CATH Classification

Domain Context

CATH Clusters

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

Enzyme Information

2.7.12.2
Mitogen-activated protein kinase kinase.
based on mapping to UniProt Q02750
ATP + a protein = ADP + a phosphoprotein.
-!- A dual-specific protein kinase and requires mitogen-activated protein kinase kinase kinase (MAPKKK) for activation. -!- It is required for activation of EC 2.7.11.24. -!- Phosphorylation of MEK1 by Raf involves phosphorylation of two serine residues. -!- 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.

UniProtKB Entries (1)

Q02750
MP2K1_HUMAN
Homo sapiens
Dual specificity mitogen-activated protein kinase kinase 1

PDB Structure

PDB 4ARK
External Links
Method X-RAY DIFFRACTION
Organism
Primary Citation
Optimization of Allosteric Mek Inhibitors - Part 1: Venturing Into Unexplored Sar Territories
Hartung, I.V., Hitchcock, M., Puehler, F., Neuhaus, R., Scholz, A., Hammer, S., Petersen, K., Siemeister, G., Brittain, D., Hillig, R.C.
Bioorg.Med.Chem.Lett.