CATH Classification

Domain Context

CATH Clusters

Superfamily Transferase(Phosphotransferase) domain 1
Functional Family Mitogen-activated protein kinase 1

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 4ZZO
External Links
Method X-RAY DIFFRACTION
Organism
Primary Citation
Structure-Guided Design of Highly Selective and Potent Covalent Inhibitors of Erk1/2.
Ward, R.A., Colclough, N., Challinor, M., Debreczeni, J., Eckersley, K., Fairley, G., Feron, L., Flemington, V., Graham, M.A., Greenwood, R., Hopcroft, P., Howard, T.D., James, M., Jones, C.D., Jones, C.R., Renshaw, J., Roberts, K., Snow, L., Tonge, M., Yeung, K.
J.Med.Chem.