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GeneE
10 sources retrieved · Most recent: April 2026 · Index updated 14 days ago
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PIK3R3
phosphoinositide-3-kinase regulatory subunit 3
Chromosome 1 · 1p34.1
NCBI Gene: 8503Ensembl: ENSG00000117461.16HGNC: HGNC:8981UniProt: B4DXM8
119PubMed Papers
20Diseases
24Drugs
0Pathogenic Variants
FUNCTIONAL ROLE
Hub Gene
CLINICAL
Clinical Trials
DATA QUALITY
✓ Experimental GO Evidence✓ Swiss-Prot Reviewed
positive regulation of gene expressionphosphotyrosine residue bindingcell migration involved in sprouting angiogenesisphosphatidylinositol 3-kinase/protein kinase B signal transductionneurodegenerative diseasecancerbreast cancerlysosomal storage disease
✦AI Summary

PIK3R3 is a regulatory subunit of phosphoinositide-3-kinase (PI3K) that modulates PI3K/AKT signaling through multiple mechanisms. As a regulatory protein, PIK3R3 binds to activated protein-tyrosine kinases via its SH2 domain and regulates their kinase activity, particularly during insulin stimulation when it binds to IRS-1 1. PIK3R3 functions in diverse cellular contexts: it regulates tight junction integrity through the NF-κB pathway in intestinal epithelial cells 1, controls stem cell differentiation and senescence via FOXO1 modulation 2, and mediates NMDAR-dependent AKT signaling for memory updating in neurons 3. Dysregulation of PIK3R3 is implicated in multiple diseases. In inflammatory bowel disease, PIK3R3 overexpression disrupts tight junction protein ZO-1 expression and increases intestinal permeability; PIK3R3 inhibition ameliorates disease symptoms in mouse models 1. PIK3R3 amplification occurs in pancreatic cancer as a focal oncogenic event 4, while miR-511-mediated PIK3R3 suppression inhibits hepatocellular carcinoma progression via the AKT/mTOR pathway 5. Notably, CARD11-PIK3R3 gene fusions enhance therapeutic T cell efficacy in cancer immunotherapy 6. PIK3R3 variants show protective associations against liver cancer in Chinese populations 7. VHL loss in renal cell carcinomas stabilizes PIK3R3 mRNA through m6A modification, promoting oncogenic PI3K signaling 8.

Sources cited
1
PIK3R3 regulates ZO-1 expression through NF-κB pathway and controls intestinal permeability in IBD
PMID: 32473571
2
PIK3R3 regulates stem cell differentiation and senescence through FOXO1 expression modulation
PMID: 39862908
3
PIK3R3 (p55PIK) mediates NMDAR-dependent AKT signaling for memory updating and is disrupted in Alzheimer's disease
PMID: 36796600
4
PIK3R3 amplification occurs as a focal oncogenic event in pancreatic ductal adenocarcinoma
PMID: 25719666
5
miR-511 suppresses hepatocellular carcinoma by targeting PIK3R3 and inhibiting AKT/mTOR signaling
PMID: 25608840
6
CARD11-PIK3R3 gene fusion enhances therapeutic T cell anti-tumor efficacy
PMID: 38326614
7
PIK3R3 genetic variants are associated with reduced liver cancer susceptibility
PMID: 36535266
8
VHL governs PIK3R3 mRNA stability through m6A modification, affecting PI3K/AKT signaling in renal cell carcinoma
PMID: 38618953
Disease Associationsⓘ20
neurodegenerative diseaseOpen Targets
0.55Moderate
cancerOpen Targets
0.49Moderate
breast cancerOpen Targets
0.45Moderate
lysosomal storage diseaseOpen Targets
0.37Weak
prostate carcinomaOpen Targets
0.33Weak
breast carcinomaOpen Targets
0.31Weak
sleep apneaOpen Targets
0.29Weak
infectionOpen Targets
0.28Weak
placenta praeviaOpen Targets
0.28Weak
head and neck malignant neoplasiaOpen Targets
0.28Weak
hearing lossOpen Targets
0.27Weak
Respiratory tract infectionOpen Targets
0.26Weak
Sensorineural hearing impairmentOpen Targets
0.25Weak
neoplasmOpen Targets
0.22Weak
hepatocellular carcinomaOpen Targets
0.21Weak
head and neck squamous cell carcinomaOpen Targets
0.21Weak
non-small cell lung carcinomaOpen Targets
0.21Weak
gastrointestinal stromal tumorOpen Targets
0.21Weak
chronic lymphocytic leukemiaOpen Targets
0.21Weak
pancreatic neuroendocrine tumorOpen Targets
0.21Weak
Pathogenic Variants
No pathogenic variants reported on ClinVar for this gene.
