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 3I5Z
External Links
Method X-RAY DIFFRACTION
Organism
Primary Citation
Structure-guided design of potent and selective pyrimidylpyrrole inhibitors of extracellular signal-regulated kinase (ERK) using conformational control.
Aronov, A.M., Tang, Q., Martinez-Botella, G., Bemis, G.W., Cao, J., Chen, G., Ewing, N.P., Ford, P.J., Germann, U.A., Green, J., Hale, M.R., Jacobs, M., Janetka, J.W., Maltais, F., Markland, W., Namchuk, M.N., Nanthakumar, S., Poondru, S., Straub, J., ter Haar, E., Xie, X.
J.Med.Chem.