Selective Chemical Inhibition of PGC-1? Gluconeogenic Activity Ameliorates Type 2 Diabetes.
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ABSTRACT:
SUBMITTER: Sharabi K
PROVIDER: S-EPMC5398763 | biostudies-literature | 2017 Mar
REPOSITORIES: biostudies-literature
Publications
Selective Chemical Inhibition of PGC-1α Gluconeogenic Activity Ameliorates Type 2 Diabetes.
Sharabi Kfir K Lin Hua H Tavares Clint D J CDJ Dominy John E JE Camporez Joao Paulo JP Perry Rachel J RJ Schilling Roger R Rines Amy K AK Lee Jaemin J Hickey Marc M Bennion Melissa M Palmer Michelle M Nag Partha P PP Bittker Joshua A JA Perez José J Jedrychowski Mark P MP Ozcan Umut U Gygi Steve P SP Kamenecka Theodore M TM Shulman Gerald I GI Schreiber Stuart L SL Griffin Patrick R PR Puigserver Pere P
Cell 20170301 1
Type 2 diabetes (T2D) is a worldwide epidemic with a medical need for additional targeted therapies. Suppression of hepatic glucose production (HGP) effectively ameliorates diabetes and can be exploited for its treatment. We hypothesized that targeting PGC-1α acetylation in the liver, a chemical modification known to inhibit hepatic gluconeogenesis, could be potentially used for treatment of T2D. Thus, we designed a high-throughput chemical screen platform to quantify PGC-1α acetylation in cells ...[more]
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