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 69
Pathways AMPK Signaling, Colorectal Carcinoma, EGFR Signaling, Glioblastoma Multiforme, Luminal Breast Cancer, Malignant Melanoma, MTOR Signaling, Myostatin, Prostate Cancer, Rhabdomyosarcoma, Satellite: miRNA network
Inhibitors XL765; IC-87114; pictrelisib; ZSTK-474; BKM120; wortmannin; GSK2126458; PKI-587; torkinib; D-106669; CH5132799; 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; PIK-75 Hydrochloride; GSK1059615; PP121; PKI-402; XL147; PI-103; (2S)-N1-[5-(2-tert-butyl-4-thiazolyl)-4-methyl-2-thiazolyl]pyrrolidine-1,2-dicarboxamide; CUDC-907; dactolisib; PIK-90
Function Phosphoinositide-3-kinase (PI3K) phosphorylates phosphatidylinositol (PI) and its phosphorylated derivatives at position 3 of the inositol ring to produce 3-phosphoinositides (PubMed:15135396, PubMed:23936502, PubMed:28676499). Uses ATP and PtdIns(4,5)P2 (phosphatidylinositol 4,5-bisphosphate) to generate phosphatidylinositol 3,4,5-trisphosphate (PIP3) (PubMed:15135396, PubMed:28676499). 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. In addition to its lipid kinase activity, it displays a serine-protein kinase activity that results in the autophosphorylation of the p85alpha regulatory subunit as well as phosphorylation of other proteins such as 4EBP1, H-Ras, the IL-3 beta c receptor and possibly others (PubMed:23936502, PubMed:28676499). Plays a role in the positive regulation of phagocytosis and pinocytosis (By similarity).

