PIK3CA

phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha

About This Gene

Phosphoinositide-3-kinase (PI3K) phosphorylates phosphatidylinositol (PI) and its phosphorylated derivatives at position 3 of the inositol ring to produce 3-phosphoinositides (PubMed:15135396, PubMed:23936502, PubMed:28676499). Uses ATP and PtdIns(4,5)P2 (phosphatidylinositol 4,5-bisphosphate) to generate phosphatidylinositol 3,4,5-trisphosphate (PIP3) (PubMed:15135396, PubMed:28676499). 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. Participates in cellular signaling in response to various growth factors. Involved in the activation of AKT1 upon stimulation by receptor tyrosine kinases ligands such as EGF, insulin, IGF1, VEGFA and PDGF. Involved in signaling via insulin-receptor substrate (IRS) proteins. Essential in endothelial cell migration during vascular development through VEGFA signaling, possibly by regulating RhoA activity. Required for lymphatic vasculature development, possibly by binding to RAS and by activation by EGF and FGF2, but not by PDGF. Regulates invadopodia formation through the PDPK1-AKT1 pathway. Participates in cardiomyogenesis in embryonic stem cells through a AKT1 pathway. Participates in vasculogenesis in embryonic stem cells through PDK1 and protein kinase C pathway. In addition to its lipid kinase activity, it displays a serine-protein kinase activity that results in the autophosphorylation of the p85alpha regulatory subunit as well as phosphorylation of other proteins such as 4EBP1, H-Ras, the IL-3 beta c receptor and possibly others (PubMed:23936502, PubMed:28676499). Plays a role in the positive regulation of phagocytosis and pinocytosis (By similarity). {ECO:0000250|UniProtKB:P42337, ECO:0000269|PubMed:15135396, ECO:0000269|PubMed:21708979, ECO:0000269|PubMed:23936502, ECO:0000269|PubMed:26593112, ECO:0000269|PubMed:28676499}.

Chromosome

Biotype

protein_coding

Diseases

Variants

Also Known As

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformPI3-kinase subunit alphaPI3K-alphaPI3KalphaPtdIns-3-kinase subunit alphaPtdIns-3-kinase subunit p110-alphap110alphaPIK3CAPI3KPhosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit alphaPhosphoinositide 3-kinase alphaPhosphoinositide-3-kinase catalytic alpha polypeptideSerine/threonine protein kinase PIK3CACCM4CLAPOCLOVECWS5HMHMCAPMCMMCMTCp110-alphaphosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoformPI3-kinase p110 subunit alphamutant phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alphaphosphatidylinositol 3-kinase, catalytic, 110-KD, alphaphosphatidylinositol 3-kinase, catalytic, alpha polypeptidephosphatidylinositol-4,5-bisphosphate 3-kinase 110 kDa catalytic subunit alphaphosphoinositide 3-kinase alphaphosphoinositide-3-kinase, catalytic, alpha polypeptideptdIns-3-kinase subunit p110-alphaserine/threonine protein kinase PIK3CA

Associated Diseases

25 disease associations found

Disease	Score	Therapeutic Areas
megalencephaly-capillary malformation-polymicrogyria syndrome	0.85	nervous system disordergenetic, familial or congenital disease
CLOVE syndrome	0.80	integumentary system disordergenetic, familial or congenital diseasecancer or benign tumor
CLOVES syndrome	0.79	integumentary system disordergenetic, familial or congenital diseasecancer or benign tumor
PIK3CA-related overgrowth spectrum	0.77	genetic, familial or congenital disease
breast cancer	0.75	reproductive system or breast diseasecancer or benign tumor
Cowden syndrome 5	0.75	genetic, familial or congenital diseaseintegumentary system disorder
ovarian cancer	0.73	endocrine system disorderreproductive system or breast diseasecancer or benign tumor
seborrheic keratosis	0.73	integumentary system disordergenetic, familial or congenital disease
breast adenocarcinoma	0.73	integumentary system disordercancer or benign tumorreproductive system or breast disease
CLAPO syndrome	0.72	genetic, familial or congenital disease
pik3ca related overgrowth spectrum	0.72	genetic, familial or congenital disease
Cowden disease	0.68	integumentary system disordergenetic, familial or congenital disease
megalodactyly	0.68	genetic, familial or congenital disease
hepatocellular carcinoma	0.67	hepatobiliary disorderendocrine system disordergastrointestinal diseasecancer or benign tumor
non-small cell lung carcinoma	0.67	respiratory or thoracic diseasecancer or benign tumor

