PIK3CA
ENSG00000121879
Target class
Enzyme
Chromosome
3
Approved drugs
4
Clinical candidates (approved and in development)
35
- Approved drugs
- 4
- ClinGen gene-disease validity
- Definitive
- Clinical candidates (approved and in development)
- 35
- Chemical probe available
- Yes
- Other names
- PI3K
- Target name
- PIK3CA
- Gene name
- Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha
- Gene symbol
- PIK3CA
- Protein name
- Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (PI3-kinase subunit alpha) (PI3K-alpha) (PI3Kalpha) (PtdIns-3-kinase subunit alpha) (EC 2.7.1.137) (EC 2.7.1.153) (Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit alpha) (PtdIns-3-kinase subunit p110-alpha) (p110alpha) (Phosphoinositide 3-kinase alpha) (Phosphoinositide-3-kinase catalytic alpha polypeptide) (Serine/threonine protein kinase PIK3CA) (EC 2.7.11.1)
- Gene biotype
- Protein coding
- Gene family
- Phosphatidylinositol 3-kinase family
- Target class
- Enzyme
- Target type
- Human gene
- Tissues expressed in
- 54
- Protein localisation evidence grade
- Approved
- Highest tissue expression
- 23.19
- Tissue specificity (Gini)
- 0.328
- Tissue specificity (tau)
- 0.555
- KEGG gene identifiers
- hsa:5290
- Protein interaction confidence
- 0.876325
- Protein interaction partners
- 191
- R-HSA-109704
- R-HSA-112399
- R-HSA-114604
- R-HSA-1236382
- R-HSA-1250342
- R-HSA-1257604
- R-HSA-1433557
- R-HSA-1660499
- R-HSA-180292
- R-HSA-1839117
- R-HSA-186763
- R-HSA-1963642
- R-HSA-198203
- R-HSA-201556
- R-HSA-202424
- R-HSA-2029485
- R-HSA-210993
- R-HSA-2219530
- R-HSA-2424491
- R-HSA-2730905
- R-HSA-373753
- R-HSA-389357
- R-HSA-416476
- R-HSA-4420097
- R-HSA-512988
And 35 more, listed on the interactive page.
- End position
- 179240093
- Start position
- 179148114
- Chromosome
- 3
- Strand
- Forward
- Cytosol
- Microtubules
- Mitochondria
- Primary cilium
- Tissue specificity (tau)
- 0.555461
- Expression inequality (Gini)
- 0.327823
Expression in transcripts per million
- Artery - Tibial
- 23.19
- Cells - EBV-transformed lymphocytes
- 22.39
- Nerve - Tibial
- 21.42
- Adipose - Subcutaneous
- 20.51
- Cells - Cultured fibroblasts
- 20.48
Expression in transcripts per million
- Artery - Tibial23.19
- Cells - EBV-transformed lymphocytes22.39
- Nerve - Tibial21.42
- Adipose - Subcutaneous20.51
- Cells - Cultured fibroblasts20.48
- Uterus19.12
- Artery - Coronary18.44
- Adipose - Visceral (Omentum)18.19
- Artery - Aorta17.98
- Breast - Mammary Tissue17.86
- Lung15.64
- Ovary15.51
- Fallopian Tube15.21
- Cervix - Endocervix15.08
- Vagina14.94
- Cervix - Ectocervix14.92
- Esophagus - Muscularis14.88
- Bladder14.86
- Colon - Sigmoid14.34
- Esophagus - Gastroesophageal Junction13.73
- Skin - Sun Exposed (Lower leg)12.53
- Thyroid12.29
- Skin - Not Sun Exposed (Suprapubic)12.26
- Brain - Cerebellum10.43
- Spleen10.4
And 29 more, listed on the interactive page.
- GO:0001944
- GO:0007173
- GO:0008286
- GO:0030168
- GO:0032869
- GO:0038084
- GO:0038203
- GO:0043491
- GO:0043542
- GO:0045860
- GO:0050852
- GO:0051897
- GO:0060048
- GO:1905477
- GO:2000811
- GO:0005829
- GO:0005943
- GO:0005515
- GO:0016303
- GO:0046934
heart disease
Studies
- preclinical: Highly important for the heart and vasculature based on findings in genetically modified or kinase-inhibitor-treated mice. Role of kinase in heart/vasculature: Physiological heart growth; cardiomyocyte survival
Biological samples
- cardiovascular system
PubMed 21283106
regulation of catalytic activity
Studies
- biochemical: NVS_ENZ_hPI3Ka, is one of one assay component(s) measured or calculated from the NVS_ENZ_hPI3Ka assay. It is designed to make measurements of enzyme activity, a form of enzyme reporter, as detected with fluorescence intensity signals by Fluorescence and electrophoretic mobility shift technology.