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Modifications Tables

Relations

Regulator Mechanism target score
+ up-regulates activity img/direct-activation.png phosphorylation TPM1 0.2
Publications: 1 Organism: In Vitro
+ up-regulates activity img/indirect-activation.png AKT1 0.812
Publications: 4 Organism: Homo Sapiens
Tissue: Breast Cancer Cell, Colonic Cancer Cell
Pathways:Glioblastoma Multiforme, IGF and Myogenesis
+ up-regulates activity img/direct-activation.png phosphorylation AKT 0.812
Publications: 1 Organism: Homo Sapiens
Pathways:AMPK Signaling, EGFR Signaling, Glioblastoma Multiforme, Luminal Breast Cancer, mTOR in cancer, Malignant Melanoma, MTOR Signaling, Prostate Cancer, Rhabdomyosarcoma
+ up-regulates img/direct-activation.png binding PIK3CA 0.368
Publications: 1 Organism: Homo Sapiens
+ down-regulates img/direct_inhibition.png chemical inhibition PIK3CA 0.8
Publications: 1 Organism: Homo Sapiens
+ down-regulates activity img/direct_inhibition.png binding PIK3CA 0.2
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png binding PIK3CA 0.44
Publications: 1 Organism: Homo Sapiens
+ up-regulates quantity img/direct-activation.png chemical modification PIP3 0.8
Publications: 2 Organism: Homo Sapiens
Pathways:AMPK Signaling, EGFR Signaling, Glioblastoma Multiforme, mTOR in cancer, Malignant Melanoma, MTOR Signaling, Prostate Cancer
+ up-regulates img/direct-activation.png binding PIK3CA 0.452
Publications: 2 Organism: Homo Sapiens
+ down-regulates img/direct_inhibition.png chemical inhibition PIK3CA 0.8
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/indirect-activation.png AKT2 0.658
Publications: 1 Organism: Homo Sapiens
+ down-regulates img/direct_inhibition.png chemical inhibition PIK3CA 0.8
Publications: 1 Organism: Homo Sapiens
Tissue: Breast
+ down-regulates img/direct_inhibition.png chemical inhibition PIK3CA 0.8
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png binding PIK3CA 0.386
Publications: 1 Organism: Homo Sapiens
+ up-regulates activity img/indirect-activation.png AKT 0.812
Publications: 1 Organism: Homo Sapiens
Tissue: Breast Cancer Cell
Pathways:AMPK Signaling, EGFR Signaling, Glioblastoma Multiforme, Luminal Breast Cancer, mTOR in cancer, Malignant Melanoma, MTOR Signaling, Prostate Cancer, Rhabdomyosarcoma
+ down-regulates img/direct_inhibition.png chemical inhibition PIK3CA 0.8
Publications: 1 Organism: Homo Sapiens
+ down-regulates img/direct_inhibition.png chemical inhibition PIK3CA 0.8
Publications: 2 Organism: Homo Sapiens
+ down-regulates img/direct_inhibition.png chemical inhibition PIK3CA 0.8
Publications: 1 Organism: Homo Sapiens
+ down-regulates img/direct_inhibition.png chemical inhibition PIK3CA 0.8
Publications: 1 Organism: Homo Sapiens
+ down-regulates activity img/direct_inhibition.png chemical inhibition PIK3CA 0.8
Publications: 1 Organism: In Vitro
+ up-regulates activity img/direct-activation.png binding PIK3CA 0.934
Publications: 1 Organism: Chlorocebus Aethiops
Pathways:Glioblastoma Multiforme, MTOR Signaling, IGF and Myogenesis
+ up-regulates img/direct-activation.png binding PIK3CA 0.403
Publications: 2 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png phosphorylation BTK 0.49
Publications: 1 Organism: Mus Musculus
+ down-regulates img/direct_inhibition.png chemical inhibition PIK3CA 0.8
Publications: 1 Organism: Homo Sapiens
+ down-regulates activity img/direct_inhibition.png chemical inhibition PIK3CA 0.8
Publications: 1 Organism: In Vitro
+ up-regulates img/direct-activation.png binding PIK3CA 0.352
Publications: 2 Organism: Homo Sapiens
+ down-regulates img/direct_inhibition.png chemical inhibition PIK3CA 0.8
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png binding PIK3CA 0.837
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png binding PIK3CA 0.423
Publications: 1 Organism: Homo Sapiens
Pathways:EGFR Signaling, Rhabdomyosarcoma
+ up-regulates img/direct-activation.png binding PIK3CA 0.39
Publications: 1 Organism: Homo Sapiens
+ down-regulates img/direct_inhibition.png chemical inhibition PIK3CA 0.8
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png binding PIK3CA 0.368
Publications: 1 Organism: Homo Sapiens
+ up-regulates activity img/indirect-activation.png PIK3CA 0.278
Publications: 1 Organism: Mus Musculus
Pathways:MTOR Signaling
+ down-regulates img/direct_inhibition.png chemical inhibition PIK3CA 0.8
Publications: 1 Organism: Homo Sapiens
+ down-regulates img/direct_inhibition.png chemical inhibition PIK3CA 0.8
Publications: 1 Organism: Homo Sapiens
+ down-regulates img/direct_inhibition.png chemical inhibition PIK3CA 0.8
Publications: 1 Organism: Homo Sapiens
+ down-regulates img/direct_inhibition.png chemical inhibition PIK3CA 0.8
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/indirect-activation.png RAC1 0.545
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png binding PIK3CA 0.594
Publications: 1 Organism: Homo Sapiens
+ down-regulates img/direct_inhibition.png chemical inhibition PIK3CA 0.8
Publications: 1 Organism: Homo Sapiens
+ down-regulates img/direct_inhibition.png chemical inhibition PIK3CA 0.8
Publications: 1 Organism: Homo Sapiens
+ down-regulates img/direct_inhibition.png chemical inhibition PIK3CA 0.8
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/indirect-activation.png Survival 0.7
Publications: 1 Organism: Chlorocebus Aethiops
Pathways:Colorectal Carcinoma, Glioblastoma Multiforme, Luminal Breast Cancer, Malignant Melanoma, Prostate Cancer, Rhabdomyosarcoma
+ form complex img/form-complex.png binding PI3K 0.934
Publications: 1 Organism: Homo Sapiens
Pathways:mTOR in cancer
+ up-regulates activity img/direct-activation.png binding PIK3CA 0.709
Publications: 1 Organism: Homo Sapiens
Pathways:AMPK Signaling, Luminal Breast Cancer, mTOR in cancer, MTOR Signaling, IGF and Myogenesis
+ up-regulates activity img/direct-activation.png binding PIK3CA 0.835
Publications: 1 Organism: Homo Sapiens
Pathways:Malignant Melanoma
+ down-regulates activity img/indirect_inhibition.png PIK3CA 0.724
Publications: 1 Organism: Homo Sapiens
Pathways:Colorectal Carcinoma, Glioblastoma Multiforme, Luminal Breast Cancer, Malignant Melanoma, MTOR Signaling, Prostate Cancer
+ down-regulates activity img/indirect_inhibition.png IRS1 0.709
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 0.8
Publications: 1 Organism: Homo Sapiens
+ down-regulates activity img/direct_inhibition.png chemical inhibition PIK3CA 0.8
Publications: 1 Organism: In Vitro
+ up-regulates activity img/direct-activation.png binding PIK3CA 0.669
Publications: 1 Organism: Homo Sapiens
Pathways:Colorectal Carcinoma
+ down-regulates img/direct_inhibition.png chemical inhibition PIK3CA 0.8
Publications: 1 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png binding PIK3CA 0.922
Publications: 1 Organism: Chlorocebus Aethiops
Pathways:EGFR Signaling, Glioblastoma Multiforme
+ up-regulates activity img/direct-activation.png binding PIK3CA 0.2
Publications: 1 Organism: Homo Sapiens
+ down-regulates img/direct_inhibition.png chemical inhibition PIK3CA 0.8
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png binding PIK3CA 0.696
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png binding PIK3CA 0.541
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png binding PIK3CA 0.907
Publications: 1 Organism: Homo Sapiens
Pathways:Colorectal Carcinoma, Glioblastoma Multiforme, Luminal Breast Cancer, Rhabdomyosarcoma
+ up-regulates img/direct-activation.png binding PIK3CA 0.922
Publications: 1 Organism: Homo Sapiens
Pathways:EGFR Signaling, Glioblastoma Multiforme
+ up-regulates img/indirect-activation.png MTOR 0.525
Publications: 1 Organism: Homo Sapiens
Pathways:Glioblastoma Multiforme, MTOR Signaling
+ up-regulates activity img/direct-activation.png binding PIK3CA 0.383
Publications: 1 Organism: Homo Sapiens