CATH Classification

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 (1)

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

PDB Structure

PDB 4JPS
External Links
Method X-RAY DIFFRACTION
Organism
Primary Citation
Discovery of NVP-BYL719 a potent and selective phosphatidylinositol-3 kinase alpha inhibitor selected for clinical evaluation.
Furet, P., Guagnano, V., Fairhurst, R.A., Imbach-Weese, P., Bruce, I., Knapp, M., Fritsch, C., Blasco, F., Blanz, J., Aichholz, R., Hamon, J., Fabbro, D., Caravatti, G.
Bioorg.Med.Chem.Lett.