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Aliases for PIK3CA Gene

Aliases for PIK3CA Gene

  • Phosphatidylinositol-4,5-Bisphosphate 3-Kinase Catalytic Subunit Alpha 2 3 5
  • Phosphoinositide-3-Kinase, Catalytic, Alpha Polypeptide 2 3
  • Serine/Threonine Protein Kinase PIK3CA 3 4
  • PtdIns-3-Kinase Subunit P110-Alpha 3 4
  • PI3K-Alpha 3 4
  • Phosphatidylinositol-4,5-Bisphosphate 3-Kinase Catalytic Subunit, Alpha Isoform 3
  • Phosphatidylinositol 4,5-Bisphosphate 3-Kinase Catalytic Subunit Alpha Isoform 3
  • Phosphatidylinositol-4,5-Bisphosphate 3-Kinase 110 KDa Catalytic Subunit Alpha 3
  • Phosphatidylinositol 4,5-Bisphosphate 3-Kinase 110 KDa Catalytic Subunit Alpha 4
  • Phosphatidylinositol-4,5-Bisphosphate 3-Kinase, Catalytic Subunit Alpha 2
  • Phosphatidylinositol 3-Kinase, Catalytic, Alpha Polypeptide 3
  • Phosphatidylinositol 3-Kinase, Catalytic, 110-KD, Alpha 3
  • Phosphoinositide-3-Kinase Catalytic Alpha Polypeptide 4
  • PI3-Kinase P110 Subunit Alpha 3
  • PtdIns-3-Kinase Subunit Alpha 4
  • PI3-Kinase Subunit Alpha 4
  • EC 2.7.1.153 4
  • EC 2.7.11.1 4
  • P110-Alpha 3
  • PI3Kalpha 4
  • P110alpha 4
  • CLOVE 3
  • MCMTC 3
  • CWS5 3
  • MCAP 3
  • PI3K 3
  • MCM 3

External Ids for PIK3CA Gene

Previous GeneCards Identifiers for PIK3CA Gene

  • GC03P175570
  • GC03P179758
  • GC03P180318
  • GC03P180237
  • GC03P180399
  • GC03P180349
  • GC03P178865
  • GC03P176269

Summaries for PIK3CA Gene

Entrez Gene Summary for PIK3CA Gene

  • Phosphatidylinositol 3-kinase is composed of an 85 kDa regulatory subunit and a 110 kDa catalytic subunit. The protein encoded by this gene represents the catalytic subunit, which uses ATP to phosphorylate PtdIns, PtdIns4P and PtdIns(4,5)P2. This gene has been found to be oncogenic and has been implicated in cervical cancers. A pseudogene of this gene has been defined on chromosome 22. [provided by RefSeq, Apr 2016]

CIViC summary for PIK3CA Gene

  • PIK3CA is the most recurrently mutated gene in breast cancer, and has been found to important in a number of cancer types. An integral part of the PI3K pathway, PIK3CA has long been described as an oncogene, with two main hotspots for activating mutations, the 542/545 region of the helical domain, and the 1047 region of the kinase domain. PIK3CA, and its interaction with the AKT and mTOR pathways, is the subject of an immense amount of research and development, and PI3K inhibition has seen some limited success in recent clinical trials. While monotherapies seem to be limited in their potential, there is a recent interest in pursuing PI3K inhibition as part of a combination therapy regiment with inhibition partners including TKI's, MEK inhibitors, PARP inhibitors, and in breast cancer, aromatase inhibitors.

GeneCards Summary for PIK3CA Gene

PIK3CA (Phosphatidylinositol-4,5-Bisphosphate 3-Kinase Catalytic Subunit Alpha) is a Protein Coding gene. Diseases associated with PIK3CA include Congenital Lipomatous Overgrowth, Vascular Malformations, And Epidermal Nevi and Megalencephaly-Capillary Malformation-Polymicrogyria Syndrome. Among its related pathways are mTOR Pathway and Focal Adhesion. Gene Ontology (GO) annotations related to this gene include transferase activity, transferring phosphorus-containing groups and protein serine/threonine kinase activity. An important paralog of this gene is PIK3CD.

UniProtKB/Swiss-Prot for PIK3CA Gene

  • Phosphoinositide-3-kinase (PI3K) that phosphorylates PtdIns (Phosphatidylinositol), PtdIns4P (Phosphatidylinositol 4-phosphate) and 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. 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. Also has serine-protein kinase activity: phosphorylates PIK3R1 (p85alpha regulatory subunit), EIF4EBP1 and HRAS. Plays a role in the positive regulation of phagocytosis and pinocytosis (By similarity).

Tocris Summary for PIK3CA Gene

  • PI 3-Kinases (phosphoinositide 3-kinases, PI 3-Ks) are a family of lipid kinases capable of phosphorylating the 3'OH of the inositol ring of phosphoinositides. They are responsible for coordinating a diverse range of cell functions including proliferation and survival.

