CATH Domain 4an2A01

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	4AN2
External Links	PDBSum Proteopedia
Method	X-RAY DIFFRACTION
Organism
Primary Citation	Novel Carboxamide-Based Allosteric Mek Inhibitors: Discovery and Optimization Efforts Toward Xl518 (Gdc-0973) Rice, K.D., Aay, N., Anand, N.K., Blazey, C.M., Bowles, O.J., Bussenius, J., Costanzo, S., Curtis, J.K., Defina, S.C., Dubenko, L., Engst, S., Joshi, A.A., Kennedy, A.R., Kim, A.I., Koltun, E.S., Lougheed, J.C., Manalo, J.C.L., Martini, J.F., Nuss, J.M., Peto, C.J., Tsang, T.H., Yu, P., Johnston, S. Acs Med.Chem.Lett.