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 GSK2126458; PKI-402; pictrelisib; PIK-75 Hydrochloride; XL765; torkinib; PI-103; wortmannin; IC-87114; ZSTK-474; D-106669; (2S)-N1-[5-(2-tert-butyl-4-thiazolyl)-4-methyl-2-thiazolyl]pyrrolidine-1,2-dicarboxamide; PP121; dactolisib; GSK1059615; CH5132799; PIK-90; 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; BKM120; PKI-587; CUDC-907
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 0.934
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 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
Tissue: Breast
+ up-regulates activity img/direct-activation.png phosphorylation BTK 0.506
Publications: 1 Organism: Mus Musculus
+ up-regulates img/direct-activation.png binding PIK3CA 0.371
Publications: 2 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 0.678
Publications: 1 Organism: Homo Sapiens
Pathways:Colorectal Carcinoma
+ 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 0.458
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png binding PIK3CA 0.44
Publications: 1 Organism: Homo Sapiens
Pathways:EGFR Signaling, Rhabdomyosarcoma
+ up-regulates img/direct-activation.png binding PIK3CA 0.839
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
+ down-regulates activity img/direct_inhibition.png chemical inhibition PIK3CA 0.8
Publications: 1 Organism: In Vitro
+ up-regulates activity img/indirect-activation.png AKT1 0.82
Publications: 4 Organism: Homo Sapiens
Tissue: Breast Cancer Cell, Colonic 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 0.671
Publications: 1 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png phosphorylation AKT 0.82
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/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 img/direct_inhibition.png chemical inhibition PIK3CA 0.8
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
+ up-regulates img/direct-activation.png binding PIK3CA 0.407
Publications: 1 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png binding PIK3CA 0.838
Publications: 1 Organism: Homo Sapiens
Pathways:Malignant Melanoma
+ up-regulates activity img/direct-activation.png binding PIK3CA 0.717
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 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 MTOR 0.54
Publications: 1 Organism: Homo Sapiens
Pathways:Glioblastoma Multiforme, MTOR Signaling
+ up-regulates img/direct-activation.png binding PIK3CA 0.924
Publications: 1 Organism: Homo Sapiens
Pathways:EGFR Signaling, Glioblastoma Multiforme
+ up-regulates activity img/indirect-activation.png AKT 0.82
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
+ up-regulates img/direct-activation.png binding PIK3CA 0.405
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 0.277
Publications: 1 Organism: Mus Musculus
Pathways:MTOR Signaling
+ up-regulates img/indirect-activation.png RAC1 0.555
Publications: 1 Organism: Homo Sapiens
+ down-regulates activity img/direct_inhibition.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
+ down-regulates img/direct_inhibition.png chemical inhibition PIK3CA 0.8
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png binding PIK3CA 0.422
Publications: 2 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png binding PIK3CA 0.2
Publications: 1 Organism: Homo Sapiens
+ form complex img/form-complex.png binding PI3K 0.934
Publications: 1 Organism: Homo Sapiens
Pathways:mTOR in cancer
+ down-regulates activity img/indirect_inhibition.png PIK3CA 0.736
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 0.387
Publications: 1 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png binding PIK3CA 0.47
Publications: 2 Organism: Homo Sapiens
+ up-regulates img/direct-activation.png binding PIK3CA 0.909
Publications: 1 Organism: Homo Sapiens
Pathways:Colorectal Carcinoma, Glioblastoma Multiforme, Luminal Breast Cancer, Rhabdomyosarcoma
+ up-regulates img/direct-activation.png binding PIK3CA 0.706
Publications: 1 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png binding PIK3CA 0.934
Publications: 1 Organism: Chlorocebus Aethiops
Pathways:Glioblastoma Multiforme, MTOR Signaling, IGF and Myogenesis
+ 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 0.609
Publications: 1 Organism: Homo Sapiens
+ up-regulates activity img/direct-activation.png binding PIK3CA 0.402
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/direct-activation.png binding PIK3CA 0.554
Publications: 1 Organism: Homo Sapiens
+ down-regulates activity img/indirect_inhibition.png IRS1 0.717
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 ubiquitination PIK3CA 0.447
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/direct-activation.png binding PIK3CA 0.387
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