Gene Wiki entry for PIK3CA Gene

Additional gene information for PIK3CA Gene

No data available for PharmGKB "VIP" Summary , fRNAdb sequence ontologies and piRNA Summary for PIK3CA Gene

Genomics for PIK3CA Gene

GeneHancer (GH) Regulatory Elements for PIK3CA Gene

Promoters and enhancers for PIK3CA Gene
GeneHancer (GH) Identifier GH Type GH
Score
GH Sources Gene Association Score Total Score TSS distance (kb) Number of Genes Away Size (kb) Transcription Factor
Binding Sites
Gene Targets
GH03J179146 Promoter/Enhancer 1.6 Ensembl ENCODE 650.7 +0.4 413 3.6 HDGF PKNOX1 FOXA2 SMAD1 ZFP64 ARID4B SIN3A DMAP1 ZNF2 ZBTB7B PIK3CA LOC101928739 ENSG00000242539 ZNF639 ENSG00000201957
GH03J179068 Promoter/Enhancer 2.3 EPDnew FANTOM5 Ensembl ENCODE 11 -77.4 -77397 3.8 HDGF SMAD1 ARID4B SIN3A FEZF1 IRF4 ZNF143 ZNF207 ZHX2 MXD4 ZMAT3 PIK3CA LOC101928739 ZNF639 GC03M179018
GH03J179321 Promoter/Enhancer 2 EPDnew Ensembl ENCODE 10.5 +175.4 175397 4.3 HDGF PKNOX1 ARNT SIN3A FEZF1 DMAP1 ZBTB7B YY1 ZNF213 ZNF207 ZNF639 MFN1 ENSG00000242539 LOC101928739 PIK3CA ENSG00000260743
GH03J179033 Enhancer 1.4 FANTOM5 Ensembl ENCODE dbSUPER 10.5 -111.7 -111717 5.8 FOXA2 DMAP1 TCF12 EGR2 ZNF680 SP5 SMARCA4 GLIS1 NR2C1 KDM1A PIK3CA LOC101928739 ZMAT3 KCNMB3 GC03M179018
GH03J179179 Enhancer 1.1 Ensembl ENCODE 12 +33.0 33043 3.1 PKNOX1 ZSCAN4 KLF17 FEZF1 ZEB1 ZNF121 ZNF366 SCRT2 FOS ATF7 PIK3CA LOC101928739 KCNMB3 ENSG00000201957 GC03P179235
- Elite GeneHancer and/or Elite GeneHancer-gene association Download GeneHancer data from 2017 publication | Request up-to-date GeneHancer data (full dataset)

GeneHancers around PIK3CA on UCSC Golden Path with GeneCards custom track

Top Transcription factor binding sites by QIAGEN in the PIK3CA gene promoter:
  • PPAR-gamma2
  • PPAR-gamma1
  • FOXO4
  • FOXO1a
  • FOXO1
  • CUTL1

Genomic Locations for PIK3CA Gene

Genomic Locations for PIK3CA Gene
chr3:179,148,114-179,240,093
(GRCh38/hg38)
Size:
91,980 bases
Orientation:
Plus strand
chr3:178,865,902-178,957,881
(GRCh37/hg19)
Size:
91,980 bases
Orientation:
Plus strand

Genomic View for PIK3CA Gene

Genes around PIK3CA on UCSC Golden Path with GeneCards custom track

Cytogenetic band:
PIK3CA Gene in genomic location: bands according to Ensembl, locations according to GeneLoc (and/or Entrez Gene and/or Ensembl if different)
Genomic Location for PIK3CA Gene
GeneLoc Logo Genomic Neighborhood Exon StructureGene Density

RefSeq DNA sequence for PIK3CA Gene

Proteins for PIK3CA Gene

  • Protein details for PIK3CA Gene (UniProtKB/Swiss-Prot)

    Protein Symbol:
    P42336-PK3CA_HUMAN
    Recommended name:
    Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
    Protein Accession:
    P42336
    Secondary Accessions:
    • Q14CW1
    • Q99762

    Protein attributes for PIK3CA Gene

    Size:
    1068 amino acids
    Molecular mass:
    124284 Da
    Quaternary structure:
    • Heterodimer of a catalytic subunit PIK3CA and a p85 regulatory subunit (PIK3R1, PIK3R2 or PIK3R3) (PubMed:26593112). Interacts with IRS1 in nuclear extracts (By similarity). Interacts with RUFY3 (By similarity). Interacts with RASD2 (By similarity). Interacts with APPL1. Interacts with HRAS and KRAS (By similarity). Interaction with HRAS/KRAS is required for PI3K pathway signaling and cell proliferation stimulated by EGF and FGF2 (By similarity). Interacts with FAM83B; activates the PI3K/AKT signaling cascade (PubMed:23676467).
    Miscellaneous:
    • The avian sarcoma virus 16 genome encodes an oncogene derived from PIK3CA.

    Three dimensional structures from OCA and Proteopedia for PIK3CA Gene

neXtProt entry for PIK3CA Gene

Post-translational modifications for PIK3CA Gene

  • Ubiquitination at Lys100
  • Modification sites at PhosphoSitePlus

Other Protein References for PIK3CA Gene

No data available for DME Specific Peptides for PIK3CA Gene

Domains & Families for PIK3CA Gene

Gene Families for PIK3CA Gene

HGNC:
IUPHAR :
Human Protein Atlas (HPA):
  • Cancer-related genes
  • Disease related genes
  • Enzymes
  • Potential drug targets
  • Predicted intracellular proteins

Graphical View of Domain Structure for InterPro Entry

P42336

UniProtKB/Swiss-Prot:

