Summary

Name PIK3CA
Full Name Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
Synonyms PI3-kinase subunit alpha, PI3K-alpha, PI3Kalpha, PtdIns-3-kinase subunit alpha, Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit alpha, PtdIns-3-kinase subunit p110-alpha, p110alpha, Phosphoinositide-3-kinase catalytic alpha polypeptide, Serine/threonine protein kinase PIK3CA, 2.7.11.1
Primary ID P42336
Links - -
Type protein
Relations 67
Pathways AMPK Signaling, EGFR, Glioblastoma Multiforme, Malignant Melanoma, Acute Myeloid Leukemia, IGF and Myogenesis, Colorectal Carcinoma, Luminal Breast Cancer, Prostate Cancer, Rhabdomyosarcoma, MTOR Signaling, mTOR in cancer
Inhibitors pictrelisib; ZSTK-474; GSK2126458; BKM120; GSK1059615; XL147; 1-[4-[[2-(2-amino-5-pyrimidinyl)-7-methyl-4-(4-morpholinyl)-6-thieno[3,2-d]pyrimidinyl]methyl]-1-piperazinyl]-2-hydroxy-1-propanone; wortmannin; IC-87114; PI-103; PP121; torkinib; (2S)-N1-[5-(2-tert-butyl-4-thiazolyl)-4-methyl-2-thiazolyl]pyrrolidine-1,2-dicarboxamide; dactolisib; PIK-75 Hydrochloride; PKI-587; PIK-90; PKI-402; XL765; CUDC-907; CH5132799; D-106669
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

