PDK1 Human
Description
Product Specs
Product Science Overview
Pyruvate Dehydrogenase Kinase Isozyme 1 (PDK1) is a crucial enzyme in the regulation of glucose metabolism and energy homeostasis in mammals. This enzyme is part of the pyruvate dehydrogenase complex (PDC), a mitochondrial multienzyme complex responsible for the oxidative decarboxylation of pyruvate, a key step in cellular respiration.
PDK1 is a mitochondrial enzyme that phosphorylates and inactivates the pyruvate dehydrogenase complex by targeting the E1 alpha subunit . This phosphorylation prevents the conversion of pyruvate to acetyl-CoA, thereby regulating the flow of carbon through the tricarboxylic acid (TCA) cycle and influencing the balance between glucose and fatty acid metabolism .
The enzyme is encoded by the PDK1 gene located on chromosome 2 in humans . The mature protein consists of 407 amino acids and forms an active dimeric structure . The catalytic domain of PDK1 is essential for its kinase activity and regulation of its substrates .
PDK1 plays a pivotal role in cellular responses to metabolic stress and hypoxia. By inhibiting the pyruvate dehydrogenase complex, PDK1 reduces aerobic respiration and promotes anaerobic glycolysis, which is crucial for cell survival under low oxygen conditions . This mechanism is particularly important in rapidly proliferating cells, such as cancer cells, which often experience hypoxic environments .
Alterations in PDK1 activity have been associated with various metabolic disorders and diseases. Overexpression of PDK1 has been observed in certain cancers, where it contributes to the Warburg effect, a metabolic shift favoring glycolysis over oxidative phosphorylation even in the presence of oxygen . Inhibiting PDK1 activity has been proposed as a therapeutic strategy for targeting cancer metabolism .
Additionally, PDK1 is involved in the regulation of glucose homeostasis and insulin sensitivity. Dysregulation of PDK1 activity can lead to metabolic conditions such as diabetes and obesity .
Human recombinant PDK1 is produced using recombinant DNA technology, which involves cloning the PDK1 gene into an expression vector and introducing it into a host cell for protein production. This recombinant enzyme is used in various research applications to study its function, regulation, and potential as a therapeutic target .
