CATH Classification

Domain Context

CATH Clusters

Superfamily Phosphatidylinositol 3-kinase Catalytic Subunit; Chain A, domain 4
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 5FI4
External Links
Method X-RAY DIFFRACTION
Organism
Primary Citation
Discovery of imidazo[1,2-a]-pyridine inhibitors of pan-PI3 kinases that are efficacious in a mouse xenograft model.
Han, W., Menezes, D.L., Xu, Y., Knapp, M.S., Elling, R., Burger, M.T., Ni, Z.J., Smith, A., Lan, J., Williams, T.E., Verhagen, J., Huh, K., Merritt, H., Chan, J., Kaufman, S., Voliva, C.F., Pecchi, S.
Bioorg.Med.Chem.Lett.