CATH Classification

Domain Context

CATH Clusters

Superfamily C2 domain
Functional Family Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform

Enzyme Information

2.7.1.153
Phosphatidylinositol-4,5-bisphosphate 3-kinase.
based on mapping to UniProt P48736
ATP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate = ADP + 1-phosphatidyl-1D-myo-inositol 3,4,5-trisphosphate.
-!- This enzyme also catalyzes the phosphorylation of PtdIns4P to PtdIns(3,4)P(2), and of PtdIns to PtdIns3P.
2.7.11.1
Non-specific serine/threonine protein kinase.
based on mapping to UniProt P48736
ATP + a protein = ADP + a phosphoprotein.
-!- This is a heterogeneous group of serine/threonine protein kinases that do not have an activating compound and are either non-specific or their specificity has not been analyzed to date. -!- Formerly EC 2.7.1.37 and EC 2.7.1.70.

UniProtKB Entries (1)

P48736
PK3CG_HUMAN
Homo sapiens
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform

PDB Structure

PDB 3DBS
External Links
Method X-RAY DIFFRACTION
Organism
Primary Citation
The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer
Folkes, A.J., Ahmadi, K., Alderton, W.K., Alix, S., Baker, S.J., Box, G., Chuckowree, I.S., Clarke, P.A., Depledge, P., Eccles, S.A., Friedman, L.S., Hayes, A., Hancox, T.C., Kugendradas, A., Lensun, L., Moore, P., Olivero, A.G., Pang, J., Patel, S., Pergl-Wilson, G.H., Raynaud, F.I., Robson, A., Saghir, N., Salphati, L., Sohal, S., Ultsch, M.H., Valenti, M., Wallweber, H.J.A., Wan, N.C., Wiesmann, C., Workman, P., Zhyvoloup, A., Zvelebil, M.J., Shuttleworth, S.J.
J.Med.Chem.
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