CATH Classification

Domain Context

CATH Clusters

Superfamily Transferase(Phosphotransferase) domain 1
Functional Family Receptor protein-tyrosine kinase

Enzyme Information

2.7.10.1
Receptor protein-tyrosine kinase.
based on mapping to UniProt P00533
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)

P00533
EGFR_HUMAN
Homo sapiens
Epidermal growth factor receptor

PDB Structure

PDB 5HG8
External Links
Method X-RAY DIFFRACTION
Organism
Primary Citation
Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants.
Cheng, H., Nair, S.K., Murray, B.W., Almaden, C., Bailey, S., Baxi, S., Behenna, D., Cho-Schultz, S., Dalvie, D., Dinh, D.M., Edwards, M.P., Feng, J.L., Ferre, R.A., Gajiwala, K.S., Hemkens, M.D., Jackson-Fisher, A., Jalaie, M., Johnson, T.O., Kania, R.S., Kephart, S., Lafontaine, J., Lunney, B., Liu, K.K., Liu, Z., Matthews, J., Nagata, A., Niessen, S., Ornelas, M.A., Orr, S.T., Pairish, M., Planken, S., Ren, S., Richter, D., Ryan, K., Sach, N., Shen, H., Smeal, T., Solowiej, J., Sutton, S., Tran, K., Tseng, E., Vernier, W., Walls, M., Wang, S., Weinrich, S.L., Xin, S., Xu, H., Yin, M.J., Zientek, M., Zhou, R., Kath, J.C.
J.Med.Chem.