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 74
Pathways AMPK Signaling, Colorectal Carcinoma, EGFR Signaling, Glioblastoma Multiforme, GPCR_CRC, Luminal Breast Cancer, Malignant Melanoma, MTOR Signaling, Myostatin, Prostate Cancer, Rhabdomyosarcoma, Satellite: miRNA network
Inhibitors PKI-587; GSK1059615; CH5132799; (2S)-N1-[5-(2-tert-butyl-4-thiazolyl)-4-methyl-2-thiazolyl]pyrrolidine-1,2-dicarboxamide; 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; XL147; PI-103; XL765; dactolisib; D-106669; torkinib; PP121; wortmannin; CUDC-907; PIK-90; GSK2126458; BKM120; pictrelisib; PIK-75 Hydrochloride; IC-87114; ZSTK-474; PKI-402
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 PIK3R1 0.936
Publications: 1 Organism: In Vitro
Pathways:Glioblastoma Multiforme, MTOR Signaling, IGF and Myogenesis
+ up-regulates activity img/direct-activation.png phosphorylation TPM1 0.2
Publications: 1 Organism: In Vitro
+ down-regulates activity img/direct_inhibition.png phosphorylation PIK3CA 0.2
Publications: 1 Organism: In Vitro
+ down-regulates activity img/direct_inhibition.png phosphorylation PIK3CA 0.2
Publications: 1 Organism: In Vitro
+ down-regulates activity img/direct_inhibition.png phosphorylation PIK3CA 0.2
Publications: 1 Organism: In Vitro
+ down-regulates activity img/indirect_inhibition.png PIK3CA 0.731
Publications: 1 Organism: Homo Sapiens
Pathways:Colorectal Carcinoma, Glioblastoma Multiforme, Luminal Breast Cancer, Malignant Melanoma, MTOR Signaling, Prostate Cancer
+ up-regulates img/direct-activation.png binding PIK3CA 0.397
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png binding PIK3CA 0.397
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png binding PIK3CA 0.429
Publications: 2 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
+ down-regulates img/direct_inhibition.png chemical inhibition PIK3CA 0.8
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png binding PIK3CA 0.413
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png binding PIK3CA 0.91
Publications: 1 Organism: Homo Sapiens
Pathways:Colorectal Carcinoma, Glioblastoma Multiforme, Luminal Breast 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: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png binding PIK3CA 0.562
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png binding PIK3CA 0.475
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
+ up-regulates activity img/indirect-activation.png PIK3CA 0.273
Publications: 1 Organism: Mus Musculus
Pathways:MTOR Signaling
+ up-regulates activity img/direct-activation.png binding PIK3CA 0.936
Publications: 1 Organism: Chlorocebus Aethiops
Pathways:Glioblastoma Multiforme, MTOR Signaling, IGF and Myogenesis
+ up-regulates activity img/indirect-activation.png AKT 0.816
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: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png binding PIK3CA 0.924
Publications: 1 Organism: Homo Sapiens
Pathways:EGFR Signaling, Glioblastoma Multiforme
+ 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 activity img/direct-activation.png binding PIK3CA 0.924
Publications: 1 Organism: Chlorocebus Aethiops
Pathways:EGFR Signaling, Glioblastoma Multiforme
+ up-regulates activity img/indirect-activation.png AKT1 0.816
Publications: 4 Organism: Homo Sapiens
Tissue: Colonic Cancer Cell, Breast Cancer Cell
Pathways:Glioblastoma Multiforme, IGF and Myogenesis
+ down-regulates activity img/direct_inhibition.png chemical inhibition PIK3CA 0.8
Publications: 1 Organism: In Vitro
+ up-regulates img/indirect-activation.png AKT2 0.669
Publications: 1 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png binding PIK3CA 0.411
Publications: 1 Organism: Homo Sapiens
+ down-regulates activity img/direct_inhibition.png chemical inhibition PIK3CA 0.8
Publications: 1 Organism: In Vitro
+ down-regulates img/direct_inhibition.png chemical inhibition PIK3CA 0.8
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/indirect-activation.png MTOR 0.546
Publications: 1 Organism: Homo Sapiens
Pathways:Glioblastoma Multiforme, MTOR Signaling
+ up-regulates activity img/direct-activation.png phosphorylation AKT 0.816
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
+ down-regulates activity img/direct_inhibition.png binding PIK3CA 0.2
Publications: 1 Organism: Homo Sapiens
+ down-regulates activity img/indirect_inhibition.png IRS1 0.721
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 0.2
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png binding PIK3CA 0.382
Publications: 2 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png binding PIK3CA 0.684
Publications: 1 Organism: Homo Sapiens
Pathways:Colorectal Carcinoma
+ 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
+ up-regulates img/direct-activation.png binding PIK3CA 0.846
Publications: 1 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png binding PIK3CA 0.844
Publications: 1 Organism: Homo Sapiens
Pathways:Malignant Melanoma
+ down-regulates img/direct_inhibition.png chemical inhibition PIK3CA 0.8
Publications: 1 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png ubiquitination PIK3CA 0.455
Publications: 1 Organism: Homo Sapiens
+ down-regulates img/direct_inhibition.png chemical inhibition PIK3CA 0.8
Publications: 1 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png phosphorylation BTK 0.512
Publications: 1 Organism: Mus Musculus
+ up-regulates img/indirect-activation.png RAC1 0.568
Publications: 1 Organism: Homo Sapiens
+ form complex img/form-complex.png binding PI3K 0.936
Publications: 1 Organism: Homo Sapiens
Pathways:mTOR in cancer
+ up-regulates img/direct-activation.png binding PIK3CA 0.608
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
+ 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 0.414
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 activity img/direct-activation.png binding PIK3CA 0.721
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
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 0.449
Publications: 1 Organism: Homo Sapiens
Pathways:EGFR Signaling, Rhabdomyosarcoma
+ down-regulates img/direct_inhibition.png chemical inhibition PIK3CA 0.8
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png binding PIK3CA 0.464
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png binding PIK3CA 0.707
Publications: 1 Organism: Homo Sapiens