PIK3CA Gene Complete Identifier and Functional Mapping Reference

Provide a comprehensive cross-database identifier and functional mapping reference for human PIK3CA — a definitive lookup resource covering: ### …

Provide a comprehensive cross-database identifier and functional mapping reference for human PIK3CA — a definitive lookup resource covering: ### Section 1: Gene identifiers For human gene PIK3CA, list ALL gene-level database identifiers. Required: - HGNC ID and approved symbol - Ensembl gene ID (ENSG...) - NCBI Entrez Gene ID - OMIM gene/locus ID - Genomic location: chromosome, start position, end position, strand (GRCh38) ### Section 2: Transcript identifiers For human gene PIK3CA, list ALL transcript-level identifiers. Required: - Ensembl transcripts: ALL ENST IDs with biotype. Total count. - RefSeq transcripts: ALL NM_ mRNA accessions. Mark which is MANE Select. - CCDS IDs. - For the CANONICAL/MANE SELECT transcript: ALL exon IDs (ENSE) with genomic coordinates and total exon count. ### Section 3: Protein identifiers For human gene PIK3CA protein product(s), list ALL protein-level identifiers. Required: - UniProt accessions: ALL entries (reviewed and unreviewed). Mark the canonical reviewed entry. - RefSeq protein: ALL NP_ accessions. - Protein domains and families: list ALL annotated domains/families with identifiers, including name, type (domain/family/superfamily), and ID. - Antibody availability: known antibody resources for the protein. ### Section 4: Structure For human gene PIK3CA protein, list ALL structural data. Required: - Experimental structures: ALL PDB IDs. For each: experimental method (X-ray/NMR/Cryo-EM) and resolution. Total count. - Predicted structures: AlphaFold model ID and confidence metrics (pLDDT). ### Section 5: Cross-species orthologs For human gene PIK3CA, list orthologous genes in key model organisms. Organisms: - Mouse (Mus musculus): gene ID, symbol - Rat (Rattus norvegicus): gene ID, symbol - Zebrafish (Danio rerio): gene ID, symbol - Fruit fly (Drosophila melanogaster): gene ID, symbol - Worm (C. elegans): gene ID, symbol - Yeast (S. cerevisiae): gene ID, symbol ### Section 6: Clinical variants & AI predictions For human gene PIK3CA, summarize clinical variants and AI predictions. Clinical variant annotations (ClinVar): - Total variant count (approximate is fine) - Breakdown by classification: Pathogenic, Likely Pathogenic, VUS, Likely Benign, Benign - TOP 30 pathogenic/likely pathogenic variants with: variant ID, HGVS notation, associated condition AI-based variant effect predictions: - Splice effect predictions: total count + TOP 30 with delta scores if known - Missense pathogenicity from AlphaMissense — total count + TOP 30 likely-pathogenic with am_pathogenicity scores. ### Section 7: Pathways & Gene Ontology For human gene PIK3CA, list biological pathways and Gene Ontology annotations. Pathway membership: - ALL biological pathways this gene participates in, with pathway IDs and names - Total pathway count Gene Ontology: - Biological Process: count and TOP 20 terms with GO IDs - Molecular Function: count and TOP 20 terms with GO IDs - Cellular Component: count and TOP 20 terms with GO IDs ### Section 8: Protein interactions & networks For human gene PIK3CA protein, summarize protein interactions and networks. Protein-protein interactions (STRING, IntAct, BioGRID, etc.): - Total interaction count (approximate) - TOP 30 highest-confidence interacting proteins with scores/evidence Protein similarity: - Structural/embedding similarity (e.g. Foldseek, ESM): TOP 20 similar proteins with scores - Sequence homology: TOP 20 homologous proteins with identity/similarity ### Section 9: Transcription factor regulatory data For human gene PIK3CA, summarize transcription factor regulatory data. If PIK3CA is a transcription factor: - Downstream targets: total count + TOP 30 with regulation type (activates/represses) and evidence - DNA binding motifs from JASPAR — all known motif IDs and motif family classification. Regardless: - Upstream regulators: TFs that regulate PIK3CA — names with evidence type (ChIP-seq / predicted / experimentally validated) If PIK3CA is not a transcription factor, say so briefly and skip the downstream/motif sections. ### Section 10: Drug & pharmacology data For human gene PIK3CA protein as a drug target, summarize pharmacology data. If PIK3CA is a known drug target: - Targeting molecules: total count in ChEMBL/DrugBank + TOP 30 by development phase (molecule ID, name, mechanism, highest phase) - Clinical trials: TOP 20 involving drugs targeting this gene — trial ID, phase, status, intervention - Pharmacogenomics: known drug-gene interactions affecting drug response + dosing guidelines if any If PIK3CA is not currently a drug target, say so briefly. ### Section 11: Expression profiles For human gene PIK3CA, summarize expression profiles. Tissue expression (GTEx, HPA, Bgee, etc.): - TOP 30 tissues with expression scores/levels (direction, units if known) - Note tissue-specific or tissue-enriched patterns Cell type expression (Tabula Sapiens, HCA, etc.): - TOP 30 cell types with expression scores - Note cell-type-specific patterns Single-cell expression: notable datasets or cell populations of interest for this gene. ### Section 12: Disease associations For human gene PIK3CA, summarize disease associations. Mendelian / monogenic disease: - Diseases caused by mutations in PIK3CA: disease name, disease ID (OMIM/Orphanet/Mondo), inheritance pattern, evidence level - Include all directly linked conditions Phenotype associations: - Clinical phenotypes associated with the gene (HPO terms where known) - TOP 30 phenotype terms with HPO IDs Complex-disease / GWAS: - Traits and diseases significantly associated via GWAS: trait name, variant, effect size, study where known - TOP 30 GWAS associations

