Scopus Publication Detail
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Structure-guided development of specific pyruvate dehydrogenase kinase inhibitors targeting the ATP-binding pocketDavid T Chuang; Philipp E Scherer; Uttam K Tambar; Noelle S Williams; Richard M Wynn)
Journal of Biological Chemistry. 2014;289(7):4432-4443.Abstract
Background: Up-regulated pyruvate dehydrogenase kinase isoforms (PDKs) are associated with impaired glucose homeostasis in diabetes. Results: Novel PDK inhibitors were developed using structure-based design, which improves glucose tolerance with reduced hepatic steatosis in diet-induced obese mice. Conclusion: Obesity phenotypes are effectively treated by chemical intervention with PDK inhibitors. Significance: PDKs are potential drug targets for obesity and type 2 diabetes. © 2014 by The American Society for Biochemistry and Molecular Biology, Inc..
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