View on ClinVar ↗
Drug Targets24
APITOLISIBPhase II
PI3-kinase class I inhibitor
non-Hodgkins lymphoma
AZD-6482Phase I
PI3-kinase class I inhibitor
BGT-226Phase I/II
PI3-kinase class I inhibitor
BUPARLISIBPhase III
PI3-kinase class I inhibitor
breast cancer
DACTOLISIBPhase III
PI3-kinase class I inhibitor
Respiratory tract infection
DS-7423Phase I
Serine/threonine-protein kinase mTOR inhibitor
GEDATOLISIBPhase III
PI3-kinase class I inhibitor
breast cancer
GSK-1059615Phase I
PI3-kinase class I inhibitor
breast cancer
IZORLISIBPhase I/II
PI3-kinase class I inhibitor
colorectal cancer
OMIPALISIBPhase I
PI3-kinase class I inhibitor
lymphoma
PANULISIBPhase I
PI3-kinase class I inhibitor
PAXALISIBPhase II
PI3-kinase class I inhibitor
brain glioblastoma
PF-04691502Phase II
PI3-kinase class I inhibitor
endometrial cancer
PICTILISIBPhase II
PI3-kinase class I inhibitor
breast cancer
PILARALISIBPhase II
PI3-kinase class I inhibitor
RECILISIBPhase I
PI3-kinase class I inhibitor
SAMOTOLISIBPhase II
PI3-kinase class I inhibitor
prostate cancer
SF-1126Phase II
PI3-kinase class I inhibitor
head and neck malignant neoplasia
SONOLISIBPhase II
PI3-kinase class I inhibitor
TASELISIBPhase III
PI3-kinase class I inhibitor
breast cancer
VOXTALISIBPhase II
Serine/threonine-protein kinase mTOR inhibitor
VS-5584Phase I
Serine/threonine-protein kinase mTOR inhibitor
Malignant Mesothelioma
WX-037Phase I
PI3-kinase class I inhibitor
neoplasm
ZSTK-474Phase I
PI3-kinase class I inhibitor
Related Genes
AKT2Protein interaction100%ALKProtein interaction100%BTKProtein interaction100%CBLBProtein interaction100%CD19Protein interaction100%CD28Protein interaction100%
Tissue Expression6 tissues
Heart
100%
Brain
99%
Lung
53%
Ovary
14%
Liver
12%
Bone Marrow
9%
Gene Interaction Network
Click a node to explore
PIK3R3AKT2ALKBTKCBLBCD19CD28
PROTEIN STRUCTURE
Preparing viewer…
AlphaFoldAI-predicted · UniProt Q8N381
View on AlphaFold ↗
Constraintⓘ
LOEUFⓘ
1.53LoF Tolerant
pLIⓘ
0.00Tolerant
Observed/Expected LoF1.09 [0.79–1.53]
RankingsWhere PIK3R3 stands among ~20K protein-coding genes
  • #3,971of 20,598
    Most Researched119 · top quartile
  • #15,370of 17,882
    Most Constrained (LOEUF)1.53
Genes detectedPIK3R3
Sources retrieved10 papers
Response time—
📄 Sources
10▼
1
PIK3R3 regulates ZO-1 expression through the NF-kB pathway in inflammatory bowel disease.
PMID: 32473571
Int Immunopharmacol · 2020
1.00
2
Naturally occurring T cell mutations enhance engineered T cell therapies.
PMID: 38326614
Nature · 2024
0.90
3
Whole genomes redefine the mutational landscape of pancreatic cancer.
PMID: 25719666
Nature · 2015
0.80
4
PIK3R3 regulates differentiation and senescence of periodontal ligament stem cells and mitigates age-related alveolar bone loss by modulating FOXO1 expression.
PMID: 39862908
J Adv Res · 2025
0.70
5
VHL governs m6A modification and PIK3R3 mRNA stability in clear cell renal cell carcinomas.
PMID: 38618953
J Clin Invest · 2024
0.60