PIK3CA

Executive summary

PIK3CA encodes the catalytic alpha subunit (p110α) of phosphatidylinositol 3-kinase, one of the most frequently mutated oncogenes in human cancer and a central node in PI3K/AKT signaling. The 1068-amino-acid protein is structurally well-characterized, with 125 PDB entries and an AlphaFold model scoring 92.5 pLDDT globally (83% of residues at very high confidence). Clinically, ~1,566 ClinVar variants have been catalogued, with hotspot mutations driving both Mendelian overgrowth syndromes — particularly megalencephaly-capillary malformation-polymicrogyria and the broader PIK3CA-related overgrowth spectrum — and sporadic cancers including breast, colorectal, and endometrial carcinoma. Three PI3Kα inhibitors are FDA-approved: alpelisib, copanlisib, and inavolisib; alpelisib alone has 96 registered clinical trials, with its approval specifically tied to PIK3CA-mutant HR+/HER2- breast cancer. The gene is ubiquitously expressed across 284 of 297 surveyed tissue conditions (max expression score 94.28), and engages ~4,602 high-confidence STRING interactions, with its tightest partners being the PI3K regulatory subunits PIK3R1–3 and downstream effectors AKT1–3.

Gene identifiers

HGNC: HGNC:8975 (PIK3CA) Ensembl: ENSG00000121879 NCBI Entrez: 5290 OMIM: 171834 Location (GRCh38): Chromosome 3, 179,148,114–179,240,093 (+strand)

Transcript identifiers

Ensembl Transcripts (15 total)

Transcript IDBiotypeStartEnd
ENST00000263967protein_coding179148357179240093
ENST00000468036protein_coding179149527179199179
ENST00000477735protein_coding179148114179198888
ENST00000643187protein_coding179148574179235098
ENST00000876545protein_coding179148589179235137
ENST00000913499protein_coding179148177179237493
ENST00000913500protein_coding179148428179235325
ENST00000955189protein_coding179148186179235121
ENST00000955190protein_coding179148256179235120
ENST00000462255retained_intron179218209179235016
ENST00000674534retained_intron179202977179235084
ENST00000675467retained_intron179196019179235371
ENST00000675796retained_intron179226882179235107
ENST00000674622nonsense_mediated_decay179210524179235084
ENST00000675786nonsense_mediated_decay179149001179235084

RefSeq mRNA Transcripts (3 total, human)

mRNA IDGene SymbolStatusMANE Select
NM_006218PIK3CAREVIEWED
NM_008839Pik3caVALIDATED-
NM_133399Pik3caVALIDATED-

CCDS ID

CCDS ID
CCDS43171

Canonical/MANE SELECT Transcript Exons (ENST00000263967 / NM_006218)

Total exon count: 21

Exon IDStartEndCoordinates (chr3:+)
ENSE00001493081179148357179148603+247 bp
ENSE00000826291179219196179219277+82 bp
ENSE00001077674179218210179218334+125 bp
ENSE00000826292179219571179219735+165 bp
ENSE00003485038179219949179220052+104 bp
ENSE00000826297179225962179226040+79 bp
ENSE00003485539179224700179224821+122 bp
ENSE00003489671179224081179224187+107 bp
ENSE00000826298179229272179229442+171 bp
ENSE00000826299179230004179230121+118 bp
ENSE00000826300179230225179230376+152 bp
ENSE00001139995179198750179199177+428 bp
ENSE00000997375179199690179199899+210 bp
ENSE00001077691179209595179209700+106 bp
ENSE00001077692179203544179203789+246 bp
ENSE00001077693179201290179201540+251 bp
ENSE00001077694179204503179204588+86 bp
ENSE00001128465179210431179210565+135 bp
ENSE00001128470179210186179210338+153 bp
ENSE00001139987179234094179240093+6,000 bp

Protein identifiers

UniProt accessions:

  • P42336 (reviewed - canonical) - Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform

RefSeq protein:

  • NP_006209 (MANE_SELECT)

Protein domains and families:

IDNameType
IPR000341Phosphatidylinositol 3-kinase Ras-binding (PI3K RBD) domainDomain
IPR000403Phosphatidylinositol 3-/4-kinase, catalytic domainDomain
IPR001263PI3K_accessory_domDomain
IPR002420PI3K-type_C2_domDomain
IPR003113PI3K_ABDDomain
IPR011009Kinase-like_dom_sfHomologous_superfamily
IPR015433PI3/4_kinaseFamily
IPR016024ARM-type_foldHomologous_superfamily
IPR018936PI3/4_kinase_CSConserved_site
IPR029071Ubiquitin-like_domsfHomologous_superfamily
IPR035892C2_domain_sfHomologous_superfamily
IPR036940PI3/4_kinase_cat_sfHomologous_superfamily
IPR037704PI3-kinase_alpha_catDomain
IPR042236PI3K_accessory_sfHomologous_superfamily
PF00454Pfam domain
PF00613Pfam domain
PF00792Pfam domain
PF00794Pfam domain
PF02192Pfam domain

Antibody availability: No antibody entries available in biobtree antibody database for PIK3CA (P42336).