PK3CA_HUMAN :
  • The PI3K-ABD domain and the PI3K-RBD domain interact with the PI3K/PI4K kinase domain. The C2 PI3K-type domain may facilitate the recruitment to the plasma membrane. The inhibitory interactions with PIK3R1 are mediated by the PI3K-ABD domain and the C2 PI3K-type domain with the iSH2 (inter-SH2) region of PIK3R1, and the C2 PI3K-type domain, the PI3K helical domain, and the PI3K/PI4K kinase domain with the nSH2 (N-terminal SH2) region of PIK3R1.
  • Belongs to the PI3/PI4-kinase family.
Domain:
  • The PI3K-ABD domain and the PI3K-RBD domain interact with the PI3K/PI4K kinase domain. The C2 PI3K-type domain may facilitate the recruitment to the plasma membrane. The inhibitory interactions with PIK3R1 are mediated by the PI3K-ABD domain and the C2 PI3K-type domain with the iSH2 (inter-SH2) region of PIK3R1, and the C2 PI3K-type domain, the PI3K helical domain, and the PI3K/PI4K kinase domain with the nSH2 (N-terminal SH2) region of PIK3R1.
Family:
  • Belongs to the PI3/PI4-kinase family.
genes like me logo Genes that share domains with PIK3CA: view

Function for PIK3CA Gene

Molecular function for PIK3CA Gene

UniProtKB/Swiss-Prot Function:
Phosphoinositide-3-kinase (PI3K) that phosphorylates PtdIns (Phosphatidylinositol), PtdIns4P (Phosphatidylinositol 4-phosphate) and 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. 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. Also has serine-protein kinase activity: phosphorylates PIK3R1 (p85alpha regulatory subunit), EIF4EBP1 and HRAS. Plays a role in the positive regulation of phagocytosis and pinocytosis (By similarity).
UniProtKB/Swiss-Prot CatalyticActivity:
ATP + 1-phosphatidyl-1D-myo-inositol 4,5-bisphosphate = ADP + 1-phosphatidyl-1D-myo-inositol 3,4,5-trisphosphate.
UniProtKB/Swiss-Prot CatalyticActivity:
ATP + a protein = ADP + a phosphoprotein.
GENATLAS Biochemistry:
phosphatidylinositol-3-kinase,catalytic,class 1,alpha subunit,widely expressed, activated by growth factors,through binding p785 adaptor proteins (PIK3R1,PIK3R2,PIK3R3),activating Akts in the antiapoptotic PIK3 pathway,antagonized by PTEN,mediating angiogenes is and expression of VEGF in endothelial cells,involved in the regulation of cellular processes,potentially oncogenic in ovarian cancer

Enzyme Numbers (IUBMB) for PIK3CA Gene

Gene Ontology (GO) - Molecular Function for PIK3CA Gene

GO ID Qualified GO term Evidence PubMed IDs
GO:0004674 protein serine/threonine kinase activity IEA --
GO:0005488 binding IEA --
GO:0005515 protein binding IPI 10490823
GO:0005524 ATP binding IEA --
GO:0016301 kinase activity TAS,IEA --
genes like me logo Genes that share ontologies with PIK3CA: view
genes like me logo Genes that share phenotypes with PIK3CA: view

Human Phenotype Ontology for PIK3CA Gene

HPO Id HPO Name Alternative Ids Definition Synonyms

Animal Models for PIK3CA Gene

MGI Knock Outs for PIK3CA:

Animal Model Products

Clone Products

No data available for Phenotypes From GWAS Catalog , Transcription Factor Targets and HOMER Transcription for PIK3CA Gene

Localization for PIK3CA Gene

Subcellular locations from

COMPARTMENTS
Extracellular space Cytosol Plasma membrane Cytoskeleton Lysosome Endosome Peroxisome ER Golgi Apparatus Nucleus Mitochondrion 0 1 2 3 4 5 Confidence
COMPARTMENTS Subcellular localization image for PIK3CA gene
Compartment Confidence
cytosol 5
plasma membrane 4
nucleus 3
mitochondrion 2
extracellular 1
cytoskeleton 1
peroxisome 1
endoplasmic reticulum 1
golgi apparatus 1

Subcellular locations from the

Human Protein Atlas (HPA)

Gene Ontology (GO) - Cellular Components for PIK3CA Gene

GO ID Qualified GO term Evidence PubMed IDs
GO:0005622 intracellular IEA --
GO:0005737 cytoplasm IBA --
GO:0005829 cytosol TAS --
GO:0005886 plasma membrane IBA --
GO:0005942 phosphatidylinositol 3-kinase complex IEA,ISS --
genes like me logo Genes that share ontologies with PIK3CA: view

No data available for Subcellular locations from UniProtKB/Swiss-Prot for PIK3CA Gene

Pathways & Interactions for PIK3CA Gene

SuperPathways for PIK3CA Gene

SuperPathway Contained pathways
1 RET signaling
2 Downstream signaling of activated FGFR2
3 Regulation of lipid metabolism Insulin signaling-generic cascades
4 Development HGF signaling pathway
5 PI3K/AKT activation
genes like me logo Genes that share pathways with PIK3CA: view

Pathways by source for PIK3CA Gene

SIGNOR curated interactions for PIK3CA Gene

Gene Ontology (GO) - Biological Process for PIK3CA Gene

GO ID Qualified GO term Evidence PubMed IDs
GO:0001525 angiogenesis IEA --
GO:0001889 liver development IEA --
GO:0001944 vasculature development TAS 19200708
GO:0002250 adaptive immune response IBA --
GO:0006006 glucose metabolic process IEA --
genes like me logo Genes that share ontologies with PIK3CA: view

Drugs & Compounds for PIK3CA Gene

(190) Drugs for PIK3CA Gene - From: DrugBank, PharmGKB, ClinicalTrials, ApexBio, DGIdb, FDA Approved Drugs, HMDB, Tocris, and Novoseek

