CATH Domain 6g9nA01

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	6G9N
External Links	PDBSum Proteopedia
Method	X-RAY DIFFRACTION
Organism
Primary Citation	Fragment-Based Discovery of a Potent, Orally Bioavailable Inhibitor That Modulates the Phosphorylation and Catalytic Activity of ERK1/2. Heightman, T.D., Berdini, V., Braithwaite, H., Buck, I.M., Cassidy, M., Castro, J., Courtin, A., Day, J.E.H., East, C., Fazal, L., Graham, B., Griffiths-Jones, C.M., Lyons, J.F., Martins, V., Muench, S., Munck, J.M., Norton, D., O'Reilly, M., Palmer, N., Pathuri, P., Reader, M., Rees, D.C., Rich, S.J., Richardson, C., Saini, H., Thompson, N.T., Wallis, N.G., Walton, H., Wilsher, N.E., Woolford, A.J., Cooke, M., Cousin, D., Onions, S., Shannon, J., Watts, J., Murray, C.W. J. Med. Chem.