Structure-guided Development of Specific Pyruvate Dehydrogenase Kinase Inhibitors Targeting the ATP-binding Pocket

Pyruvate dehydrogenase kinase isoforms (PDKs 1–4) negatively regulate activity of the mitochondrial pyruvate dehydrogenase complex by reversible phosphorylation. PDK isoforms are up-regulated in obesity, diabetes, heart failure, and cancer and are potential therapeutic targets for these important hu...

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Veröffentlicht in:	J. Biol. Chem 2014-02, Vol.289 (7), p.4432-4443
Hauptverfasser:	Tso, Shih-Chia, Qi, Xiangbing, Gui, Wen-Jun, Wu, Cheng-Yang, Chuang, Jacinta L., Wernstedt-Asterholm, Ingrid, Morlock, Lorraine K., Owens, Kyle R., Scherer, Philipp E., Williams, Noelle S., Tambar, Uttam K., Wynn, R. Max, Chuang, David T.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Diabetes Diabetes Mellitus, Type 2 - drug therapy Diabetes Mellitus, Type 2 - enzymology Diabetes Mellitus, Type 2 - genetics Diabetes Mellitus, Type 2 - pathology Drug Delivery Systems Drug Design Drug Development Enzyme Inhibitors Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology Fatty Liver - drug therapy Fatty Liver - enzymology Fatty Liver - genetics Fatty Liver - pathology Glucose Metabolism Hepatic Steatosis HSP90 Heat-Shock Proteins Humans Isoenzymes - antagonists & inhibitors Isoenzymes - chemistry Isoenzymes - genetics Isoenzymes - metabolism Isoindoles - chemistry Isoindoles - pharmacology Male Metabolism Mice Mice, Obese Mitochondrial Protein Kinase Obesity - drug therapy Obesity - enzymology Obesity - genetics Obesity - pathology Protein-Serine-Threonine Kinases - antagonists & inhibitors Protein-Serine-Threonine Kinases - chemistry Protein-Serine-Threonine Kinases - genetics Protein-Serine-Threonine Kinases - metabolism Pyruvate Dehydrogenase Acetyl-Transferring Kinase Pyruvate Dehydrogenase Complex Pyruvate Dehydrogenase Kinase Structure-based Inhibitor Design Sulfones - chemistry Sulfones - pharmacology
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