Name Status Disease Links Group Role Mechanism of Action Clinical Trials
Everolimus Approved Pharma inhibitor, Biomarker mTOR inhibitor, mTOR Inhibitors, Kinase Inhibitors, Mammalian target of rapamycin (mTOR) inhibitors 2011
Cisplatin Approved Pharma Inhibits DNA synthesis,chemotherapy drug, Platinum, Potent pro-apoptotic anticancer agent; activates caspase-3 2906
Paclitaxel Approved, Vet_approved Pharma Tubulin and Bcl2 inhibitor, Taxanes 3027
Copanlisib Approved, Investigational Pharma Target, inhibitor 0
Caffeine Approved Nutra Antagonist, Activator, Target, inhibitor 434

(417) Additional Compounds for PIK3CA Gene - From: HMDB, Novoseek, and Tocris

Name Synonyms Role CAS Number PubChem IDs PubMed IDs
ADP
  • 5'-Adenylphosphoric acid
  • Adenosine 5'-diphosphate
  • ADENOSINE-5'-diphosphATE
  • H3ADP
  • 5'-Adenylphosphate
Full agonist, Agonist, Partial agonist, Antagonist, Gating inhibitor 58-64-0
Phosphatidylinositol-3,4,5-trisphosphate
  • 1,2-Diacyl-sn-glycero-3-phospho-(1'-myo-inositol-3',4',5'-bisphosphate)
  • 1-Phosphatidyl-1D-myo-inositol 3,4,5-trisphosphate
1-Phosphatidyl-D-myo-inositol
  • (3-Phosphatidyl)-1-D-inositol
  • 1,2-Diacyl-sn-glycero-3-phosphoinositol
  • 1-Phosphatidyl-1D-myo-inositol
  • 1-Phosphatidyl-myo-inositol
  • Phosphatidyl-1D-myo-inositol
PI(16:0/16:0)
  • 1,2-Dihexadecanoyl-rac-glycero-3-phospho-(1'-myo-inositol)
  • 1,2-Dipalmitoyl-rac-glycero-3-phosphoinositol
  • Phosphatidylinositol(16:0/16:0)
  • Phosphatidylinositol(32:0)
  • PI(32:0)
PI(16:0/16:1(9Z))
  • 1-Hexadecanoyl-2-(9Z-hexadecenoyl)-sn-glycero-3-phospho-(1'-myo-inositol)
  • 1-Palmitoyl-2-palmitoleoyl-sn-glycero-3-phosphoinositol
  • Phosphatidylinositol(16:0/16:1)
  • Phosphatidylinositol(16:0/16:1n7)
  • Phosphatidylinositol(16:0/16:1W7)

(5) Tocris Compounds for PIK3CA Gene

Compound Action Cas Number
3-Methyladenine Class III PI 3-kinase inhibitor; also inhibits autophagy 5142-23-4
LY 294002 hydrochloride Prototypical PI 3-kinase inhibitor; also inhibits other kinases 934389-88-5
PI 103 hydrochloride Inhibitor of PI 3-kinase, mTOR and DNA-PK 371935-79-4
Quercetin Non-selective PI 3-kinase inhibitor 117-39-5
Wortmannin Potent, irreversible inhibitor of PI 3-kinase. Also inhibitor of PLK1 19545-26-7

