CATH Classification

Domain Context

CATH Clusters

Superfamily Phosphorylase Kinase; domain 1
Functional Family Mitogen-activated protein kinase 14

Enzyme Information

2.7.11.24
Mitogen-activated protein kinase.
based on mapping to UniProt Q16539
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)

Q16539
MK14_HUMAN
Homo sapiens
Mitogen-activated protein kinase 14

PDB Structure

PDB 3S4Q
External Links
Method X-RAY DIFFRACTION
Organism
Primary Citation
Discovery of pyrrolo[2,1-f][1,2,4]triazine C6-ketones as potent, orally active p38α MAP kinase inhibitors.
Dyckman, A.J., Li, T., Pitt, S., Zhang, R., Shen, D.R., McIntyre, K.W., Gillooly, K.M., Shuster, D.J., Doweyko, A.M., Sack, J.S., Kish, K., Kiefer, S.E., Newitt, J.A., Zhang, H., Marathe, P.H., McKinnon, M., Barrish, J.C., Dodd, J.H., Schieven, G.L., Leftheris, K.
Bioorg.Med.Chem.Lett.