CATH Classification

Domain Context

CATH Clusters

Superfamily Phosphatidylinositol 3-kinase Catalytic Subunit; Chain A, domain 1
Functional Family Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit

Enzyme Information

2.7.1.153
Phosphatidylinositol-4,5-bisphosphate 3-kinase.
based on mapping to UniProt P42336
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 P42336
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)

P42336
PK3CA_HUMAN
Homo sapiens
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform

PDB Structure

PDB 5DXT
External Links
Method X-RAY DIFFRACTION
Organism
Primary Citation
The Rational Design of Selective Benzoxazepin Inhibitors of the alpha-Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of (S)-2-((2-(1-Isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide (GDC-0326).
Heffron, T.P., Heald, R.A., Ndubaku, C., Wei, B., Augistin, M., Do, S., Edgar, K., Eigenbrot, C., Friedman, L., Gancia, E., Jackson, P.S., Jones, G., Kolesnikov, A., Lee, L.B., Lesnick, J.D., Lewis, C., McLean, N., Mortl, M., Nonomiya, J., Pang, J., Price, S., Prior, W.W., Salphati, L., Sideris, S., Staben, S.T., Steinbacher, S., Tsui, V., Wallin, J., Sampath, D., Olivero, A.G.
J.Med.Chem.