(63) ApexBio Compounds for PIK3CA Gene

Compound Action Cas Number
3-Methyladenine Class III PI3K inhibitor 5142-23-4
740 Y-P PI 3-kinase activator,cell permeable 1236188-16-1
A66 P110α inhibitor 1166227-08-2
AS-252424 PI3Kγ inhibitor,novel and potent 900515-16-4
AS-604850 PI3Kγ inhibitor,selective and ATP-competitve 648449-76-7
AZD6482 PI3Kβ inhibitor,potent and selective 1173900-33-8
AZD8186 Potent and selective inhibitor of PI3Kβ and PI3Kδ 1627494-13-6
BAY 80-6946 (Copanlisib) PI3K inhibitor 1032568-63-0
BEZ235 (NVP-BEZ235) PI3K/mTOR inhibitor,ATP-competitve 915019-65-7
BEZ235 Tosylate MTOR/P13K inhibitor 1028385-32-1
BKM120 Inhibitor of pan-Class I PI3K 944396-07-0
BYL-719 Selective PI3Kα inhibitor 1217486-61-7
CAL-101 (Idelalisib, GS-1101) PI3K inhibitor 870281-82-6
CAL-130 PI3K inhibitor 1431697-74-3
CAL-130 Hydrochloride PI3K inhibitor 1431697-78-7
CAL-130 Racemate PI3K inhibitor 474012-90-3
CAY10505 Potent PI3Kγ inhibitor 1218777-13-9
CH5132799 Class I PI3K inhibitor 1007207-67-1
CNX1351 PI3Kα inhibitor 1276105-89-5
CZC24832 Selective PI3K-γ inhibitor 1159824-67-5
GDC-0032 PI3Kα inhibitor 1282512-48-4
GDC-0941 PI3K inhibitor,potent and selective 957054-30-7
GDC-0941 dimethanesulfonate PI3K inhibitor 957054-33-0
GDC-0980 (RG7422) Class I PI3K inhibitor for PI3Kα/β/δ/γ 1032754-93-0
GNE-317 1394076-92-6
GSK1059615 PI3K and mTOR inhibitor,potent and reversible 958852-01-2
GSK2126458 PI3K/mTOR inhibitor 1086062-66-9
GSK2636771 PIK3 inhibitor 1372540-25-4
HS-173 1276110-06-5
INK 128 (MLN0128) MTOR(TORC-1/-2) inhibitor,potent and selective 1224844-38-5
KU-0060648 Dual DNA-PK/PI3-K inhibitor, ATP-competitive 881375-00-4
LY 294002 Potent PI3K inhibitor 154447-36-6
Miltefosine PI3K/Akt inhibitor 58066-85-6
NVP-BGT226 PI3K/mTOR inhibitor,selective and novel 1245537-68-1
NVP-QAV-572 957209-68-6
Palomid 529 PI3K/Akt/mTOR inhibitor 914913-88-5
PF-04691502 PI3K/mTOR (FRAP) inhibitor 1013101-36-4
PF-05212384 (PKI-587) PI3Kα, PI3Kγ and mTOR inhibitor 1197160-78-3
PF-4989216 Selective oral PI3K inhibitor 1276553-09-3
PI 828 942289-87-4
PI-103 Class I PI3K, mTOR and DNA-PK inhibitor 371935-74-9
PI-103 Hydrochloride DNA-PK/PI 3-kinase/mTOR inhibitor 371935-79-4
PI3k-delta inhibitor 1 PI3k-delta inhibitor 1332075-63-4
PI3Kγ inhibitor 1 1172118-03-4
PIK-293 900185-01-5
PIK-294 900185-02-6
PIK-75 Inhibitor of PI3K isoform p110α 372196-77-5
PIK-90 PI3K inhibitor,potent selective 677338-12-4
PIK-93 PI3Kγ/PI4KIIIβ/PI3Kα inhibitor 593960-11-3
PKI-402 PI3K inhibitor,selective, reversible and ATP-competitive 1173204-81-3
PP121 Dual inhibitor of tyrosine and phosphoinositide kinases 1092788-83-4
Quercetin Antitumor agent 117-39-5
Quercetin dihydrate PLA2 and PI 3-kinase inhibitor 6151-25-3
Rigosertib sodium 592542-60-4
SAR245409 (XL765) mTOR/PI3K inhibitor 1349796-36-6
TG100713 925705-73-3
TGX-221 PI3Kβ inhibitor,potent,selective and ATP competitive 663619-89-4
VS-5584 (SB2343) MTOR/P13K inhibitor,potent and selective 1246560-33-7
Wortmannin PI3K inhibitor,selective and irreversible 19545-26-7
XL147 PI3K inhibitor,selective and reversible 956958-53-5
XL765 PI3K/mTOR inhibitor 1123889-87-1
ZSTK474 Potent PI3K inhibitor 475110-96-4
α-mangostin PI3K/AKT inhibitor 6147-11-1
genes like me logo Genes that share compounds with PIK3CA: view

Drug Products

Transcripts for PIK3CA Gene

mRNA/cDNA for PIK3CA Gene

Unigene Clusters for PIK3CA Gene

Phosphatidylinositol-4,5-bisphosphate 3-kinase, catalytic subunit alpha:
Representative Sequences:

Clone Products

Alternative Splicing Database (ASD) splice patterns (SP) for PIK3CA Gene

No ASD Table

Relevant External Links for PIK3CA Gene

GeneLoc Exon Structure for
PIK3CA
ECgene alternative splicing isoforms for
PIK3CA

Expression for PIK3CA Gene

mRNA expression in normal human tissues from GTEx, Illumina, BioGPS, and CGAP SAGE for PIK3CA Gene

Protein differential expression in normal tissues from HIPED for PIK3CA Gene

This gene is overexpressed in Plasma (30.0) and Peripheral blood mononuclear cells (10.8).

Integrated Proteomics: protein expression in normal tissues and cell lines from ProteomicsDB, MaxQB, and MOPED for PIK3CA Gene



Protein tissue co-expression partners for PIK3CA Gene

NURSA nuclear receptor signaling pathways regulating expression of PIK3CA Gene:

PIK3CA

SOURCE GeneReport for Unigene cluster for PIK3CA Gene:

Hs.553498

Evidence on tissue expression from TISSUES for PIK3CA Gene

  • Lung(4.8)
  • Nervous system(3.9)
  • Intestine(3.6)
  • Lymph node(2.4)
  • Thyroid gland(2.4)
  • Kidney(2.3)
  • Pancreas(2.2)
  • Skin(2.2)
  • Blood(2.1)
  • Liver(2.1)
  • Gall bladder(2)
  • Heart(2)
  • Muscle(2)

Phenotype-based relationships between genes and organs from Gene ORGANizer for PIK3CA Gene

Germ Layers:
  • ectoderm
  • endoderm
  • mesoderm
Systems:
  • cardiovascular
  • digestive
  • endocrine
  • immune
  • integumentary
  • lymphatic
  • nervous
  • reproductive
  • respiratory
  • skeletal muscle
  • skeleton
  • urinary
Regions:
Head and neck:
  • brain
  • cerebellum
  • cerebrospinal fluid
  • cheek
  • chin
  • cranial nerve
  • ear
  • eye
  • eyelid
  • face
  • forehead
  • head
  • hypothalamus
  • jaw
  • lip
  • mandible
  • maxilla
  • meninges
  • mouth
  • neck
  • nose
  • outer ear
  • parathyroid
  • pituitary gland
  • salivary gland
  • skull
  • thyroid
  • tongue
  • tooth
Thorax:
  • breast
  • chest wall
  • clavicle
  • esophagus
  • heart
  • lung
  • rib
  • rib cage
  • scapula
  • sternum
Abdomen:
  • abdominal wall
  • adrenal gland
  • appendix
  • biliary tract
  • duodenum
  • gallbladder
  • intestine
  • kidney
  • large intestine
  • liver
  • pancreas
  • small intestine
  • spleen
  • stomach
Pelvis:
  • anus
  • ovary
  • pelvis
  • penis
  • rectum
  • testicle
  • ureter
  • urethra
  • urinary bladder
  • uterus
Limb:
  • ankle
  • arm
  • digit
  • elbow
  • femur
  • fibula
  • finger
  • foot
  • forearm
  • hand
  • hip
  • humerus
  • knee
  • lower limb
  • nail
  • radius
  • shin
  • shoulder
  • thigh
  • tibia
  • toe
  • ulna
  • upper limb
  • wrist
General:
  • blood
  • blood vessel
  • bone marrow
  • coagulation system
  • hair
  • peripheral nerve
  • peripheral nervous system
  • red blood cell
  • skin
  • spinal column
  • spinal cord
  • vertebrae
  • white blood cell
genes like me logo Genes that share expression patterns with PIK3CA: view

