CATH Classification

Domain Context

CATH Clusters

Superfamily Histidine kinase-like ATPase, C-terminal domain
Functional Family Mitochondrial pyruvate dehydrogenase kinase isoform 2

Enzyme Information

2.7.11.2
[Pyruvate dehydrogenase (acetyl-transferring)] kinase.
based on mapping to UniProt Q15119
ATP + [pyruvate dehydrogenase (acetyl-transferring)] = ADP + [pyruvate dehydrogenase (acetyl-transferring)] phosphate.
-!- Has no activating compound but is specific for its substrate. -!- A mitochondrial enzyme associated with the pyruvate dehydrogenase complex in mammals. -!- Phosphorylation inactivates EC 1.2.4.1. -!- Formerly EC 2.7.1.99.

UniProtKB Entries (1)

Q15119
PDK2_HUMAN
Homo sapiens
[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 2, mitochondrial

PDB Structure

PDB 4V26
External Links
Method X-RAY DIFFRACTION
Organism
Primary Citation
VER-246608, a novel pan-isoform ATP competitive inhibitor of pyruvate dehydrogenase kinase, disrupts Warburg metabolism and induces context-dependent cytostasis in cancer cells.
Moore, J.D., Staniszewska, A., Shaw, T., D'Alessandro, J., Davis, B., Surgenor, A., Baker, L., Matassova, N., Murray, J., Macias, A., Brough, P., Wood, M., Mahon, P.C.
Oncotarget