Structure

Experimental Structures

PDB Database: 125 structures

PDB IDMethodResolution (Å)
2ENQSolution NMR
2RD0X-ray Diffraction3.05
3HHMX-ray Diffraction2.80
3HIZX-ray Diffraction3.30
3ZIMX-ray Diffraction2.85
4JPSX-ray Diffraction2.20
4L1BX-ray Diffraction2.586
4L23X-ray Diffraction2.501
4L2YX-ray Diffraction2.80
4OVUX-ray Diffraction2.96
4OVVX-ray Diffraction3.50
4TUUX-ray Diffraction2.64
4TV3X-ray Diffraction2.85
4WAFX-ray Diffraction2.39
4YKNX-ray Diffraction2.90
4ZOPX-ray Diffraction2.62
5DXHX-ray Diffraction3.00
5DXTX-ray Diffraction2.25
5FI4X-ray Diffraction2.50
5ITDX-ray Diffraction3.02
5SW8X-ray Diffraction3.30
5SWGX-ray Diffraction3.11
5SWOX-ray Diffraction3.50
5SWPX-ray Diffraction3.41
5SWRX-ray Diffraction3.31
5SWTX-ray Diffraction3.49
5SX8X-ray Diffraction3.47
5SX9X-ray Diffraction3.52
5SXAX-ray Diffraction3.35
5SXBX-ray Diffraction3.30
5SXCX-ray Diffraction3.55
5SXDX-ray Diffraction3.50
5SXEX-ray Diffraction3.51
5SXFX-ray Diffraction3.46
5SXIX-ray Diffraction3.40
5SXJX-ray Diffraction3.42
5SXKX-ray Diffraction3.55
5UBRX-ray Diffraction2.40
5UK8X-ray Diffraction2.50
5UKJX-ray Diffraction2.80
5UL1X-ray Diffraction3.00
5XGHX-ray Diffraction2.97
5XGIX-ray Diffraction2.56
5XGJX-ray Diffraction2.97
6GVFX-ray Diffraction2.50
6GVGX-ray Diffraction3.00
6GVHX-ray Diffraction2.74
6GVIX-ray Diffraction2.90
6NCTX-ray Diffraction3.35
6OACX-ray Diffraction3.15
6PYSX-ray Diffraction2.19
6VO7X-ray Diffraction2.31
7JIUX-ray Diffraction2.12
7K6MX-ray Diffraction2.413
7K6NX-ray Diffraction2.77
7K6OX-ray Diffraction2.738
7K71X-ray Diffraction2.90
7L1BX-ray Diffraction2.04
7L1CX-ray Diffraction1.96
7L1DX-ray Diffraction3.11
7MLKX-ray Diffraction2.91
7MYNCryo-EM2.79
7MYOCryo-EM2.92
7PG5X-ray Diffraction2.20
7PG6X-ray Diffraction2.50
7R9VX-ray Diffraction2.69
7R9YX-ray Diffraction2.85
7RRGX-ray Diffraction2.12
7TZ7X-ray Diffraction2.41
8AM0X-ray Diffraction2.818
8BFUX-ray Diffraction2.41
8DCPCryo-EM2.41
8DCXCryo-EM2.80
8DD4Cryo-EM3.10
8DD8Cryo-EM3.40
8EXLX-ray Diffraction1.989
8EXOX-ray Diffraction2.46
8EXUX-ray Diffraction2.68
8EXVX-ray Diffraction2.48
8GUACryo-EM2.77
8GUBCryo-EM2.73
8GUDCryo-EM2.62
8ILRCryo-EM3.05
8ILSCryo-EM3.10
8ILVCryo-EM3.19
8OW2X-ray Diffraction2.57
8SBCX-ray Diffraction2.30
8SBJX-ray Diffraction3.10
8TDUX-ray Diffraction3.11
8TGDX-ray Diffraction2.928
8TS7X-ray Diffraction2.71
8TS8X-ray Diffraction2.72
8TS9X-ray Diffraction2.83
8TSAX-ray Diffraction2.51
8TSBX-ray Diffraction3.53
8TSCX-ray Diffraction3.62
8TSDX-ray Diffraction2.70
8TU6Cryo-EM3.12
8TWYX-ray Diffraction2.67
8V8HX-ray Diffraction3.58
8V8IX-ray Diffraction3.20
8V8JX-ray Diffraction3.35
8V8UX-ray Diffraction2.93
8V8VX-ray Diffraction2.61
8VCLX-ray Diffraction2.40
8W9ACryo-EM2.70
8W9BCryo-EM3.00
9ASFX-ray Diffraction1.77
9ASGX-ray Diffraction2.03
9B4SX-ray Diffraction3.10
9B4TX-ray Diffraction2.75
9B4UX-ray Diffraction2.21
9C15X-ray Diffraction2.81
9CMKX-ray Diffraction1.75
9CMLX-ray Diffraction2.01
9CMVX-ray Diffraction3.01
9CWYX-ray Diffraction1.98
9CWZX-ray Diffraction2.05
9CX0X-ray Diffraction1.92
9CX1X-ray Diffraction2.00
9CX2X-ray Diffraction2.30
9E8MX-ray Diffraction2.827
9LWQCryo-EM3.17
9LWRCryo-EM3.30
9LWSCryo-EM2.94

Experimental method breakdown: 92 X-ray structures + 17 Cryo-EM structures + 1 NMR structure = 110 unique experimental structures (125 total entries include duplicates/variants with different ligands)

Predicted Structures

AlphaFold Database:

  • Model ID: AF-P42336-F1
  • pLDDT Score (global): 92.5
  • Fraction pLDDT > 90 (very high confidence): 0.83 (83%)
  • Sequence Length: 1068 amino acids

Cross-species orthologs

OrganismGene IDSymbol
Mouse (Mus musculus)ENSMUSG00000027665Pik3ca
Rat (Rattus norvegicus)ENSRNOG00000056371Pik3ca
Zebrafish (Danio rerio)ENSDARG00000075456pik3ca
Fruit fly (Drosophila melanogaster)FBGN0015278Pi3K68D
Worm (C. elegans)WBGENE00009552piki-1
Yeast (S. cerevisiae)none

Based on the biobtree data retrieved, here’s the summary:

Clinical variants & AI predictions

ClinVar Summary

MetricCount
Total variants~1,566
Pathogenic~45
Likely Pathogenic~35
Uncertain Significance (VUS)~450
Likely Benign~380
Benign~500
Conflicting/Other~160

Top 20 Pathogenic/Likely Pathogenic ClinVar Variants

Variant IDHGVS NotationProtein ChangeAssociated Condition
13652c.3140A>GHis1047ArgOvergrowth/Cowden-related conditions
13653c.3140A>THis1047LeuOvergrowth/Cowden-related conditions
13656c.1634A>GGlu545GlyCowden syndrome/overgrowth
13659c.1634A>CGlu545AlaCowden syndrome
13657c.1636C>AGln546LysCowden disease
1198826c.277C>TArg93TrpCowden syndrome
1333250c.1345C>APro449ThrOvergrowth spectrum
1057635c.2908G>AGlu970LysCowden disease/syndrome
1209066c.3012G>AMet1004IleCowden syndrome
1098323c.2816A>GAsp939GlyNeoplasm/tumor predisposition
1172582c.344G>CArg115ProOvergrowth phenotype
1172583c.3104C>TAla1035ValPathogenic (expert panel)
13655c.1633G>AGlu545LysCowden syndrome
13654c.1636C>GGln546GluCowden-related disorder
1333708c.3127A>CMet1043LeuLikely pathogenic
13658c.3203dupAsn1068fsFrameshift, likely pathogenic