No data available for mRNA expression in embryonic tissues and stem cells from LifeMap Discovery , mRNA differential expression in normal tissues and mRNA Expression by UniProt/SwissProt for PIK3CA Gene

Orthologs for PIK3CA Gene

This gene was present in the common ancestor of animals.

Orthologs for PIK3CA Gene

Organism Taxonomy Gene Similarity Type Details
chimpanzee
(Pan troglodytes)
Mammalia PIK3CA 34 33
  • 99.94 (n)
OneToOne
platypus
(Ornithorhynchus anatinus)
Mammalia PIK3CA 34
  • 97 (a)
OneToOne
oppossum
(Monodelphis domestica)
Mammalia PIK3CA 34
  • 97 (a)
OneToOne
cow
(Bos Taurus)
Mammalia PIK3CA 34 33
  • 96.35 (n)
OneToOne
dog
(Canis familiaris)
Mammalia PIK3CA 34 33
  • 96.13 (n)
OneToOne
mouse
(Mus musculus)
Mammalia Pik3ca 16 34 33
  • 89.64 (n)
rat
(Rattus norvegicus)
Mammalia Pik3ca 33
  • 89.45 (n)
chicken
(Gallus gallus)
Aves PIK3CA 34 33
  • 85.3 (n)
OneToOne
lizard
(Anolis carolinensis)
Reptilia PIK3CA 34
  • 95 (a)
OneToOne
tropical clawed frog
(Silurana tropicalis)
Amphibia pik3ca 33
  • 79.04 (n)
African clawed frog
(Xenopus laevis)
Amphibia pik3ca-A 33
zebrafish
(Danio rerio)
Actinopterygii PIK3CA (2 of 3) 34
  • 92 (a)
OneToMany
PIK3CA (3 of 3) 34
  • 91 (a)
OneToMany
PIK3CA (1 of 3) 34
  • 82 (a)
OneToMany
LOC561737 33
  • 76.25 (n)
fruit fly
(Drosophila melanogaster)
Insecta Pi3K92E 35
  • 34 (a)
worm
(Caenorhabditis elegans)
Secernentea age-1 33
  • 47.81 (n)
sea squirt
(Ciona savignyi)
Ascidiacea -- 34
  • 49 (a)
OneToOne
Species where no ortholog for PIK3CA was found in the sources mined by GeneCards:
  • A. gosspyii yeast (Ashbya gossypii)
  • Actinobacteria (Mycobacterium tuberculosis)
  • African malaria mosquito (Anopheles gambiae)
  • Alicante grape (Vitis vinifera)
  • alpha proteobacteria (Wolbachia pipientis)
  • amoeba (Dictyostelium discoideum)
  • Archea (Pyrococcus horikoshii)
  • baker's yeast (Saccharomyces cerevisiae)
  • barley (Hordeum vulgare)
  • beta proteobacteria (Neisseria meningitidis)
  • bread mold (Neurospora crassa)
  • Chromalveolata (Phytophthora infestans)
  • common water flea (Daphnia pulex)
  • corn (Zea mays)
  • E. coli (Escherichia coli)
  • filamentous fungi (Aspergillus nidulans)
  • Firmicute bacteria (Streptococcus pneumoniae)
  • fission yeast (Schizosaccharomyces pombe)
  • green algae (Chlamydomonas reinhardtii)
  • honey bee (Apis mellifera)
  • K. lactis yeast (Kluyveromyces lactis)
  • loblloly pine (Pinus taeda)
  • malaria parasite (Plasmodium falciparum)
  • medicago trunc (Medicago Truncatula)
  • moss (Physcomitrella patens)
  • orangutan (Pongo pygmaeus)
  • pig (Sus scrofa)
  • rainbow trout (Oncorhynchus mykiss)
  • rice (Oryza sativa)
  • rice blast fungus (Magnaporthe grisea)
  • schistosome parasite (Schistosoma mansoni)
  • sea anemone (Nematostella vectensis)
  • sea urchin (Strongylocentrotus purpuratus)
  • sorghum (Sorghum bicolor)
  • soybean (Glycine max)
  • stem rust fungus (Puccinia graminis)
  • sugarcane (Saccharum officinarum)
  • thale cress (Arabidopsis thaliana)
  • tomato (Lycopersicon esculentum)
  • toxoplasmosis (Toxoplasma gondii)
  • Trichoplax (Trichoplax adhaerens)
  • wheat (Triticum aestivum)

Evolution for PIK3CA Gene

ENSEMBL:
Gene Tree for PIK3CA (if available)
TreeFam:
Gene Tree for PIK3CA (if available)
Aminode:
Evolutionary constrained regions (ECRs) for PIK3CA: view image

