CATH Domain 3os3A01

CATH Classification

Level	CATH Code	Description
	3	Alpha Beta
	3.30	2-Layer Sandwich
	3.30.200	Phosphorylase Kinase; domain 1
	3.30.200.20	Phosphorylase Kinase; domain 1

Domain Context

CATH Clusters

Superfamily	Phosphorylase Kinase; 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	3OS3
External Links	PDBSum Proteopedia
Method	X-RAY DIFFRACTION
Organism
Primary Citation	Design and synthesis of novel allosteric MEK inhibitor CH4987655 as an orally available anticancer agent. Isshiki, Y., Kohchi, Y., Iikura, H., Matsubara, Y., Asoh, K., Murata, T., Kohchi, M., Mizuguchi, E., Tsujii, S., Hattori, K., Miura, T., Yoshimura, Y., Aida, S., Miwa, M., Saitoh, R., Murao, N., Okabe, H., Belunis, C., Janson, C., Lukacs, C., Schuck, V., Shimma, N. Bioorg.Med.Chem.Lett.