Allosteric Coupling in Pyruvate Dehydrogenase Kinase 2
نویسندگان
چکیده
منابع مشابه
Pyruvate Dehydrogenase Kinase 4
OBJECTIVE Pyruvate dehydrogenase complex (PDC) serves as the metabolic switch between glucose and fatty acid utilization. PDC activity is inhibited by PDC kinase (PDK). PDC shares the same substrate, i.e., pyruvate, as glyceroneogenesis, a pathway controlling fatty acid release from white adipose tissue (WAT). Thiazolidinediones activate glyceroneogenesis. We studied the regulation by rosiglita...
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The pyruvate dehydrogenase (E1) and acetyltransferase (E2) components of pig heart and ox kidney pyruvate dehydrogenase (PDH) complex were separated and purified. The E1 component was phosphorylated (alpha-chain) and inactivated by MgATP. Phosphorylation was mainly confined to site 1. Addition of E2 accelerated phosphorylation of all three sites in E1 alpha and inactivation of E1. On the basis ...
متن کاملAllosteric properties of skeletal muscle pyruvate kinase.
The phenylalanine inhibition of skeletal muscle pyruvate kinase has been further studied. Even at high levels of the inhibitor the plots of reaction rates as a function of phosphoenolpyruvate concentration give hyperbolic curves; the inhibition by phenylalanine is of the mixed type. The enzyme exhibits a homotropic cooperative effect with respect to this inhibitor. This property is strongly dep...
متن کاملAZD7545 is a selective inhibitor of pyruvate dehydrogenase kinase 2.
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 in...
متن کاملEvidence that rat liver pyruvate dehydrogenase kinase activator protein is a pyruvate dehydrogenase kinase.
It is shown here that rat liver pyruvate dehydrogenase (PDH) kinase activator protein (KAP) catalyses ATP-dependent inactivation and [32P]phosphorylation of pig heart PDHE1 and of yeast (Saccharomyces cerevisiae) PDH complex devoid of PDH kinase activity, that fluorosulphonylbenzoyladenosine inactivates rat liver KAP and the intrinsic PDH kinase of rat liver PDH complex, and that KAP, like PDH ...
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ژورنال
عنوان ژورنال: Biochemistry
سال: 2008
ISSN: 0006-2960,1520-4995
DOI: 10.1021/bi800631h