Paralogs for PIK3CA Gene

Paralogs for PIK3CA Gene

(5) SIMAP similar genes for PIK3CA Gene using alignment to 4 proteins:

  • PK3CA_HUMAN
  • C9J951_HUMAN
  • C9JAM9_HUMAN
  • E2I6G1_HUMAN

Pseudogenes.org Pseudogenes for PIK3CA Gene

genes like me logo Genes that share paralogs with PIK3CA: view

Variants for PIK3CA Gene

Sequence variations from dbSNP and Humsavar for PIK3CA Gene

SNP ID Clin Chr 03 pos Variation AA Info Type
rs104885999 not-provided, Familial cancer of breast 179,218,241(+) G/A coding_sequence_variant, missense_variant
rs104886000 not-provided, Familial cancer of breast 179,218,334(+) G/A coding_sequence_variant, missense_variant
rs104886001 not-provided, Familial cancer of breast 179,218,352(+) G/A intron_variant
rs104886002 not-provided, Endometrial carcinoma 179,218,154(+) C/T intron_variant
rs104886003 pathogenic, not-provided, likely-pathogenic, Breast adenocarcinoma, Ovarian epithelial cancer, Carcinoma of colon, Neoplasm of stomach, Keratosis, seborrheic, Non-small cell lung cancer, Megalencephaly cutis marmorata telangiectatica congenita, Sarcoma, Adenocarcinoma of prostate, Squamous cell carcinoma of lung, Pancreatic adenocarcinoma, Squamous cell carcinoma of the head and neck, Renal cell carcinoma, Ovarian Neoplasms, Carcinoma of esophagus, Malignant neoplasm of body of uterus, Ovarian Serous Cystadenocarcinoma, Transitional cell carcinoma of the bladder, Nasopharyngeal Neoplasms, Uterine cervical neoplasms, Neoplasm of the breast, Malignant melanoma of skin, Papillary renal cell carcinoma, sporadic, Small cell lung cancer, Hepatocellular carcinoma, Carcinoma of gallbladder, Glioblastoma, Colorectal Neoplasms, Adenocarcinoma of lung, Adenocarcinoma of stomach, Uterine Carcinosarcoma, Brainstem glioma, Neoplasm of brain, Head and Neck Neoplasms, Breast cancer (BC) [MIM:114480], Colorectal cancer (CRC) [MIM:114500], Keratosis, seborrheic (KERSEB) [MIM:182000], Megalencephaly-capillary malformation-polymicrogyria syndrome (MCAP) [MIM:602501] 179,218,303(+) G/A/C coding_sequence_variant, missense_variant

Structural Variations from Database of Genomic Variants (DGV) for PIK3CA Gene

Variant ID Type Subtype PubMed ID
dgv4999n100 CNV gain 25217958
dgv842n67 CNV gain 20364138
esv1007496 CNV loss 20482838
esv2659099 CNV deletion 23128226
esv2726256 CNV deletion 23290073
esv275373 CNV gain+loss 21479260
esv2763744 CNV gain+loss 21179565
esv3598835 CNV loss 21293372
esv3893827 CNV gain 25118596
nsv1003540 CNV loss 25217958
nsv1005062 CNV loss 25217958
nsv1010571 CNV gain 25217958
nsv1114454 CNV deletion 24896259
nsv1161006 CNV duplication 26073780
nsv1161007 CNV deletion 26073780
nsv461026 CNV gain 19166990
nsv524471 CNV loss 19592680
nsv592649 CNV gain 21841781
nsv819800 CNV gain 19587683
nsv822351 CNV loss 20364138
nsv829806 CNV gain 17160897
nsv979905 CNV duplication 23825009

Variation tolerance for PIK3CA Gene

Residual Variation Intolerance Score: 8.83% of all genes are more intolerant (likely to be disease-causing)
Gene Damage Index Score: 4.25; 62.38% of all genes are more intolerant (likely to be disease-causing)

Additional Variant Information for PIK3CA Gene

Human Gene Mutation Database (HGMD)
PIK3CA
SNPedia medical, phenotypic, and genealogical associations of SNPs for
PIK3CA

No data available for Polymorphic Variants from UniProtKB/Swiss-Prot for PIK3CA Gene

Disorders for PIK3CA Gene

MalaCards: The human disease database

(120) MalaCards diseases for PIK3CA Gene - From: HGMD, OMIM, ClinVar, GTR, Orphanet, Swiss-Prot, DISEASES, Novoseek, and GeneCards