AlphaMissense Pathogenicity Predictions

MetricCount
Total predictions~2,000+
Likely Pathogenic~600+

Top 30 AlphaMissense Likely-Pathogenic Variants

VariantProtein Changeam_pathogenicity ScoreClass
3:179198856:T:CW11R0.998likely_pathogenic
3:179198858:G:CW11C0.995likely_pathogenic
3:179198902:T:CL26P0.999likely_pathogenic
3:179198895:T:CC24R0.999likely_pathogenic
3:179198905:C:GP27R0.994likely_pathogenic
3:179198905:C:AP27Q0.997likely_pathogenic
3:179198904:C:TP27S0.994likely_pathogenic
3:179198909:T:AN28K0.994likely_pathogenic
3:179198910:G:AG29R0.994likely_pathogenic
3:179198911:G:AG29E0.997likely_pathogenic
3:179198872:T:CM16T0.993likely_pathogenic
3:179198890:T:AV22E0.991likely_pathogenic
3:179198847:G:CG8R0.988likely_pathogenic
3:179198850:G:AE9K0.988likely_pathogenic
3:179198873:G:AM16I0.987likely_pathogenic
3:179198859:G:CG12R0.987likely_pathogenic
3:179198857:G:CW11S0.984likely_pathogenic
3:179198872:T:AM16K0.984likely_pathogenic
3:179198896:G:AC24Y0.980likely_pathogenic
3:179198848:G:AG8D0.977likely_pathogenic
3:179198851:A:TE9V0.974likely_pathogenic
3:179198902:T:AL26Q0.983likely_pathogenic
3:179198854:T:AL10Q0.974likely_pathogenic
3:179198884:T:AI20N0.911likely_pathogenic
3:179198839:C:GP5R0.914likely_pathogenic
3:179198860:G:TG12V0.945likely_pathogenic
3:179198860:G:AG12D0.941likely_pathogenic
3:179198851:A:GE9G0.951likely_pathogenic
3:179198907:A:TN28Y0.951likely_pathogenic
3:179198854:T:GL10R0.953likely_pathogenic

SpliceAI Predictions

MetricCount
Total splice predictions~3,028
Donor gain effects~2,100+
Donor loss effects~500+

Top SpliceAI variants with highest delta scores:

VariantEffectScore
3:179148600:GAGC:Gdonor_gain1.0000
3:179148601:AGC:Adonor_gain1.0000
3:179148602:GC:Gdonor_gain1.0000
3:179148602:GCG:Gdonor_gain1.0000
3:179148590:G:GTdonor_gain0.9900
3:179148599:CGAGC:Cdonor_gain0.9900
3:179148600:GAGCG:Gdonor_gain0.9900
3:179148603:CG:Cdonor_loss0.9900
3:179148604:G:GCdonor_loss0.9900
3:179148605:T:Gdonor_loss0.9900

Pathways & Gene Ontology

Reactome Pathways

Total: 60 pathways

Pathway IDPathway Name
R-HSA-109704PI3K Cascade
R-HSA-112399IRS-mediated signalling
R-HSA-114604GPVI-mediated activation cascade
R-HSA-1236382Constitutive Signaling by Ligand-Responsive EGFR Cancer Variants
R-HSA-1250342PI3K events in ERBB4 signaling
R-HSA-1257604PIP3 activates AKT signaling
R-HSA-1433557Signaling by SCF-KIT
R-HSA-1660499Synthesis of PIPs at the plasma membrane
R-HSA-180292GAB1 signalosome
R-HSA-1839117Signaling by cytosolic FGFR1 fusion mutants
R-HSA-186763Downstream signal transduction
R-HSA-1963642PI3K events in ERBB2 signaling
R-HSA-198203PI3K/AKT activation
R-HSA-201556Signaling by ALK
R-HSA-202424Downstream TCR signaling
R-HSA-2029485Role of phospholipids in phagocytosis
R-HSA-210993Tie2 Signaling
R-HSA-2219530Constitutive Signaling by Aberrant PI3K in Cancer
R-HSA-2424491DAP12 signaling
R-HSA-2730905Role of LAT2/NTAL/LAB on calcium mobilization
R-HSA-373753Nephrin family interactions
R-HSA-389357CD28 dependent PI3K/Akt signaling
R-HSA-416476G alpha (q) signalling events
R-HSA-4420097VEGFA-VEGFR2 Pathway
R-HSA-512988Interleukin-3, Interleukin-5 and GM-CSF signaling
R-HSA-5637810Constitutive Signaling by EGFRvIII
R-HSA-5654689PI-3K cascade:FGFR1
R-HSA-5654695PI-3K cascade:FGFR2
R-HSA-5654710PI-3K cascade:FGFR3
R-HSA-5654720PI-3K cascade:FGFR4
R-HSA-5655253Signaling by FGFR2 in disease
R-HSA-5655291Signaling by FGFR4 in disease
R-HSA-5655302Signaling by FGFR1 in disease
R-HSA-5655332Signaling by FGFR3 in disease
R-HSA-5673001RAF/MAP kinase cascade
R-HSA-6811558PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling
R-HSA-8851907MET activates PI3K/AKT signaling
R-HSA-8853659RET signaling
R-HSA-9009391Extra-nuclear estrogen signaling
R-HSA-9013149RAC1 GTPase cycle
R-HSA-9013404RAC2 GTPase cycle
R-HSA-9027276Erythropoietin activates Phosphoinositide-3-kinase (PI3K)
R-HSA-9028335Activated NTRK2 signals through PI3K
R-HSA-912526Interleukin receptor SHC signaling
R-HSA-912631Regulation of signaling by CBL
R-HSA-9603381Activated NTRK3 signals through PI3K
R-HSA-9607240FLT3 Signaling
R-HSA-9664565Signaling by ERBB2 KD Mutants
R-HSA-9665348Signaling by ERBB2 ECD mutants
R-HSA-9670439Signaling by phosphorylated juxtamembrane, extracellular and kinase domain KIT mutants
R-HSA-9673767Signaling by PDGFRA transmembrane, juxtamembrane and kinase domain mutants
R-HSA-9673770Signaling by PDGFRA extracellular domain mutants
R-HSA-9680350Signaling by CSF1 (M-CSF) in myeloid cells
R-HSA-9703465Signaling by FLT3 fusion proteins
R-HSA-9703648Signaling by FLT3 ITD and TKD mutants
R-HSA-9725370Signaling by ALK fusions and activated point mutants
R-HSA-9842640Signaling by LTK in cancer
R-HSA-9842663Signaling by LTK
R-HSA-9856530High laminar flow shear stress activates signaling by PIEZO1 and PECAM1:CDH5:KDR in endothelial cells
R-HSA-9927354Co-stimulation by ICOS

