CATH Domain 4o6eA01

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	Mitogen-activated protein kinase

Enzyme Information

2.7.11.24

Mitogen-activated protein kinase.

based on mapping to UniProt P28482

ATP + a protein = ADP + a phosphoprotein.

-!- Phosphorylation of specific tyrosine and threonine residues in the activation loop of this enzyme by EC 2.7.12.2 is necessary for enzyme activation. -!- Once activated, the enzyme phosphorylates target substrates on serine or threonine residues followed by a proline. -!- A distinguishing feature of all MAPKs is the conserved sequence Thr- Xaa-Tyr (TXY). -!- 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. -!- Formerly EC 2.7.1.37.

UniProtKB Entries (1)

P28482

MK01_HUMAN

Homo sapiens

Mitogen-activated protein kinase 1

PDB Structure

PDB	4O6E
External Links	PDBSum Proteopedia
Method	X-RAY DIFFRACTION
Organism
Primary Citation	Discovery of 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine inhibitors of Erk2. Blake, J.F., Gaudino, J.J., De Meese, J., Mohr, P., Chicarelli, M., Tian, H., Garrey, R., Thomas, A., Siedem, C.S., Welch, M.B., Kolakowski, G., Kaus, R., Burkard, M., Martinson, M., Chen, H., Dean, B., Dudley, D.A., Gould, S.E., Pacheco, P., Shahidi-Latham, S., Wang, W., West, K., Yin, J., Moffat, J., Schwarz, J.B. Bioorg.Med.Chem.Lett.