Biological samples
- cell-free
Evidence source
Related records
Trials (562)
- 24VA022; VATCH Alpelisib for TIE2/PIK3CA Pathway VAs
- 5G-PEARL: Paxalisib in Malignant Brain Tumours
- A 3-Part Study to Determine the Relative Bioavailability of Capsule and Tablet Formulations of GDC-0980, the Effect of Food, and the Effect of Rabeprazole on the Pharmacokinetics of the Tablet
- A Bioavailability and Pharmacokinetic Study of GDC-0032 in Healthy Volunteers
- A Clinical Study of Novel Pneumococcal Vaccine V118C in Children (V118C-002)
- A Clinical Trial Evaluating the Efficacy and Safety of Leflutrozole on Testicular Function
- A Clinical Trial of Buparlisib and Ibrutinib in Lymphoma
- A Dose Escalation Study Evaluating the Safety and Tolerability of GDC-0032 in Participants With Locally Advanced or Metastatic Solid Tumors or Non-Hodgkin's Lymphoma (NHL) and in Combination With Endocrine Therapy in Locally Advanced or Metastatic Hormone Receptor-Positive Breast Cancer
- A Dose-escalation Study to Assess the Safety, Tolerability, and Pharmacokinetics of GDC-0032 in Combination With Docetaxel or With Paclitaxel in Patients With HER2-negative Locally Recurrent or Metastatic Breast Cancer or Non-small Cell Lung Cancer
- A Dose-finding Study of a Combination of Imatinib and BYL719 in the Treatment of 3rd Line GIST Patients
- A Drug Interaction Study of GDC-0032 Co-administered With Rifampin or Itraconazole in Healthy Volunteers
- A Drug-drug Interaction Study Evaluating the Perpetrator Potential of LY4100511 (DC-853) on Midazolam, Repaglinide, Digoxin, Rosuvastatin in Healthy Participants
- A First in Human Study to Assess the Safety, Tolerability, and Pharmacokinetics of DGX-001
- A First in Human Study to Evaluate the Safety, Tolerability, Pharmacokinetics and Immunogenicity of PMG1015
- A Multicenter Phase I/II Trial of Abiraterone Acetate + BEZ235 in Metastatic, Castration-Resistant Prostate Cancer
- A Multicenter, Single Arm Study to Evaluate the Preliminary Efficacy and Safety Profile of Inavolisib in Previously Treated Pancreatic Ductal Adenocarcinoma Patients
- A Novel Aromatase Inhibitor, Leflutrozole, for Treatment of Non-Obstructive Azoospermia
- A Pharmacokinetics Study to Assess Abiraterone Acetate Capsule and Tablet Formulations in Patients With Prostate Cancer
- A Phase 1 Dose Escalation Study of VS-5584 Administered in Combination With VS-6063, in Subjects With Relapsed Malignant Mesothelioma
- A Phase 1a/1b Study of CB4211 in Healthy Non-obese Subjects and Subjects With Nonalcoholic Fatty Liver Disease
Drugs (37)
- Alpelisib PI3-kinase p110-alpha subunit inhibitor
- Apitolisib PI3-kinase class I inhibitor
- AZD-6482 PI3-kinase class I inhibitor
- BAY-1082439 PI3-kinase p110-alpha subunit inhibitor
- BGT-226 PI3-kinase class I inhibitor
- BGT-226 FREE BASE PI3-kinase class I inhibitor
- Buparlisib PI3-kinase class I inhibitor
- Copanlisib PI3-kinase p110-alpha subunit inhibitor
- Copanlisib hydrochloride PI3-kinase p110-alpha subunit inhibitor
- Dactolisib PI3-kinase class I inhibitor
- DS-7423 PI3-kinase class I inhibitor
- Fimepinostat PI3-kinase p110-alpha subunit inhibitor
- Gedatolisib PI3-kinase class I inhibitor
- GSK-1059615 PI3-kinase class I inhibitor
- Inavolisib PI3-kinase p110-alpha subunit inhibitor
- Izorlisib PI3-kinase class I inhibitor
- Omipalisib PI3-kinase class I inhibitor
- Panulisib PI3-kinase class I inhibitor
- Paxalisib PI3-kinase class I inhibitor
- PF-04691502 PI3-kinase class I inhibitor