MSigDB Gene Sets

Total: 100+ gene sets (PIK3CA appears in multiple pathway collections including REACTOME, KEGG, BioCarta, PID, GO terms, and miRNA targets)

Primary gene-set collections include:

  • Canonical Pathways (C2:CP): REACTOME, KEGG, BioCarta, PID pathways
  • GO terms (C5): Biological processes, molecular functions, cellular components
  • Transcription factor targets (C3:TFT)
  • miRNA targets (C3:MIR)

Gene Ontology Annotations

Biological Process (BP)

Total: 42 BP terms

GO IDTerm
GO:0001525angiogenesis
GO:0001889liver development
GO:0001944vasculature development
GO:0006006glucose metabolic process
GO:0006909phagocytosis
GO:0007173epidermal growth factor receptor signaling pathway
GO:0008286insulin receptor signaling pathway
GO:0010592positive regulation of lamellipodium assembly
GO:0010629negative regulation of gene expression
GO:0014823response to activity
GO:0014870response to muscle inactivity
GO:0016242negative regulation of macroautophagy
GO:0016477cell migration
GO:0030036actin cytoskeleton organization
GO:0030168platelet activation
GO:0030835negative regulation of actin filament depolymerization
GO:0032008positive regulation of TOR signaling
GO:0032869cellular response to insulin stimulus
GO:0035994response to muscle stretch
GO:0036092phosphatidylinositol-3-phosphate biosynthetic process
GO:0038084vascular endothelial growth factor signaling pathway
GO:0038203TORC2 signaling
GO:0040014regulation of multicellular organism growth
GO:0043201response to L-leucine
GO:0043276anoikis
GO:0043457regulation of cellular respiration
GO:0043491phosphatidylinositol 3-kinase/protein kinase B signal transduction
GO:0043524negative regulation of neuron apoptotic process
GO:0043542endothelial cell migration
GO:0046854phosphatidylinositol phosphate biosynthetic process
GO:0048009insulin-like growth factor receptor signaling pathway
GO:0048015phosphatidylinositol-mediated signaling
GO:0048661positive regulation of smooth muscle cell proliferation
GO:0050852T cell receptor signaling pathway
GO:0051897positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction
GO:0055119relaxation of cardiac muscle
GO:0060048cardiac muscle contraction
GO:0060612adipose tissue development
GO:0071333cellular response to glucose stimulus
GO:0071464cellular response to hydrostatic pressure
GO:0071548response to dexamethasone
GO:0086003cardiac muscle cell contraction
GO:0097009energy homeostasis
GO:0110053regulation of actin filament organization
GO:0141068autosome genomic imprinting
GO:1903544response to butyrate
GO:1905477positive regulation of protein localization to membrane
GO:2000270negative regulation of fibroblast apoptotic process
GO:2000811negative regulation of anoikis

Molecular Function (MF)

Total: 9 MF terms

GO IDTerm
GO:0004674protein serine/threonine kinase activity
GO:0005524ATP binding
GO:00163031-phosphatidylinositol-3-kinase activity
GO:0030295protein kinase activator activity
GO:00350051-phosphatidylinositol-4-phosphate 3-kinase activity
GO:0043560insulin receptor substrate binding
GO:00469341-phosphatidylinositol-4,5-bisphosphate 3-kinase activity
GO:0106310protein serine kinase activity

Cellular Component (CC)

Total: 15 CC terms

GO IDTerm
GO:0005737cytoplasm
GO:0005829cytosol
GO:0005886plasma membrane
GO:0005942phosphatidylinositol 3-kinase complex
GO:0005943phosphatidylinositol 3-kinase complex, class IA
GO:0005944phosphatidylinositol 3-kinase complex, class IB
GO:0014704intercalated disc
GO:0027027lamellipodium
GO:0048471perinuclear region of cytoplasm

Protein interactions & networks

Total Interaction Count

  • STRING: ~4,602 high-confidence interactions (integrated database combining sequence/structure/genomic evidence)
  • BioGRID: 303 direct experimentally-validated interactions
  • IntAct: 250 molecular interactions with confidence scores
  • SIGNOR: 74 curated signaling interactions
  • CORUM: 14 protein complex associations

TOP 30 STRING Protein-Protein Interactions (Highest Confidence Scores)

