Phosphoinositide 3-kinaCatalytic subunitInositolActivation of phosphatidylinositolPhosphorylation of phosphatidylinositolProteinPathwaysBiosynthetic processPtdInsInhibitorSubstratesActivatesSignalingReceptorPhospholipidsCellsInhibitionMechanismMolecularMembraneAssayTypeMalignantActivityVesicleBiologicalLiverFamilyLevelsExpressionBelongsBrainCommonAcidRegulatory
Phosphoinositide 3-kina3
- Previous studies reported that ATF-3 was induced by treating cells with antitumorigenic compounds [ 14 - 18 ] and a phosphoinositide 3-kinase inhibitor [ 19 ]. (hindawi.com)
- Enhancement of phosphoinositide 3-kinase (PI 3-kinase) activity by membrane curvature and inositol-phospholipid-binding peptides. (tamu.edu)
- The phosphorylation of phosphatidylinositol (PtdIns) on the 3' position of the inositol ring by phosphoinositide 3-kinase (PI 3-kinase) is shown to depend strongly on the curvature of liposomes containing a mixture of phosphatidylcholine (PtdCho) and PtdIns. (tamu.edu)
Catalytic subunit2
- Orthologous to human PIK3C2A (phosphatidylinositol-4-phosphate 3-kinase catalytic subunit type 2 alpha). (nih.gov)
- PI3K is composed of two subunits: the p85 regulatory subunit, containing two Src homology-2 domains, and the p110 catalytic subunit ( 2 - 4 ). (diabetesjournals.org)
Inositol10
- In enzymology, a 1-phosphatidylinositol 4-kinase (EC 2.7.1.67) is an enzyme that catalyzes the chemical reaction ATP + 1-phosphatidyl-1D-myo-inositol ⇌ {\displaystyle \rightleftharpoons } ADP + 1-phosphatidyl-1D-myo-inositol 4-phosphate Thus, the two substrates of this enzyme are ATP and 1-phosphatidyl-1D-myo-inositol, whereas its two products are ADP and 1-phosphatidyl-1D-myo-inositol 4-phosphate. (wikipedia.org)
- The systematic name of this enzyme class is ATP:1-phosphatidyl-1D-myo-inositol 4-phosphotransferase. (wikipedia.org)
- This enzyme participates in inositol phosphate metabolism and phosphatidylinositol signaling system. (wikipedia.org)
- The majority of inositol lipids reside in membranes and serve as substrates for kinases, phosphatases, and phospholipases. (asm.org)
- Phosphatidylinositol 3-kinases (PI3Ks) are important signaling molecules that phosphorylate the 3′ OH position of the inositol ring of phosphoinositides (PIs), generating the second messengers PI(3)P, PI(3,4)P 2 , and PI(3,4,5)P 3 ( 4 , 17 ). (asm.org)
- Phosphatidylinositols are acidic (anionic) phospholipids that consist of a phosphatidic acid backbone, linked via the phosphate group to inositol (hexahydroxycyclohexane). (ymdb.ca)
- Phosphatidylinositol can be phosphorylated by a number of different kinases that place the phosphate moiety on positions 4 and 5 of the inositol ring, although position 3 can also be phosphorylated by a specific kinase. (ymdb.ca)
- PIs composed exclusively of non-phosphorylated inositol exhibit a net charge of -1 at physiological pH. (ymdb.ca)
- The synthesis of PI involves CDP-activated 1,2-diacylglycerol condensation with myo-inositol. (ymdb.ca)
- Activated PI3K phosphorylates the 3′-position of the ring in inositol phospholipids, generating phosphatidylinositol ( 3 , 4 ), diphosphate, and phosphatidylinositol (3,4,5)-triphosphate (PIP3). (diabetesjournals.org)
Activation of phosphatidylinositol1
- Quercetin also inhibited Ang II-induced Shc·p85 association and subsequent activation of phosphatidylinositol 3-kinase (PI3-K)/Akt pathway in RASMC. (aspetjournals.org)
Phosphorylation of phosphatidylinositol1
- Catalyzes the phosphorylation of phosphatidylinositol 4-phosphate (PtdIns4P) to form phosphatidylinositol 4,5-bisphosphate (PtdIns(4,5)P2). (gliome.org)
Protein13
- Phosphatidylinositol-4 kinase III beta and oxysterol-binding protein accumulate unesterified cholesterol on poliovirus-induced membrane structure. (microbiologyresearch.org)
- Ang II-induced cellular events have been implicated, in part, in the activation of mitogen-activated protein (MAP) kinases. (aspetjournals.org)
- Subsequently, the phosphatidylinositol-3-kinase and mitogen-activated protein kinase pathways can be activated, resulting in proliferation and inhibition of apoptosis ( 13 , 14 ). (snmjournals.org)
- Western blotting assay was implemented to check the levels of phosphatidylinositol 3-kinase and protein kinase B. Results revealed that piperine induced dose reliant cytotoxicity in MCF-7 human breast cancer cells. (ijpsonline.com)
