PIK3CG
PIK3CG (Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform) is a protein kinase, an enzyme that switches other proteins on by adding phosphate groups. The public catalogues list it as a drug target, and an approved or late-stage drug is recorded against it. Tied to Non-Hodgkin lymphoma, Leukaemia, Acute lymphoblastic leukaemia and 2 more.
Overview
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 signalling cascades involved in cell growth, survival, proliferation, motility and morphology. Links G protein coupled receptor activation to PIP3 production.
Open Targets scores its association with cancer at 0.54 (direct and indirect evidence; datatypes clinical 0.67, affected pathway 0.61, literature 0.99, genetic association 0.30, somatic mutation 0.23).
- Target · the protein and the cell it sits on
- Drug · antibody, small molecule, cell or radioligand
- Effect · signal, damage or kill
In plain words · PIK3CG (Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform) is a protein kinase, an enzyme that switches other proteins on by adding phosphate groups. The public catalogues list it as a drug target, and an approved or late-stage drug is recorded against it. Tied to Non-Hodgkin lymphoma, Leukaemia, Acute lymphoblastic leukaemia and 2 more.
- 1 · What it is
PIK3CG (Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform) is a protein kinase, an enzyme that switches other proteins on by adding phosphate groups. The public catalogues list it as a drug target, and an approved or late-stage drug is recorded against it. Tied to Non-Hodgkin lymphoma, Leukaemia, Acute lymphoblastic leukaemia and 2 more.
- 2 · What goes wrong in cancer
Phosphoinositide-3-kinase (PI3K) that phosphorylates PtdIns(4,5)P2 (Phosphatidylinositol 4,5-bisphosphate) to generate phosphatidylinositol 3,4,5-trisphosphate (PIP3).
- 3 · How drugs use it
No product in this corpus aims at PIK3CG yet. Kinases are switched on by binding ATP inside the cell, so most drugs are small molecules shaped to plug that ATP pocket.
External identifiers
Sources: HGNC HGNC:8978 (approved symbol, name, aliases, locus and cross-references (hgnc_complete_set.txt)); UniProt P48736 (protein name, function text, keywords and locations (REST API)); Open Targets ENSG00000105851 (association with cancer (MONDO_0004992) 0.54; per-cancer scores at or above 0.5: acute lymphoblastic leukaemia 0.58, B-cell chronic lymphocytic leukaemia 0.57, non-Hodgkin lymphoma 0.61, follicular lymphoma 0.55, leukaemia 0.58 (GraphQL API, CC0))
Biology
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 signalling 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 polarisation and migration by regulating the spatial accumulation of PIP3 and by regulating the organisation of F-actin formation and integrin-based adhesion at the leading edge. Location: Cytoplasm; Cell membrane (UniProt). Locus 7q22.3 (HGNC).
- Non-Hodgkin lymphoma: Open Targets association 0.61 with non-Hodgkin lymphoma (MONDO_0018908)
- Leukaemia: Open Targets association 0.58 with leukaemia (MONDO_0005059)
- Acute lymphoblastic leukaemia: Open Targets association 0.58 with acute lymphoblastic leukaemia (MONDO_0004967)
- Chronic lymphocytic leukaemia: Open Targets association 0.57 with B-cell chronic lymphocytic leukaemia (MONDO_0004948)
- Follicular lymphoma: Open Targets association 0.55 with follicular lymphoma (MONDO_0018906)
Notes
top- Written by scripts/fetch-cancer-genes.ts from CIViC, Open Targets, IntOGen, HGNC and UniProt; the function text is UniProt's, condensed and in UK spelling. Roles: Open Targets known-drug datatype score 0.95. Evidence tier "approved-drug" is the strongest of those signals.
- Prevalence not recorded: none of the sources gives a positivity rate.
Latest papers
topQuery for this target: (TITLE:"PIK3CG" OR ABSTRACT:"PIK3CG" OR TITLE:"phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma" OR ABSTRACT:"phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma" OR TITLE:"Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform" OR ABSTRACT:"Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about PIK3CG, not a curated reading list.
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