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PIK3R1 (Phosphatidylinositol 3-kinase regulatory subunit alpha) is a gene whose normal job is to hold cell growth in check. The public catalogues list it as a drug target, an oncogene driver, a tumour suppressor and a biomarker, and clinical evidence ties its variants to diagnosis, prognosis or drug response. Tied to Endometrial cancer, Colorectal cancer, Breast cancer and 5 more.
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 signalling in response to FGFR1, FGFR2, FGFR3, FGFR4, KITLG/SCF, KIT, PDGFRA and PDGFRB.
CIViC holds 4 clinical evidence items and 0 assertions across 2 variants, naming Doxorubicin, Buparlisib, MTOR Kinase Inhibitor PP242 and Aspirin. Open Targets scores its association with cancer at 0.87 (direct and indirect evidence; datatypes clinical 0.67, affected pathway 0.85, literature 0.98, genetic association 0.71, somatic mutation 0.91). IntOGen calls it a driver in 24 cohorts (9 activating, 14 loss-of-function), covering Adenoid Cystic Carcinoma, Invasive Breast Carcinoma, Cholangiocarcinoma, Colon Adenocarcinoma, Colorectal Adenocarcinoma, Glioblastoma and others.
In plain words · PIK3R1 (Phosphatidylinositol 3-kinase regulatory subunit alpha) is a gene whose normal job is to hold cell growth in check. The public catalogues list it as a drug target, an oncogene driver, a tumour suppressor and a biomarker, and clinical evidence ties its variants to diagnosis, prognosis or drug response. Tied to Endometrial cancer, Colorectal cancer, Breast cancer and 5 more.
PIK3R1 (Phosphatidylinositol 3-kinase regulatory subunit alpha) is a gene whose normal job is to hold cell growth in check. The public catalogues list it as a drug target, an oncogene driver, a tumour suppressor and a biomarker, and clinical evidence ties its variants to diagnosis, prognosis or drug response. Tied to Endometrial cancer, Colorectal cancer, Breast cancer and 5 more.
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.
No product in this corpus aims at PIK3R1 yet. Because the protein is lost rather than overactive, drugs either restore its function or exploit the weakness its loss leaves (synthetic lethality).
Tumour-specific alteration: the catalogues call it an oncogene driver (IntOGen cohort analysis finds it activated more often than chance) and a tumour suppressor (IntOGen finds it knocked out more often than chance), so the direction differs between cohorts but the alteration is somatic either way; what a medicine would aim at or exploit is the altered form or its loss, absent from normal cells; no corpus medicine is aimed at it yet. HPA PIK3R1: RNA low tissue specificity; high antibody staining in 11 normal tissues; highest cancer staining lymphoma (9 of 12 high). Distribution: 8 cancer families in the corpus carry a prevalence row, label threshold or catalogue link for it (Endometrial cancer, Colorectal cancer, Breast cancer (all types), Skin cancer (all types), Sarcomas (soft tissue, bone, GIST), Gastric & gastro-oesophageal junction cancer, Leukaemia and more); Open Targets associates it with 1 specific cancer type at or above 0.5 (endometrial cancer). (Rule 6 of scripts/fetch-target-specificity.ts.)
Sources: UniProt P27986; CIViC gene PIK3R1; IntOGen PIK3R1; Human Protein Atlas PIK3R1 tissue; Open Targets ENSG00000145675 associations
First described 1991. Earliest sequence paper UniProt cites for the protein: Skolnik E.Y. et al, Cell, 1991, "Cloning of PI3 kinase-associated p85 utilizing a novel method for expression/cloning of target proteins for receptor tyrosine kinases". Source.
Sources: HGNC HGNC:8979 (approved symbol, name, aliases, locus and cross-references (hgnc_complete_set.txt)); UniProt P27986 (protein name, function text, keywords and locations (REST API)); CIViC gene PIK3R1 (4 evidence items, 0 assertions, 2 variants; diseases: Colorectal Cancer, Glioblastoma, Breast Cancer, Sarcoma (GraphQL API, CC0)); Open Targets ENSG00000145675 (association with cancer (MONDO_0004992) 0.87; per-cancer scores at or above 0.5: colorectal cancer 0.68, ovarian cancer 0.56, endometrial cancer 0.71, melanoma 0.57, glioblastoma 0.59, skin cancer 0.63 (GraphQL API, CC0)); IntOGen PIK3R1 (driver in 24 cohorts (Act 9, LoF 14); Compendium_Cancer_Genes.tsv release 20240920, CC0 1.0)
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 signalling in response to FGFR1, FGFR2, FGFR3, FGFR4, KITLG/SCF, KIT, PDGFRA and PDGFRB. Likewise, plays a role in ITGB2 signalling. 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. Location: Cytoplasm (UniProt). Locus 5q13.1 (HGNC).
RNA: low tissue specificity, detected in all normal tissues.
Medium: Adipose tissue, Adrenal gland, Appendix, Breast, Bronchus, Caudate, Cervix, Colon.
Medium only: breast cancer, carcinoid, head and neck cancer, liver cancer.
Human Protein Atlas version 25.1, antibody staining at reliability approved, enhanced or supported; used under CC BY-SA 3.0. Staining counts are patients per level in the atlas cohort, not population prevalence.
Query for this target: (TITLE:"PIK3R1" OR ABSTRACT:"PIK3R1" OR TITLE:"phosphoinositide-3-kinase regulatory subunit 1" OR ABSTRACT:"phosphoinositide-3-kinase regulatory subunit 1" OR TITLE:"Phosphatidylinositol 3-kinase regulatory subunit alpha" OR ABSTRACT:"Phosphatidylinositol 3-kinase regulatory subunit alpha" OR TITLE:"GRB1" OR ABSTRACT:"GRB1" OR TITLE:"p85-ALPHA" OR ABSTRACT:"p85-ALPHA" OR TITLE:"p85" OR ABSTRACT:"p85") 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 PIK3R1, not a curated reading list.
Shares Leukaemia (all types), Endometrial cancer, Skin cancer (all types), Ovarian cancer.
Shares Leukaemia (all types), Endometrial cancer, Sarcomas (soft tissue, bone, GIST), CIViC.
Shares Leukaemia (all types), Sarcomas (soft tissue, bone, GIST), CIViC, Gastric & gastro-oesophageal junction cancer.
Shares Leukaemia (all types), Endometrial cancer, CIViC, IntOGen.
Shares Leukaemia (all types), Endometrial cancer, Sarcomas (soft tissue, bone, GIST), CIViC.
Shares Leukaemia (all types), Skin cancer (all types), Sarcomas (soft tissue, bone, GIST), CIViC.
Shares Leukaemia (all types), Skin cancer (all types), CIViC, IntOGen.
Shares Leukaemia (all types), Endometrial cancer, Sarcomas (soft tissue, bone, GIST), CIViC.