Tclin PIK3CA Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform

Protein Summary

Description

Phosphoinositide-3-kinase (PI3K) that phosphorylates PtdIns (Phosphatidylinositol), PtdIns4P (Phosphatidylinositol 4-phosphate) and PtdIns(4,5)P2 (Phosphatidylinositol 4,5-bisphosphate) to generate phosphatidylinositol 3,4,5-trisphosphate (PIP3). PIP3 plays a key role by recruiting PH domain-containing proteins to the membrane, including AKT1 and PDPK1, activating signaling cascades involved in cell growth, survival, proliferation, motility and morphology. Participates in cellular signaling in response to various growth factors. Involved in the activation of AKT1 upon stimulation by receptor tyrosine kinases ligands such as EGF, insulin, IGF1, VEGFA and PDGF. Involved in signaling via insulin-receptor substrate (IRS) proteins. Essential in endothelial cell migration during vascular development through VEGFA signaling, possibly by regulating RhoA activity. Required for lymphatic vasculature development, possibly by binding to RAS and by activation by EGF and FGF2, but not by PDGF. Regulates invadopodia formation through the PDPK1-AKT1 pathway. Participates in cardiomyogenesis in embryonic stem cells through a AKT1 pathway. Participates in vasculogenesis in embryonic stem cells through PDK1 and protein kinase C pathway. Also has serine-protein kinase activity: phosphorylates PIK3R1 (p85alpha regulatory subunit), EIF4EBP1 and HRAS. Plays a role in the positive regulation of phagocytosis and pinocytosis (By similarity). Phosphatidylinositol 3-kinase is composed of an 85 kDa regulatory subunit and a 110 kDa catalytic subunit. The protein encoded by this gene represents the catalytic subunit, which uses ATP to phosphorylate PtdIns, PtdIns4P and PtdIns(4,5)P2. This gene has been found to be oncogenic and has been implicated in cervical cancers. A pseudogene of this gene has been defined on chromosome 22. [provided by RefSeq, Apr 2016]

Uniprot Accession IDs

• P42336
• Q14CW1
• Q99762
• PI3-kinase subunit alpha

Gene Name

• PIK3CA

Ensembl ID

• ENST00000263967
• ENSP00000263967
• ENSG00000121879

Symbol

• MCM
• CWS5
• MCAP
• PI3K
• CLAPO
• CLOVE
• MCMTC
• PI3K-alpha
• p110-alpha

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
biological term	1
hub protein	1
molecular function	1
protein domain	1
biological process	0.99

Protein Classes

PANTHER Classes

Protein / Transferase / Kinase / Phosphatidylinositol 4,5-bisphosphate 3-kinase Catalytic Subunit Alpha Isoform

DTO Classes

Protein / Kinase / Non-protein Kinase / Lipid Kinase / Pi3/pi4 Kinase Family / Phosphatidylinositol 4,5-bisphosphate 3-kinase Catalytic Subunit Alpha Isoform

IDG Development Level Summary

Tdark

These are targets about which virtually nothing is known. They do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 2854.55   (req: < 5)

Gene RIFs: 1458   (req: <= 3)

Antibodies: 649   (req: <= 50)

Tbio

These targets do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 2854.55   (req: >= 5)

Gene RIFs: 1458   (req: > 3)

Antibodies: 649   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 53

Tchem

Target has at least one ChEMBL compound with an activity cutoff of < 30 nM - AND - satisfies the preceding conditions

Active Ligands: 1742

Tclin

Target has at least one approved drug - AND - satisfies the preceding conditions

Active Drugs: 4