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TargetEnzymes

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform

Named enzymes, including the metabolising cytochromes and the monoamine oxidases.

Measurements
2
Compounds
1
Binding constants
0
Median pX
—

I · Identity

What this target is

Its function as UniProt states it, where in a cell the protein is found, and which cell types and tissues transcribe its gene.

Protein

PK3CG_HUMANPIK3CGHomo sapiens

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform

Phosphoinositide-3-kinase (PI3K) that phosphorylates 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. Links G protein coupled receptor activation to PIP3 production. Involved in immune, inflammatory and allergic responses. Modulates leukocyte chemotaxis to inflammatory sites and in response to chemoattractant agents. May control leukocyte polarization and migration by regulating the spatial accumulation of PIP3 and by regulating the organization of F-actin formation and integrin-based adhesion at the leading edge. Controls motility of dendritic cells. Together with PIK3CD is involved in natural killer (NK) cell development and migration towards the sites of inflammation. Participates in T-lymphocyte migration. Regulates T-lymphocyte proliferation, activation, and cytokine production. Together with PIK3CD participates in T-lymphocyte development. Required for B-lymphocyte development and signaling. Together with PIK3CD participates in neutrophil respiratory burst. Together with PIK3CD is involved in neutrophil chemotaxis and extravasation. Together with PIK3CB promotes platelet aggregation and thrombosis. Regulates alpha-IIb/beta-3 integrins (ITGA2B/ ITGB3) adhesive function in platelets downstream of P2Y12 through a lipid kinase activity-independent mechanism. May have also a lipid kinase activity-dependent function in platelet aggregation. Involved in endothelial progenitor cell migration. Negative regulator of cardiac contractility. Modulates cardiac contractility by anchoring protein kinase A (PKA) and PDE3B activation, reducing cAMP levels. Regulates cardiac contractility also by promoting beta-adrenergic receptor internalization by binding to GRK2 and by non-muscle tropomyosin phosphorylation. Also has serine/threonine protein kinase activity: both lipid and protein kinase activities are required for beta-adrenergic receptor endocytosis. May also have a scaffolding role in modulating cardiac contractility. Contributes to cardiac hypertrophy under pathological stress. Through simultaneous binding of PDE3B to RAPGEF3 and PIK3R6 is assembled in a signaling complex in which the PI3K gamma complex is activated by RAPGEF3 and which is involved in angiogenesis. In neutrophils, participates in a phospholipase C-activating N-formyl peptide-activated GPCR (G protein-coupled receptor) signaling pathway downstream of RASGRP4-mediated Ras-activation, to promote neutrophil functional responses (By similarity)

Quoted from UniProt’s FUNCTION annotation for P48736 (reviewed).

What it acts with

STRING’s highest-confidence human functional partners. The combined score mixes several kinds of evidence, so each channel is shown separately — a partner supported by experiment is a different claim from one supported only by text mining, and for a receptor this is where its coupling appears as evidence rather than as assertion.

PartnerCombinedExperimentDatabaseText mining
PIK3R30.9990.3130.9140.991
PIK3R10.9990.4920.9140.987
PIK3R60.9990.3220.9000.988
PIK3R50.9990.9690.9000.998
PIK3R20.9990.3130.9140.991
HRAS0.9980.9500.9000.626
PIK3CB0.9970.0450.9000.976
PIK3CA0.9970.0450.9000.973
AKT10.9940.0980.9000.947
PIK3CD0.9940.2960.9000.923

Where it sits in the cell

  • Plasma membrane
  • Cytosoladditional

Human Protein Atlas, by antibody immunofluorescence in cell lines — a different assay from the expression figures below, which are RNA.

UniProt, curated Cytoplasm · Cell membrane

Expression by cell type

Single cell type RNA, the 10 highest of those the Human Protein Atlas reports for this gene. Transcript, not protein, and a cell type rather than a tissue.

  • Tuft cells564.9 nCPM
  • Neutrophil progenitors331.3 nCPM
  • Neutrophils326.7 nCPM
  • Plasma cells146.5 nCPM
  • pDCs112.3 nCPM
  • Monocyte progenitors82.7 nCPM
  • Microglia72.4 nCPM
  • NK-cells66.8 nCPM
  • B-cells66.2 nCPM
  • monocytes64.6 nCPM

Expression by tissue

The tissues this gene is enriched in, by consensus RNA. A tissue absent from this list is one the Atlas does not call specific for this gene, which is not the same as absent from it.

  • bone marrow41.2 nTPM
  • lymphoid tissue18.4 nTPM

IV · Evidence

Every measurement at this target

Each row links to the ChEMBL assay it came from.

Other measurements 2

Everything else ChEMBL recorded for this compound — percentage inhibition, efficacy, half-life, cytotoxicity. Reported in the assay's own units, which is why no value is converted here.

TargetClassTypeValue (nM)pXOrganismAssay
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoformEnzymesActivity— no normalized value— value does not convert to pXHomo sapiensCHEMBL4344408
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoformEnzymesInhibition— no normalized value— value does not convert to pXHomo sapiensCHEMBL5548732