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Selective Chemical Inhibition of PGC-1α Gluconeogenic Activity Ameliorates Type 2 Diabetes.

Cell | Mar 23, 2017

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 and identified small molecules that increase PGC-1α acetylation, suppress gluconeogenic gene expression, and reduce glucose production in hepatocytes. On the basis of potency and bioavailability, we selected a small molecule, SR-18292, that reduces blood glucose, strongly increases hepatic insulin sensitivity, and improves glucose homeostasis in dietary and genetic mouse models of T2D. These studies have important implications for understanding the regulatory mechanisms of glucose metabolism and treatment of T2D.

Pubmed ID: 28340340 RIS Download

Mesh terms: Acetylation | Animals | Blood Glucose | Cells, Cultured | Diabetes Mellitus, Type 2 | Gluconeogenesis | Glucose | Hepatocyte Nuclear Factor 4 | Hepatocytes | High-Throughput Screening Assays | Hypoglycemic Agents | Insulin Resistance | Mice | Peroxisome Proliferator-Activated Receptor Gamma Coactivator 1-alpha | p300-CBP Transcription Factors

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