Tchem PIK3C2A Phosphatidylinositol 4-phosphate 3-kinase C2 domain-containing subunit alpha

Protein Summary

Description

Generates phosphatidylinositol 3-phosphate (PtdIns3P) and phosphatidylinositol 3,4-bisphosphate (PtdIns(3,4)P2) that act as second messengers. Has a role in several intracellular trafficking events. Functions in insulin signaling and secretion. Required for translocation of the glucose transporter SLC2A4/GLUT4 to the plasma membrane and glucose uptake in response to insulin-mediated RHOQ activation. Regulates insulin secretion through two different mechanisms: involved in glucose-induced insulin secretion downstream of insulin receptor in a pathway that involves AKT1 activation and TBC1D4/AS160 phosphorylation, and participates in the late step of insulin granule exocytosis probably in insulin granule fusion. Synthesizes PtdIns3P in response to insulin signaling. Functions in clathrin-coated endocytic vesicle formation and distribution. Regulates dynamin-independent endocytosis, probably by recruiting EEA1 to internalizing vesicles. In neurosecretory cells synthesizes PtdIns3P on large dense core vesicles. Participates in calcium induced contraction of vascular smooth muscle by regulating myosin light chain (MLC) phosphorylation through a mechanism involving Rho kinase-dependent phosphorylation of the MLCP-regulatory subunit MYPT1. May play a role in the EGF signaling cascade. May be involved in mitosis and UV-induced damage response. Required for maintenance of normal renal structure and function by supporting normal podocyte function. The protein encoded by this gene belongs to the phosphoinositide 3-kinase (PI3K) family. PI3-kinases play roles in signaling pathways involved in cell proliferation, oncogenic transformation, cell survival, cell migration, and intracellular protein trafficking. This protein contains a lipid kinase catalytic domain as well as a C-terminal C2 domain, a characteristic of class II PI3-kinases. C2 domains act as calcium-dependent phospholipid binding motifs that mediate translocation of proteins to membranes, and may also mediate protein-protein interactions. The PI3-kinase activity of this protein is not sensitive to nanomolar levels of the inhibitor wortmanin. This protein was shown to be able to be activated by insulin and may be involved in integrin-dependent signaling. [provided by RefSeq, Jul 2008]

Uniprot Accession IDs

• O00443
• B0LPH2
• B4E2G4
• Q14CQ9
• PI3K-C2-alpha

Gene Name

• PIK3C2A

Ensembl ID

• ENST00000265970
• ENSP00000265970
• ENSG00000011405

Symbol

• CPK
• PI3-K-C2A
• PI3K-C2alpha
• PI3K-C2-alpha
• PI3-K-C2(ALPHA)

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
protein domain	1
drug perturbation	0.96
molecular function	0.96
kinase perturbation	0.93
co-expressed gene	0.89

Protein Classes

PANTHER Classes

Protein / Transferase / Kinase / Phosphatidylinositol 4-phosphate 3-kinase C2 Domain-containing Subunit Alpha

DTO Classes

Protein / Kinase / Non-protein Kinase / Lipid Kinase / Phosphoinositide 3-kinase (Pi3k) Family / Phosphatidylinositol 4-phosphate 3-kinase C2 Domain-containing Subunit Alpha

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: 5273.98   (req: < 5)

Gene RIFs: 39   (req: <= 3)

Antibodies: 594   (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: 5273.98   (req: >= 5)

Gene RIFs: 39   (req: > 3)

Antibodies: 594   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 20

Tchem

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

Active Ligands: 2

Tclin

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

Active Drug: 0