CATH Domain 5kz0A02

CATH Classification

Level	CATH Code	Description
	1	Mainly Alpha
	1.10	Orthogonal Bundle
	1.10.510	Transferase(Phosphotransferase); domain 1
	1.10.510.10	Transferase(Phosphotransferase) domain 1

Domain Context

CATH Clusters

Superfamily	Transferase(Phosphotransferase) domain 1
Functional Family	Tyrosine-protein kinase receptor

Enzyme Information

2.7.10.1

Receptor protein-tyrosine kinase.

based on mapping to UniProt Q9UM73

ATP + a [protein]-L-tyrosine = ADP + a [protein]-L-tyrosine phosphate.

-!- The receptor protein-tyrosine kinases, which can be defined as having a transmembrane domain, are a large and diverse multigene family found only in metazoans. -!- In the human genome, 58 receptor-type protein-tyrosine kinases have been identified and these are distributed into 20 subfamilies. -!- Formerly EC 2.7.1.112.

UniProtKB Entries (1)

Q9UM73

ALK_HUMAN

Homo sapiens

ALK tyrosine kinase receptor

PDB Structure

PDB	5KZ0
External Links	PDBSum Proteopedia
Method	X-RAY DIFFRACTION
Organism
Primary Citation	Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros oncogene 1 (ROS1) with preclinical brain exposure and broad-spectrum potency against ALK-resistant mutations. Johnson, T.W., Richardson, P.F., Bailey, S., Brooun, A., Burke, B.J., Collins, M.R., Cui, J.J., Deal, J.G., Deng, Y.L., Dinh, D., Engstrom, L.D., He, M., Hoffman, J., Hoffman, R.L., Huang, Q., Kania, R.S., Kath, J.C., Lam, H., Lam, J.L., Le, P.T., Lingardo, L., Liu, W., McTigue, M., Palmer, C.L., Sach, N.W., Smeal, T., Smith, G.L., Stewart, A.E., Timofeevski, S., Zhu, H., Zhu, J., Zou, H.Y., Edwards, M.P. J. Med. Chem.