Tchem PIK3R1 Phosphatidylinositol 3-kinase regulatory subunit alpha

Protein Summary

Description

Binds to activated (phosphorylated) protein-Tyr kinases, through its SH2 domain, and acts as an adapter, mediating the association of the p110 catalytic unit to the plasma membrane. Necessary for the insulin-stimulated increase in glucose uptake and glycogen synthesis in insulin-sensitive tissues. Plays an important role in signaling in response to FGFR1, FGFR2, FGFR3, FGFR4, KITLG/SCF, KIT, PDGFRA and PDGFRB. Likewise, plays a role in ITGB2 signaling (PubMed:17626883, PubMed:19805105, PubMed:7518429). Modulates the cellular response to ER stress by promoting nuclear translocation of XBP1 isoform 2 in a ER stress- and/or insulin-dependent manner during metabolic overloading in the liver and hence plays a role in glucose tolerance improvement (PubMed:20348923). Phosphatidylinositol 3-kinase phosphorylates the inositol ring of phosphatidylinositol at the 3-prime position. The enzyme comprises a 110 kD catalytic subunit and a regulatory subunit of either 85, 55, or 50 kD. This gene encodes the 85 kD regulatory subunit. Phosphatidylinositol 3-kinase plays an important role in the metabolic actions of insulin, and a mutation in this gene has been associated with insulin resistance. Alternative splicing of this gene results in four transcript variants encoding different isoforms. [provided by RefSeq, Jun 2011]

Uniprot Accession IDs

• P27986
• B3KT19
• D3DWA0
• E7EX19
• Q15747
• Q4VBZ7
• Q53EM6
• Q8IXA2
• Q8N1C5
• PI3-kinase regulatory subunit alpha

Gene Name

• PIK3R1

Ensembl ID

• ENST00000320694
• ENSP00000323512
• ENSG00000145675
• ENST00000336483
• ENSP00000338554
• ENST00000521381
• ENSP00000428056
• ENST00000521657
• ENSP00000429277
• ENST00000523872
• ENSP00000430098

Symbol

• GRB1
• p85
• AGM7
• GRB1
• IMD36
• p85-ALPHA

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
biological process	1
hub protein	1
interacting protein	1
transcription factor perturbation	1
kinase	0.99

Protein Classes

PANTHER Classes

Protein / Enzyme Modulator / Kinase Modulator / Phosphatidylinositol 3-kinase Regulatory Subunit Alpha

DTO Classes

Protein / Kinase / Non-protein Kinase / Lipid Kinase / Pi3k P85 Subunit Family / Phosphatidylinositol 3-kinase Regulatory 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: 627.55   (req: < 5)

Gene RIFs: 178   (req: <= 3)

Antibodies: 994   (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: 627.55   (req: >= 5)

Gene RIFs: 178   (req: > 3)

Antibodies: 994   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 62

Tchem

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

Active Ligands: 4

Tclin

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

Active Drug: 0