PDH (Pyruvate dehydrogenase) is a part of a mitochondrial multienzyme complex that catalyzes the oxidative decarboxylation of pyruvate and is one of the major enzymes responsible for the regulation of homeostasis of carbohydrate fuels in mammals. The enzymatic activity is regulated by a phosphorylation/dephosphorylation cycle. Phosphorylation of PDH by a specific pyruvate dehydrogenase kinase (PDK) results in inactivation. In humans, there have been four isozymes of Pyruvate Dehydrogenase Kinase that have been shown to phosphorylate these three sites: PDK1, PDK2, PDK3, and PDK4. PDK1 is the only enzyme capable of phosphorylating the 3rd serine site. When the TPP coenzyme is bound, the rates of phosphorylation by all four isozymes are drastically affected; specifically, the incorporation of phosphate groups by PDK1 into sites 2 and 3 is significantly reduced
  • DCA EI0938

    DCA是线粒体pyruvate dehydrogenase kinase (PDK) 抑制剂。

  • BAG 956 EI0524

    BAG 956是双效的 PI 3-激酶,PDK1 抑制剂。

  • JX 06 EI1418

    JX 06是活性选择性 PDK1/2/3 抑制剂。

  • BX-795 EY1632

    BX795是TBK1和PDK1双重抑制剂,IC50分别为2 nM和6 nM,比对PKA,PKC,c-Kit和GSK3β的抑制性高50倍。

  • GSK2334470 EY0632

    GSK2334470是一种新型的,高特异性的PDK1抑制剂,IC50约为10 nM,对其他AGC-激酶密切相关的蛋白无活性。

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