- elite association - COSMIC cancer census association via MalaCards

UniProtKB/Swiss-Prot

PK3CA_HUMAN
  • Note=PIK3CA mutations are involved in various type of cancer. Most of the cancer-associated mutations are missense mutations and map to one of the three hotspots: Glu-542; Glu-545 and His-1047. Mutated isoforms participate in cellular transformation and tumorigenesis induced by oncogenic receptor tyrosine kinases (RTKs) and HRAS/KRAS. Interaction with HRAS/KRAS is required for Ras-driven tumor formation. Mutations increasing the lipid kinase activity are required for oncogenic signaling. The protein kinase activity may not be required for tumorigenesis. {ECO:0000269 PubMed:15016963, ECO:0000269 PubMed:15289301, ECO:0000269 PubMed:15520168, ECO:0000269 PubMed:15712344, ECO:0000269 PubMed:15784156, ECO:0000269 PubMed:15924253, ECO:0000269 PubMed:15930273, ECO:0000269 PubMed:15994075, ECO:0000269 PubMed:16114017, ECO:0000269 PubMed:16322209, ECO:0000269 PubMed:16353168, ECO:0000269 PubMed:16432179, ECO:0000269 PubMed:16533766, ECO:0000269 PubMed:17673550, ECO:0000269 PubMed:19805105, ECO:0000269 PubMed:21708979, ECO:0000269 PubMed:22658544, ECO:0000269 PubMed:22729224}.
  • Colorectal cancer (CRC) [MIM:114500]: A complex disease characterized by malignant lesions arising from the inner wall of the large intestine (the colon) and the rectum. Genetic alterations are often associated with progression from premalignant lesion (adenoma) to invasive adenocarcinoma. Risk factors for cancer of the colon and rectum include colon polyps, long-standing ulcerative colitis, and genetic family history. {ECO:0000269 PubMed:15930273, ECO:0000269 PubMed:15994075}. Note=The gene represented in this entry may be involved in disease pathogenesis.
  • Breast cancer (BC) [MIM:114480]: A common malignancy originating from breast epithelial tissue. Breast neoplasms can be distinguished by their histologic pattern. Invasive ductal carcinoma is by far the most common type. Breast cancer is etiologically and genetically heterogeneous. Important genetic factors have been indicated by familial occurrence and bilateral involvement. Mutations at more than one locus can be involved in different families or even in the same case. {ECO:0000269 PubMed:16353168}. Note=Disease susceptibility is associated with variations affecting the gene represented in this entry.
  • Ovarian cancer (OC) [MIM:167000]: The term ovarian cancer defines malignancies originating from ovarian tissue. Although many histologic types of ovarian tumors have been described, epithelial ovarian carcinoma is the most common form. Ovarian cancers are often asymptomatic and the recognized signs and symptoms, even of late-stage disease, are vague. Consequently, most patients are diagnosed with advanced disease. {ECO:0000269 PubMed:15520168}. Note=Disease susceptibility is associated with variations affecting the gene represented in this entry.
  • Hepatocellular carcinoma (HCC) [MIM:114550]: A primary malignant neoplasm of epithelial liver cells. The major risk factors for HCC are chronic hepatitis B virus (HBV) infection, chronic hepatitis C virus (HCV) infection, prolonged dietary aflatoxin exposure, alcoholic cirrhosis, and cirrhosis due to other causes. {ECO:0000269 PubMed:15608678}. Note=The gene represented in this entry may be involved in disease pathogenesis.
  • Keratosis, seborrheic (KERSEB) [MIM:182000]: A common benign skin tumor. Seborrheic keratoses usually begin with the appearance of one or more sharply defined, light brown, flat macules. The lesions may be sparse or numerous. As they initially grow, they develop a velvety to finely verrucous surface, followed by an uneven warty surface with multiple plugged follicles and a dull or lackluster appearance. {ECO:0000269 PubMed:17673550}. Note=The disease is caused by mutations affecting the gene represented in this entry.
  • Megalencephaly-capillary malformation-polymicrogyria syndrome (MCAP) [MIM:602501]: A syndrome characterized by a spectrum of anomalies including primary megalencephaly, prenatal overgrowth, brain and body asymmetry, cutaneous vascular malformations, digital anomalies consisting of syndactyly with or without postaxial polydactyly, connective tissue dysplasia involving the skin, subcutaneous tissue, and joints, and cortical brain malformations, most distinctively polymicrogyria. {ECO:0000269 PubMed:22729224, ECO:0000269 PubMed:26593112}. Note=The disease is caused by mutations affecting the gene represented in this entry.
  • Congenital lipomatous overgrowth, vascular malformations, and epidermal nevi (CLOVE) [MIM:612918]: A sporadically occurring, non-hereditary disorder characterized by asymmetric somatic hypertrophy and anomalies in multiple organs. It is defined by four main clinical findings: congenital lipomatous overgrowth, vascular malformations, epidermal nevi, and skeletal/spinal abnormalities. The presence of truncal overgrowth and characteristic patterned macrodactyly at birth differentiates CLOVE from other syndromic forms of overgrowth. {ECO:0000269 PubMed:22658544}. Note=The disease is caused by mutations affecting the gene represented in this entry.
  • Cowden syndrome 5 (CWS5) [MIM:615108]: A form of Cowden syndrome, a hamartomatous polyposis syndrome with age-related penetrance. Cowden syndrome is characterized by hamartomatous lesions affecting derivatives of ectodermal, mesodermal and endodermal layers, macrocephaly, facial trichilemmomas (benign tumors of the hair follicle infundibulum), acral keratoses, papillomatous papules, and elevated risk for development of several types of malignancy, particularly breast carcinoma in women and thyroid carcinoma in both men and women. Colon cancer and renal cell carcinoma have also been reported. Hamartomas can be found in virtually every organ, but most commonly in the skin, gastrointestinal tract, breast and thyroid. {ECO:0000269 PubMed:23246288}. Note=The disease is caused by mutations affecting the gene represented in this entry.

Additional Disease Information for PIK3CA

Genetic Association Database
(GAD)
Human Genome Epidemiology Navigator
(HuGE)
ATLAS of Genetics and Cytogenetics in Oncology and Haematology
genes like me logo Genes that share disorders with PIK3CA: view

No data available for Genatlas for PIK3CA Gene

Publications for PIK3CA Gene

  1. PIK3CA mutations mostly begin to develop in ductal carcinoma of the breast. (PMID: 19818761) Li H … Zhu H (Experimental and molecular pathology 2010) 3 22 44 58
  2. PIK3CA amplification is predictive of poor prognosis in Tunisian patients with nasopharyngeal carcinoma.