CATH Domain 6gqkB01

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

2.7.10.1

Receptor protein-tyrosine kinase.

based on mapping to UniProt P10721

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)

P10721

KIT_HUMAN

Homo sapiens

Mast/stem cell growth factor receptor Kit

PDB Structure

PDB	6GQK
External Links	PDBSum Proteopedia
Method	X-RAY DIFFRACTION
Organism
Primary Citation	Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors. Kettle, J.G., Anjum, R., Barry, E., Bhavsar, D., Brown, C., Boyd, S., Campbell, A., Goldberg, K., Grondine, M., Guichard, S., Hardy, C.J., Hunt, T., Jones, R.D.O., Li, X., Moleva, O., Ogg, D., Overman, R.C., Packer, M.J., Pearson, S., Schimpl, M., Shao, W., Smith, A., Smith, J.M., Stead, D., Stokes, S., Tucker, M., Ye, Y. J. Med. Chem.