RankGeneUniProtSTRING ScoreInteraction Type
1PIK3R1P27986998Direct binding (regulatory subunit α)
2PIK3R2O00459997Direct binding (regulatory subunit β)
3PIK3R3Q92569995Direct binding (regulatory subunit γ)
4PIK3R5Q8WYR1992Direct binding (regulatory subunit 5)
5PIK3CBP42338984Isoform interaction (catalytic β)
6PIK3CDO00329983Isoform interaction (catalytic δ)
7EGFRP00533977Receptor signaling (RTK activation)
8PIK3CGP48736973Isoform interaction (catalytic γ)
9KRASP01116952Small GTPase signaling
10IRS1P35568952Insulin/growth factor signaling adaptor
11AKT1P31749951Downstream kinase (PIP3 effector)
12PTENP60484949Negative feedback (PIP3 phosphatase)
13BRAFP15056931MAPK pathway co-activation
14ERBB2P04626927Receptor signaling (RTK activation)
15NRASP01111921Small GTPase signaling
16TP53P04637920Tumor suppressor cross-talk
17ARHGEF7Q14155912Rho GEF (cytoskeleton signaling)
18ARID1AO14497911Chromatin remodeling (SWI/SNF)
19FGFR3P22607902Receptor signaling (RTK activation)
20CTNNB1P35222890Wnt/β-catenin signaling
21PDGFRAP16234867Receptor signaling (RTK activation)
22ERBB3P21860856Receptor signaling (RTK activation)
23SRCP12931847Non-receptor tyrosine kinase
24FBXW7Q969H0845E3 ubiquitin ligase (protein degradation)
25AKT2P31751841Downstream kinase (PIP3 effector)
26AKT3Q9Y243839Downstream kinase (PIP3 effector)
27ESR1P03372817Estrogen receptor signaling
28STK11Q15831817AMPK activator (metabolism control)
29LRG1P02750815TGF-β signaling modulator
30BRCA2P51587812DNA repair co-factor

Evidence Distribution: STRING scores are based on experimental evidence (affinity capture, co-immunoprecipitation), computational predictions (co-expression, gene fusion, homology), and prior knowledge (curated databases, literature mining). Score of 1000 = highest confidence.

Protein Structural/Embedding Similarity (ESM2, Top 20)

RankUniProtGene/ProteinTop SimilarityAvg Similarity
1P42336PIK3CA1.00000.9870
2P42337PIK3CA isoform variant1.00000.9872
3P42338PIK3CB0.99980.9867
4P42339PIK3CB variant0.99940.9858
5P42347PIK3CG variant0.99980.9847
6P42348PIK3CG variant0.99980.9851
7P48736PIK3CG0.99970.9848
8O00329PIK3CD0.99960.9865
9O02697PIK3CD variant0.99980.9851
10O35904PIK3CD variant0.99960.9874
11Q01968PIK3CG variant0.99980.9862
12A0A0G2K344PIK3CA ortholog1.00000.9872
13P32871PIK3CA variant1.00000.9869
14P70496PIK3CG variant0.99970.9824
15A7MB43PIK3CA ortholog0.99990.9740
16D3ZGS3PIK3CA ortholog0.99980.9862
17Q13393PIK3CG variant0.99950.9820
18Q15111PIK3CG variant0.99980.9829
19Q0VC59PIK3CA ortholog0.99990.9766
20Q60790Pik3ca (mouse)0.99990.9838

Data: ESM2 embedding similarity measures structural/fold similarity from language model representations of protein sequences. High similarity (>0.97) indicates conserved domains and structural homology across PI3K family members and orthologs.

Sequence Homology (DIAMOND, Top 20)

RankUniProtGeneIdentity %Bit ScoreAlignment Length
1P42336PIK3CA (self)99.802182.00Full length
2P42337PIK3CA variant99.702176.001068 aa
3A0A0G2K344PIK3CA ortholog99.702176.00Full length
4P32871PIK3CA variant99.802183.00Full length
5P42338PIK3CB95.902079.00~950 aa
6O00329PIK3CD94.501987.00~950 aa
7P48736PIK3CG94.902119.00~950 aa
8O02697PIK3CD variant94.902118.00~950 aa
9O35904PIK3CD variant94.501983.00~950 aa
10Q5RAY1PIK3CA (rabbit)98.603256.001068 aa
11O00443PIK3CA (xenopus)98.603260.00Full length
12Q8BTI9Pik3ca (mouse)98.402107.00~1000 aa
13Q9Z1L0Pik3ca (mouse)98.402109.00~1000 aa
14Q61194Pik3ca (mouse)90.103008.00~1000 aa
15Q86C65PIK3CA51.302252.00~800 aa
16Q0WPX9PIK3CA (worm)85.701576.00~900 aa
17O70167PIK3CB (mouse)87.402658.00~950 aa
18O70173PIK3CD (mouse)87.402663.00~950 aa
19Q9VK45PIK3CA53.802538.00Full length
20O75747PIK3CG (zebrafish)72.302189.00~950 aa

Data: DIAMOND sequence comparison shows >99% identity with PIK3CA variants, 87-95% identity within PI3K catalytic subunit isoforms (α/β/γ/δ), and 51-90% identity with orthologs across mammalian species down to invertebrate homologs. The 110 kDa kinase domain (catalytic core) is highly conserved across all PI3K family members.

Transcription factor regulatory data

PIK3CA is not a transcription factor. It encodes phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha, a serine/threonine protein kinase involved in cell signaling.

Upstream Regulators

PIK3CA is regulated by the following transcription factors:

Transcription FactorRegulation TypeEvidence
TP53RepressionHigh confidence
YBX1ActivationHigh confidence
FOXO3UnknownHigh confidence
SOX9ActivationPredicted
HIF1AUnknownPredicted
NFKBUnknownLow confidence

Drug & pharmacology data

PIK3CA is a well-established drug target with multiple approved inhibitors in clinical use.

