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Updated: Aug 14, 2026

Assaying the Kinase Activity of LRRK2 in vitro
Published on: January 18, 2012
AZD7545 is a selective inhibitor of pyruvate dehydrogenase kinase 2
J A Morrell1, J Orme, R J Butlin
1AstraZeneca, Alderley Park, Macclesfield, Cheshire, SK10 4TG, U.K.
Abstract:
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.
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