CATH Domain 4u81A01

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	4U81
External Links	PDBSum Proteopedia
Method	X-RAY DIFFRACTION
Organism
Primary Citation	Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479. Robarge, K.D., Lee, W., Eigenbrot, C., Ultsch, M., Wiesmann, C., Heald, R., Price, S., Hewitt, J., Jackson, P., Savy, P., Burton, B., Choo, E.F., Pang, J., Boggs, J., Yang, A., Yang, X., Baumgardner, M. Bioorg.Med.Chem.Lett.