The PDH (pyruvate dehydrogenase) multi-enzyme complex catalyses a key regulatory step in oxidative glycolysis. Phosphorylation of the E1 subunit of the complex on serine residues results in the inactivation of enzyme activity. A family of four dedicated PDH kinase isoenzymes exists, each of which displays a distinct tissue-specific expression profile. AZD7545 is one of a series of PDH kinase inhibitors developed for the treatment of type 2 diabetes. The isoenzyme-selectivity profile of AZD7545 and related compounds is described and the consequences for their in vivo mode of action are discussed.
AZD7545 is a selective inhibitor of pyruvate dehydrogenase kinase 2
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J.A. Morrell, J. Orme, R.J. Butlin, T.E. Roche, R.M. Mayers, E. Kilgour; AZD7545 is a selective inhibitor of pyruvate dehydrogenase kinase 2. Biochem Soc Trans 1 December 2003; 31 (6): 1168–1170. doi: https://doi.org/10.1042/bst0311168
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