CATH Classification

Domain Context

CATH Clusters

Superfamily Phosphorylase Kinase; domain 1
Functional Family Mitogen-activated protein kinase

Enzyme Information

2.7.11.24
Mitogen-activated protein kinase.
based on mapping to UniProt P28482
ATP + a protein = ADP + a phosphoprotein.
-!- Phosphorylation of specific tyrosine and threonine residues in the activation loop of this enzyme by EC 2.7.12.2 is necessary for enzyme activation. -!- Once activated, the enzyme phosphorylates target substrates on serine or threonine residues followed by a proline. -!- A distinguishing feature of all MAPKs is the conserved sequence Thr- Xaa-Tyr (TXY). -!- Mitogen-activated protein kinase (MAPK) signal transduction pathways are among the most widespread mechanisms of cellular regulation. -!- Mammalian MAPK pathways can be recruited by a wide variety of stimuli including hormones (e.g. insulin and growth hormone), mitogens (e.g. epidermal growth factor and platelet-derived growth factor), vasoactive peptides (e.g. angiotensin-II and endothelin), inflammatory cytokines of the tumor necrosis factor (TNF) family and environmental stresses such as osmotic shock, ionizing radiation and ischemeic injury. -!- Formerly EC 2.7.1.37.

UniProtKB Entries (1)

P28482
MK01_HUMAN
Homo sapiens
Mitogen-activated protein kinase 1

PDB Structure

PDB 4XJ0
External Links
Method X-RAY DIFFRACTION
Organism
Primary Citation
Discovery of highly potent, selective, and efficacious small molecule inhibitors of ERK1/2.
Ren, L., Grina, J., Moreno, D., Blake, J.F., Gaudino, J.J., Garrey, R., Metcalf, A.T., Burkard, M., Martinson, M., Rasor, K., Chen, H., Dean, B., Gould, S.E., Pacheco, P., Shahidi-Latham, S., Yin, J., West, K., Wang, W., Moffat, J.G., Schwarz, J.B.
J.Med.Chem.