CATH Domain 5eymA02

CATH Classification

Level	CATH Code	Description
	1	Mainly Alpha
	1.10	Orthogonal Bundle
	1.10.510	Transferase(Phosphotransferase); domain 1
	1.10.510.10	Transferase(Phosphotransferase) domain 1

Domain Context

CATH Clusters

Superfamily	Transferase(Phosphotransferase) domain 1
Functional Family

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	5EYM
External Links	PDBSum Proteopedia
Method	X-RAY DIFFRACTION
Organism
Primary Citation	Pharmacological Profile of BI 847325, an Orally Bioavailable, ATP-Competitive Inhibitor of MEK and Aurora Kinases. Sini, P., Gurtler, U., Zahn, S.K., Baumann, C., Rudolph, D., Baumgartinger, R., Strauss, E., Haslinger, C., Tontsch-Grunt, U., Waizenegger, I.C., Solca, F., Bader, G., Zoephel, A., Treu, M., Reiser, U., Garin-Chesa, P., Boehmelt, G., Kraut, N., Quant, J., Adolf, G.R. Mol.Cancer Ther.