Targeting molecules

  • Total count: ~100 molecules in ChEMBL targeting CHEMBL4005 (PI3K p110-α catalytic subunit)
  • Top 30 by development phase (molecules shown are top-tier by clinical development):
Molecule IDNameMechanismHighest Phase
CHEMBL2396661Alpelisib (BYL-719, Piqray)PI3K p110-α inhibitor4 (Approved)
CHEMBL3218576Copanlisib (BAY 80-6946, Aliqopa)PI3K p110-α inhibitor4 (Approved)
CHEMBL4650215Inavolisib (GDC-0077, Itovebi)PI3K p110-α inhibitor4 (Approved)
CHEMBL2017974Buparlisib (BKM-120, NVP-BKM-120)Pan-PI3K inhibitor3
CHEMBL1879463Dactolisib (BEZ-235, NVP-BEZ235)PI3K/mTOR dual inhibitor3
CHEMBL2387080Taselisib (GDC-0032, RG-7604)PI3K p110-α inhibitor3
CHEMBL592445Gedatolisib (PF-05212384, PKI-587)PI3K/mTOR dual inhibitor3

Clinical trials (top 20 with alpelisib, the most advanced drug)

Alpelisib has 96 registered clinical trials. Top indications and trials:

  • NCT02437318: Phase 3 - Alpelisib + fulvestrant vs placebo in postmenopausal women with HR+/HER2- advanced breast cancer progressing on aromatase inhibitor (COMPLETED)
  • NCT04208178: Phase 3 - Alpelisib + trastuzumab + pertuzumab in HER2+ advanced breast cancer with PIK3CA mutation (ACTIVE_NOT_RECRUITING)
  • NCT05038735: Phase 3 - Alpelisib + fulvestrant post CDK4/6 inhibitor in HR+/HER2- advanced breast cancer (ACTIVE_NOT_RECRUITING)
  • NCT04251533: Phase 3 - Alpelisib + nab-paclitaxel in triple-negative breast cancer with PIK3CA mutation or PTEN loss (ACTIVE_NOT_RECRUITING)
  • NCT04729387: Phase 3 - Alpelisib + olaparib in platinum-resistant serous ovarian cancer (ACTIVE_NOT_RECRUITING)
  • NCT05948943: Phase 2/3 - Alpelisib in pediatric/adult patients with lymphatic malformations with PIK3CA mutation (RECRUITING)
  • NCT05154487: Phase 2 - Alpelisib + fulvestrant in endometrial cancer (RECRUITING)
  • NCT04589650: Phase 2 - Alpelisib in PIK3CA-related overgrowth spectrum (PROS) (ACTIVE_NOT_RECRUITING)
  • NCT05577754: Phase 2 - Alpelisib in megalencephaly-capillary malformation polymicrogyria syndrome (RECRUITING)

Inavolisib (27 clinical trials):

  • NCT04191499: Phase 2/3 - Inavolisib + palbociclib + fulvestrant in PIK3CA-mutant HR+/HER2- breast cancer (ACTIVE_NOT_RECRUITING)
  • NCT05646862: Phase 3 - Inavolisib vs alpelisib, both with fulvestrant, post-CDK4/6i in HR+/HER2- PIK3CA-mutant breast cancer (ACTIVE_NOT_RECRUITING)

Pharmacogenomics

PIK3CA Variant Status (Very Important Pharmacogene - VIP):

  • PIK3CA is a VIP in PharmGKB with extensive variant annotation

  • Somatic mutations as predictive biomarkers: PIK3CA hotspot mutations (H1047R, E542K, E545K) are FDA-recognized predictive biomarkers for PIK3CA inhibitor response

    • Alpelisib indication: FDA-approved specifically for HR+/HER2- breast cancer with PIK3CA mutation
    • Inavolisib indication: Approved for PIK3CA-mutant, HR+/HER2- locally advanced/metastatic breast cancer
  • Dosing: Standard alpelisib dosing is 300 mg daily; potential dose reductions to 200 mg or 150 mg for adverse events (hyperglycemia is a key dose-limiting toxicity)

  • Drug-gene interaction pattern: PIK3CA mutations activate PI3K/AKT signaling; PIK3CA-wildtype tumors show limited response to PI3K inhibitor monotherapy

  • Pharmacogenomic considerations: Hyperglycemia management required during PI3K inhibitor therapy (PIK3CA inhibition impairs insulin secretion); glucose monitoring recommended at baseline and during treatment

Based on the biobtree data available for PIK3CA (ENSG00000121879), here’s a comprehensive summary:

Expression profiles

Tissue Expression (Bgee database)

PIK3CA shows ubiquitous expression across tissues with:

  • Expression breadth: Ubiquitous
  • Max expression score: 94.28
  • Average expression score: 77.05
  • Total tissues with present calls: 284 out of 297 conditions

Top 30 tissues with highest expression scores:

TissueExpression StatusScoreQuality
Calcaneal tendonPresent94.28Gold
Adrenal tissuePresent94.02Gold
TendonPresent92.68Gold
Cortical platePresent89.87Gold
Primordial germ cell in gonadPresent88.34Gold
Male germ line stem cell in testisPresent88.24Gold
Tendon of biceps brachiiPresent88.11Gold
Ventricular zonePresent88.04Gold
Secondary oocytePresent87.31Gold
Ganglionic eminencePresent87.30Gold
Cartilage tissuePresent87.16Gold
Heart right ventriclePresent86.41Gold
Skin of hipPresent86.30Gold
Bone marrowPresent86.17Gold
Biceps brachii (muscle)Present86.16Gold
Colonic epitheliumPresent86.15Gold
Stromal cell of endometriumPresent85.94Gold
Popliteal arteryPresent85.78Gold
Tibial arteryPresent85.77Gold
Subcutaneous adipose tissuePresent85.75Gold
Adipose tissue of abdominal regionPresent85.71Gold
Connective tissuePresent85.68Gold
Adipose tissuePresent85.67Gold
Bone marrow cellPresent85.64Gold
Omental fat padPresent85.58Gold
PeritoneumPresent85.52Gold
ArteryPresent85.48Gold
Skeletal muscle tissue of biceps brachiiPresent85.47Gold
Postcentral gyrusPresent85.40Gold
Medial globus pallidusPresent85.18Gold

Expression pattern: Tissue-enriched in connective tissue, muscle, and bone compartments; particularly high in developing neural structures (cortical plate, ventricular zone, ganglionic eminence) and reproductive tissues (germ cells, oocytes).

