boosting the Discovery of Small Molecule Inhibitors of Glucose-6-Phosphate Dehydrogenase for the Treatment of Cancer, Infectious Diseases, and Inflammation.


ABSTRACT: We present an overview of small molecule glucose-6-phosphate dehydrogenase (G6PD) inhibitors that have potential for use in the treatment of cancer, infectious diseases, and inflammation. Both steroidal and nonsteroidal inhibitors have been identified with steroidal inhibitors lacking target selectivity. The main scaffolds encountered in nonsteroidal inhibitors are quinazolinones and benzothiazinones/benzothiazepinones. Three molecules show promise for development as antiparasitic (25 and 29) and anti-inflammatory (32) agents. Regarding modality of inhibition (MOI), steroidal inhibitors have been shown to be uncompetitive and reversible. Nonsteroidal small molecules have exhibited all types of MOI. Strategies to boost the discovery of small molecule G6PD inhibitors inc

SUBMITTER: Koperniku A 

PROVIDER: S-EPMC9553131 | biostudies-literature | 2022 Mar

REPOSITORIES: biostudies-literature