Target intelligence / Profile preview

Pyruvate Dehydrogenase Kinase (PDK)

Target: PDK
Molecular classification: Enzyme, Protein Kinase, Serine/Threonine Kinase

Overview

Pyruvate dehydrogenase kinase (PDK) is a mitochondrial enzyme that regulates the activity of the pyruvate dehydrogenase complex (PDC) by phosphorylating and inactivating pyruvate dehydrogenase. This controls whether pyruvate is oxidized to acetyl-CoA or diverted toward other metabolic pathways. There are four main mammalian isoforms: PDK1–4. Altered expression or activation of specific PDK isoforms has been implicated in various diseases, including cancer, diabetes, and heart disease. PDKs are considered promising anticancer drug targets.

Mechanism of action

Small molecule inhibitors targeting different PDK isoforms

Biological functions

Regulation of metabolismCellular energy homeostasisRegulation of Pyruvate Dehydrogenase Complex (PDC) activity

Disease associations

CancerDiabetes Mellitus Type IIHeart FailureImmunometabolism

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