CATH Domain 5dxhA05

CATH Classification

Level	CATH Code	Description
	1	Mainly Alpha
	1.10	Orthogonal Bundle
	1.10.1070	Phosphatidylinositol 3-kinase Catalytic Subunit; Chain A, Domain 5
	1.10.1070.11	Phosphatidylinositol 3-/4-kinase, catalytic domain

Domain Context

CATH Clusters

Superfamily	Phosphatidylinositol 3-/4-kinase, catalytic domain
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 (2)

P23727	P85A_BOVIN Bos taurus Phosphatidylinositol 3-kinase regulatory subunit alpha
P42336	PK3CA_HUMAN Homo sapiens Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform

PDB Structure

PDB	5DXH
External Links	PDBSum Proteopedia
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.