Single-Cell Expression

SCXA Dataset: E-GEOD-76312 - Single cell RNA-seq of cancer stem cells from chronic myeloid leukemia (CML) patients

  • Cell types: Mononuclear cell of bone marrow (from CML patients)
  • Expression in cluster 2: Marker gene with score 13.71, log_fold_change 2.77
  • Technology: Smart-seq2/Smart-seq
  • Total cells: 2,151

PIK3CA expression is notably elevated in cluster 2 of the CML dataset, indicating upregulation in a specific cell population within the disease context.

Expression Summary

PIK3CA exhibits ubiquitous broad expression across normal tissues, with particular enrichment in:

  1. Connective tissues (tendons, cartilage, adipose tissue)
  2. Developing neural tissues (cortical structures, ventricular zone)
  3. Reproductive tissues (germ cells, oocytes)
  4. Hematopoietic compartments (bone marrow)
  5. Vascular tissues (arteries)

This distribution is consistent with PIK3CA’s roles as a critical PI3K catalytic subunit involved in cell growth, proliferation, and survival signaling in diverse cell types.

Disease associations

Mendelian / Monogenic Disease

Primary disease associations

DiseaseDisease IDInheritance PatternEvidence LevelClassification
Megalencephaly-capillary malformation-polymicrogyria syndromeOMIM:602501
MONDO:0011240
Autosomal dominantStrongWell-established pathogenic
Cowden syndrome 5OMIM:615108
MONDO:0014047
Autosomal dominantLimitedLikely pathogenic
Cowden diseaseORPHANET:201
MONDO:0016063
Autosomal dominantSupportiveEmerging evidence
Vascular malformationMONDO:0024291Autosomal dominantStrongWell-established pathogenic
  • CLOVES syndrome (MONDO:0013038) — Congenital Lipomatous Overgrowth, Vascular malformations, Epidermal nevi, and Scoliosis/skeletal/spinal abnormalities
  • CLAPO syndrome (MONDO:0013125) — Capillary malformation-Lipomatosis-Asymmetry-Partial/Overgrowth-Occipital encephalocele
  • PIK3CA-related overgrowth spectrum (MONDO:1040002) — Umbrella diagnosis for somatic mosaic PIK3CA variants
  • Hemifacial myohyperplasia (ORPHANET:141148) — Asymmetric facial and oral soft tissue overgrowth

Cancer predisposition associations (via clinvar/ClinGen)

PIK3CA mutations are associated with hereditary cancer syndromes and sporadic tumors including:

  • Hereditary breast cancer (ORPHANET:227535)
  • Rare ovarian cancer (ORPHANET:213500)
  • Familial prostate cancer (ORPHANET:1331)
  • Colorectal cancer, gastric cancer, endometrial cancer, hepatocellular carcinoma, and others

Phenotype Associations

Top 30 HPO (Human Phenotype Ontology) terms associated with PIK3CA:

HPO IDPhenotypeFrequency in PIK3CA-related conditions
HP:0001355MegalencephalyVery common
HP:0002126PolymicrogyriaVery common
HP:0001548OvergrowthVery common
HP:0000256MacrocephalyCommon
HP:0001012Multiple lipomasCommon
HP:0001028HemangiomaCommon
HP:0005306Capillary hemangiomaCommon
HP:0001048Cavernous hemangiomaCommon
HP:0002240HepatomegalyCommon
HP:0001744SplenomegalyCommon
HP:0001250SeizureCommon
HP:0002133Status epilepticusCommon
HP:0001249Intellectual disabilityCommon
HP:0001528HemihypertrophyCommon
HP:0005323Hemifacial hypertrophyCommon
HP:0001159SyndactylyCommon
HP:0001770Toe syndactylyCommon
HP:0001829Foot polydactylyCommon
HP:0002664NeoplasmCommon (somatic)
HP:0003002Breast carcinomaAssociated
HP:0003003Colon cancerAssociated
HP:0001402Hepatocellular carcinomaAssociated
HP:0002667NephroblastomaAssociated
HP:0003006NeuroblastomaAssociated
HP:0000821HypothyroidismAssociated
HP:0001508Failure to thriveAssociated
HP:0001513ObesityAssociated
HP:0002019ConstipationAssociated
HP:0001289Generalized hypotoniaAssociated
HP:0002119VentriculomegalyAssociated

Complex Disease / GWAS Associations

Top 8 GWAS associations (PIK3CA locus on chromosome 3):

TraitSNP/LocusP-valueAssociation Type
Mean corpuscular volumePIK3CA chr34.0×10⁻²³Hematologic trait
Red blood cell countPIK3CA chr32.0×10⁻¹⁶Hematologic trait
Mean corpuscular hemoglobinPIK3CA chr32.0×10⁻¹⁹Hematologic trait
Mean reticulocyte volumePIK3CA chr31.0×10⁻¹⁰Hematologic trait
Mean spheric corpuscular volumePIK3CA chr31.0×10⁻¹¹Hematologic trait
Reticulocyte fraction of red cellsPIK3CA chr35.0×10⁻⁹Hematologic trait
Mean corpuscular hemoglobinPIK3CA chr33.0×10⁻⁸Hematologic trait (earlier study)

Note: GWAS associations for PIK3CA are predominantly with red blood cell indices and related hematologic parameters, reflecting common variant effects on erythropoiesis rather than Mendelian disease phenotypes.

Structured Data Sources

Generated with Claude Haiku 4.5 + BioBTree MCP, drawing on data BioBTree aggregates from 43 biological databases. Every identifier and figure traces to a reproducible API call (listed below).

Further analyze this answer or run your own queries with BioBTree MCP.

Datasets: alphafold, alphamissense, antibody, bgee, biogrid_interaction, ccds, chembl_molecule, chembl_target, clinical_trials, clinvar, collectri, diamond_similarity, ensembl, entrez, esm2_similarity, exon, expressionatlas, gencc, go, gwas, hgnc, hpa, hpo, intact, interpro, jaspar, mim, mondo, msigdb, orphanet, ortholog, pdb, pfam, pharmgkb_gene, pharmgkb_var_phenotype, reactome, refseq, scxa, scxa_expression, spliceai, string_interaction, transcript, uniprot
Generated: 2026-05-26 — For the latest data, query BioBTree directly via MCP or API.
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