Overview:

PDHK1 or Pyruvate Dehydrogenase Kinase 1 is a member of the PDHK family that phosphorylate and inactivate the Pyruvate Dehydrogenase (PDH) (1). PDH is 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. PDHK1 is an important regulator of PDH in clonal β-cells and the activity of PDHK1 and PDH are important for efficient metabolic coupling. Maintaining low PDHK1 expression/activity and keeping PDH in a dephosphorylated and active state, is important for β -cells to achieve the metabolic flux rates necessary for maximal glucose-stimulated insulin secretion (2).

References:

1. Gudi, R. et al: Diversity of the pyruvate dehydrogenase kinase gene family in humans. J. Biol. Chem. 270: 28989-28994, 1995.

2. Krus, U. et al: Pyruvate dehydrogenase kinase 1 controls mitochondrial metabolism and insulin secretion in INS-1 832/13 clonal beta-cells. Biochem J. 2010 Jul 1;429(1):205-13.