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Relations

Regulator Mechanism target score
+ up-regulates activity img/direct-activation.png binding PIK3CA 0.45
Publications: 1 Organism: Homo Sapiens
Tissue: Lung Cancer Cell
Pathways:AMPK Signaling, Luminal Breast Cancer, mTOR in cancer, MTOR Signaling, IGF and Myogenesis
+ up-regulates activity img/indirect-activation.png AKT1 0.45
Publications: 4 Organism: Homo Sapiens
Tissue: Colonic Cancer Cell, Breast Cancer Cell
Pathways:Glioblastoma Multiforme, IGF and Myogenesis
+ up-regulates img/direct-activation.png binding PIK3CA 0.39
Publications: 1 Organism: Homo Sapiens
Pathways:EGFR, Rhabdomyosarcoma
+ up-regulates activity img/indirect-activation.png AKT 0.22
Publications: 1 Organism: Homo Sapiens
Tissue: Breast Cancer Cell
Pathways:Acute Myeloid Leukemia, AMPK Signaling, EGFR, Luminal Breast Cancer, mTOR in cancer, Malignant Melanoma, MTOR Signaling, Prostate Cancer, Rhabdomyosarcoma
+ up-regulates img/direct-activation.png binding PIK3CA 0.31
Publications: 1 Organism: Homo Sapiens
+ down-regulates activity img/direct_inhibition.png chemical inhibition PIK3CA 0.14
Publications: 1 Organism: In Vitro
+ down-regulates img/direct_inhibition.png chemical inhibition PIK3CA 0.08
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/indirect-activation.png Survival 0.30
Publications: 1 Organism: Chlorocebus Aethiops
Pathways:Colorectal Carcinoma, Glioblastoma Multiforme, Luminal Breast Cancer, Malignant Melanoma, Prostate Cancer, Rhabdomyosarcoma
+ up-regulates img/direct-activation.png binding PIK3CA 0.14
Publications: 2 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png binding PIK3CA 0.14
Publications: 2 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png binding PIK3CA 0.14
Publications: 2 Organism: Homo Sapiens
+ down-regulates img/direct_inhibition.png chemical inhibition PIK3CA 0.08
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png binding PIK3CA 0.08
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png binding PIK3CA 0.17
Publications: 1 Organism: Homo Sapiens
Pathways:EGFR
+ down-regulates img/direct_inhibition.png chemical inhibition PIK3CA 0.08
Publications: 1 Organism: Homo Sapiens
+ down-regulates img/direct_inhibition.png chemical inhibition PIK3CA 0.14
Publications: 1 Organism: Homo Sapiens
Tissue: Breast
+ down-regulates img/direct_inhibition.png chemical inhibition PIK3CA 0.08
Publications: 1 Organism: Homo Sapiens
+ down-regulates img/direct_inhibition.png chemical inhibition PIK3CA 0.08
Publications: 1 Organism: Homo Sapiens
+ down-regulates img/direct_inhibition.png chemical inhibition PIK3CA 0.08
Publications: 1 Organism: Homo Sapiens
+ down-regulates img/direct_inhibition.png chemical inhibition PIK3CA 0.14
Publications: 2 Organism: Homo Sapiens
+ down-regulates img/direct_inhibition.png chemical inhibition PIK3CA 0.08
Publications: 1 Organism: Homo Sapiens
+ down-regulates img/direct_inhibition.png chemical inhibition PIK3CA 0.14
Publications: 1 Organism: Homo Sapiens
+ up-regulates quantity img/direct-activation.png small molecule catalysis 1-phosphatidyl-1D-myo-inositol 3,4,5-trisphosphate 0.57
Publications: 2 Organism: Homo Sapiens
+ down-regulates img/direct_inhibition.png chemical inhibition PIK3CA 0.08
Publications: 1 Organism: Homo Sapiens
+ down-regulates activity img/direct_inhibition.png binding PIK3CA 0.08
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png binding PIK3CA 0.08
Publications: 1 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png binding PIK3CA 0.17
Publications: 1 Organism: Chlorocebus Aethiops
Pathways:EGFR
+ down-regulates activity img/direct_inhibition.png chemical inhibition PIK3CA 0.14
Publications: 1 Organism: In Vitro
+ down-regulates activity img/direct_inhibition.png chemical inhibition PIK3CA 0.08
Publications: 1 Organism: In Vitro
+ up-regulates activity img/direct-activation.png binding PIK3CA 0.17
Publications: 1 Organism: Homo Sapiens
Pathways:Malignant Melanoma
+ up-regulates img/indirect-activation.png AKT2 0.22
Publications: 1 Organism: Homo Sapiens
+ down-regulates activity img/indirect_inhibition.png IRS1 0.48
Publications: 1 Organism: Homo Sapiens
Pathways:AMPK Signaling, Luminal Breast Cancer, mTOR in cancer, MTOR Signaling, IGF and Myogenesis
+ down-regulates img/direct_inhibition.png chemical inhibition PIK3CA 0.08
Publications: 1 Organism: Homo Sapiens
+ down-regulates img/direct_inhibition.png chemical inhibition PIK3CA 0.08
Publications: 1 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png phosphorylation AKT 0.22
Publications: 1 Organism: Homo Sapiens
Pathways:Acute Myeloid Leukemia, AMPK Signaling, EGFR, Luminal Breast Cancer, mTOR in cancer, Malignant Melanoma, MTOR Signaling, Prostate Cancer, Rhabdomyosarcoma
+ down-regulates img/direct_inhibition.png chemical inhibition PIK3CA 0.08
Publications: 1 Organism: Homo Sapiens
+ down-regulates img/direct_inhibition.png chemical inhibition PIK3CA 0.08
Publications: 1 Organism: Homo Sapiens
+ down-regulates img/direct_inhibition.png chemical inhibition PIK3CA 0.08
Publications: 1 Organism: Homo Sapiens
+ down-regulates img/direct_inhibition.png chemical inhibition PIK3CA 0.08
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/indirect-activation.png MTOR 0.08
Publications: 1 Organism: Homo Sapiens
Pathways:Glioblastoma Multiforme, MTOR Signaling
+ down-regulates img/direct_inhibition.png chemical inhibition PIK3CA 0.08
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png binding PIK3CA 0.08
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png binding PIK3CA 0.08
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png binding PIK3CA 0.08
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png binding PIK3CA 0.26
Publications: 1 Organism: Homo Sapiens
Pathways:Acute Myeloid Leukemia, Colorectal Carcinoma, Glioblastoma Multiforme, Luminal Breast Cancer, Rhabdomyosarcoma
+ up-regulates activity img/direct-activation.png binding PIK3CA 0.08
Publications: 1 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png phosphorylation BTK 0.08
Publications: 1 Organism: Mus Musculus
+ form complex img/form-complex.png binding PI3K 0.08
Publications: 1 Organism: Homo Sapiens
Pathways:mTOR in cancer
+ up-regulates activity img/direct-activation.png binding PIK3CA 0.71
Publications: 1 Organism: Chlorocebus Aethiops
Pathways:Glioblastoma Multiforme, MTOR Signaling, IGF and Myogenesis
+ up-regulates img/direct-activation.png binding PIK3CA 0.08
Publications: 1 Organism: Homo Sapiens
+ down-regulates img/direct_inhibition.png chemical inhibition PIK3CA 0.08
Publications: 1 Organism: Homo Sapiens
+ up-regulates activity img/indirect-activation.png PIK3CA 0.08
Publications: 1 Organism: Mus Musculus
+ up-regulates img/indirect-activation.png RAC1 0.17
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png binding PIK3CA 0.28
Publications: 1 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png binding PIK3CA 0.25
Publications: 1 Organism: Homo Sapiens
Pathways:Colorectal Carcinoma
+ down-regulates activity img/indirect_inhibition.png PIK3CA 0.17
Publications: 1 Organism: Homo Sapiens
Pathways:Colorectal Carcinoma, Glioblastoma Multiforme, Luminal Breast Cancer, Malignant Melanoma, MTOR Signaling, Prostate Cancer
+ down-regulates img/direct_inhibition.png chemical inhibition PIK3CA 0.08
Publications: 1 Organism: Homo Sapiens
+ down-regulates img/direct_inhibition.png chemical inhibition PIK3CA 0.08
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png binding PIK3CA 0.22
Publications: 1 Organism: Homo Sapiens