Known Drug Targets

25 drugs targeting this gene

COPANLISIBApproved

PI3-kinase p110-alpha subunit inhibitor

follicular lymphomanon-Hodgkin lymphomaneoplasmindolent B-cell non-Hodgkin lymphomadiffuse large B-cell lymphomamantle cell lymphoma+29 more

COPANLISIB HYDROCHLORIDEApproved

PI3-kinase p110-alpha subunit inhibitor

follicular lymphomaneoplasm of mature B-cellsdiffuse large B-cell lymphomatriple-negative breast carcinomabreast cancerHodgkins lymphoma+1 more

ALPELISIBApproved

PI3-kinase p110-alpha subunit inhibitor

breast cancerbreast neoplasmneoplasmbreast carcinomahereditary endocrine growth diseasetriple-negative breast carcinoma+44 more

INAVOLISIBApproved

PI3-kinase p110-alpha subunit inhibitor

breast neoplasmbreast cancercentral nervous system neoplasmcentral nervous system cancerfallopian tube neoplasmovarian epithelial tumor+8 more

DACTOLISIBPhase 3

PI3-kinase class I inhibitor

Respiratory tract infectionbreast cancerendometrial carcinomapancreatic neuroendocrine tumortransitional cell carcinomakidney cancer+12 more

TASELISIBPhase 3

PI3-kinase class I inhibitor

breast cancerplasma cell myelomalymphomasquamous cell lung carcinomacancernon-Hodgkin lymphoma+1 more

BUPARLISIBPhase 3

PI3-kinase class I inhibitor

breast cancerhead and neck squamous cell carcinomaendometrial carcinomanon-small cell lung carcinomamalignant gliomaglioblastoma+36 more

GEDATOLISIBPhase 3

PI3-kinase class I inhibitor

breast cancerendometrial cancercolorectal cancermyelodysplastic syndromemyeloid neoplasmacute myeloid leukemia+15 more

PAXALISIBPhase 2/3

PI3-kinase class I inhibitor

glioblastomabrain glioblastomabreast cancerlung cancerprimary central nervous system lymphomadiffuse midline glioma+10 more

PILARALISIBPhase 2

PI3-kinase class I inhibitor

endometrial carcinomabreast cancerlymphomanon-small cell lung carcinomaovarian cancerendometrial cancer+2 more

SF-1126Phase 2

PI3-kinase class I inhibitor

head and neck cancerhead and neck squamous cell carcinomahepatocellular carcinomaB-cell chronic lymphocytic leukemianeuroblastoma

PICTILISIBPhase 2

PI3-kinase class I inhibitor

breast cancernon-Hodgkin lymphomanon-small cell lung carcinomaneoplasm

SAMOTOLISIBPhase 2

PI3-kinase class I inhibitor

prostate cancernon-small cell lung carcinomaendometrial cancerpancreatic ductal adenocarcinomapancreatic adenocarcinomanon-Hodgkin lymphoma+7 more

PF-04691502Phase 2

PI3-kinase class I inhibitor

endometrial cancerbreast cancer

SONOLISIBPhase 2

PI3-kinase class I inhibitor

glioblastomaprostate cancerhead and neck squamous cell carcinomanon-small cell lung carcinomacolorectal cancermelanoma

FIMEPINOSTATPhase 2

Histone deacetylase inhibitor

diffuse large B-cell lymphomathyroid cancerpoorly differentiated thyroid gland carcinomaACTH-dependent Cushing syndromeacute myeloid leukemianeuroblastoma+7 more

SERABELISIBPhase 2

PI3-kinase p110-alpha subunit inhibitor

renal cell carcinomaendometrial cancerbreast cancernon-small cell lung carcinomacancergastric adenocarcinoma+1 more

APITOLISIBPhase 2

PI3-kinase class I inhibitor

non-Hodgkin lymphomabreast cancerrenal cell carcinomaendometrial carcinomaprostate cancer

VOXTALISIBPhase 2

Serine/threonine-protein kinase mTOR inhibitor

mantle cell lymphomadiffuse large B-cell lymphomaB-cell chronic lymphocytic leukemiafollicular lymphomaborderline ovarian serous tumorbreast cancer+5 more

IZORLISIBPhase 1/2

PI3-kinase class I inhibitor

colorectal cancerneoplasm

BGT-226Phase 1/2

PI3-kinase class I inhibitor

breast cancer

PANULISIBPhase 1

PI3-kinase class I inhibitor

PKI-179Phase 1

PI3-kinase p110-alpha subunit inhibitor

colorectal cancerglioblastomaendometrial cancerovarian cancernon-small cell lung carcinomabreast cancer

RECILISIBPhase 1