- Finally, Western blotting assay predicted constant expression of phosphatidylinositol 3-kinase and protein kinase B and reduced expression of phosphorylated phosphatidylinositol 3-kinase. (ijpsonline.com)
- Hence, evidenced the blocking of phosphatidylinositol 3-kinase/protein kinase B signaling pathway. (ijpsonline.com)
- It induced apoptosis, suppressed cell migration and invasion, blocked cell cycle and phosphatidylinositol 3-kinase/ protein kinase B signaling pathway. (ijpsonline.com)
- GS-002 also induced endoplasmic reticular (ER) stress as evidenced by increases in ER stress-responsive proteins including glucose-regulated protein 78 (GRP78), growth arrest- and DNA damage-inducible gene 153 (GADD153), phosphorylated eukaryotic initiation factor 2 α (eIF2 α ), phosphorylated protein endoplasmic-reticular-resident kinase (PERK), and ATF-3. (hindawi.com)
- The induction of ATF-3 expression was mediated by mitogen-activated protein kinase (MAPK) signaling pathways in GS-002-treated cells. (hindawi.com)
- Description: Using a radiometric protein kinase ( 33 PanQinase activity) assay. (guidetopharmacology.org)
- Targeting malignant disorders by attacking protein kinases has become more popular recently [ 10 ]. (biomedcentral.com)
- A member of the family of PI3Ks/mTOR is a physiologically stable serine/threonine protein kinase [ 11 ]. (biomedcentral.com)
- PTEN (MMAC1) is a lipid/protein phosphatase that can negatively regulate the PI3K pathway by dephosphorylating phosphatidylinositol (3,4,5)-triphosphate, but it is unclear whether PTEN is physiologically relevant to insulin signaling in vivo. (diabetesjournals.org)
Pathways1
- TASK-1 channels are sensitive to a wide array of physiological and pharmacological mediators that affect their activity such as unsaturated fatty acids, extracellular pH, hypoxia, anaesthetics and intracellular signalling pathways. (ersjournals.com)
Biosynthetic process1
- and phosphatidylinositol-3-phosphate biosynthetic process. (nih.gov)
PtdIns4
- PtdIns(4,5)P2 is involved in a variety of cellular processes and is the substrate to form phosphatidylinositol 3,4,5-trisphosphate (PtdIns(3,4,5)P3), another second messenger. (gliome.org)
- The majority of PtdIns(4,5)P2 is thought to occur via type I phosphatidylinositol 4-phosphate 5-kinases given the abundance of PtdIns4P. (gliome.org)
- Promotes particle attachment by generating the pool of PtdIns(4,5)P2 that induces controlled actin depolymerization to facilitate Fc-gamma-R clustering. (gliome.org)
- Controls the plasma membrane pool of PtdIns(4,5)P2 implicated in synaptic vesicle endocytosis and exocytosis. (gliome.org)
Inhibitor1
- Acanthamoeba -mediated brain endothelial cell death was abolished using LY294002, a phosphatidylinositol 3-kinase inhibitor. (asm.org)
Substrates1
- Binding of insulin to its receptor activates the insulin receptor tyrosine kinase, resulting in autophosphorylation and phosphorylation of several substrates, including insulin receptor substrate (IRS)-1 through -4. (diabetesjournals.org)
Activates1
- Next, we observed that Acanthamoeba specifically activates phosphatidylinositol 3-kinase. (asm.org)
Signaling3
- Phosphatidylinositol and the phosphatidylinositol phosphates are the main source of diacylglycerols that serve as signaling molecules, via the action of phospholipase C enzymes. (ymdb.ca)
- Signaling through the phosphatidylinositol 3′-kinase (PI3K) pathway is crucial for metabolic responses to insulin, and defects in PI3K signaling have been demonstrated in type 2 diabetes. (diabetesjournals.org)
- Phosphatidylinositol 3′-kinase (PI3K) is a crucial signaling enzyme whose activity is regulated by a variety of biological stimuli, including insulin ( 1 ). (diabetesjournals.org)
Receptor6
- The insulinlike growth factor 1 receptor (IGF-1R) is a new target for the treatment of breast cancer. (snmjournals.org)
- Although they account for only 10%-17% of all breast carcinomas ( 1 - 8 ), tumors are often high grade and patients are relatively young and have a reduced breast cancer-specific survival, compared with patients with estrogen receptor- or HER2 / neu -expressing tumors ( 2 , 9 ). (snmjournals.org)
- A potential new target for the treatment of triple-negative breast cancer is the insulinlike growth factor 1 receptor (IGF-1R). (snmjournals.org)
- On binding of insulinlike growth factors to the receptor, adaptor proteins, such as insulin-receptor substrate-1 (IRS-1) and IRS-2, are recruited to the phosphorylation site of the cytoplasmic domain ( 19 - 21 ). (snmjournals.org)
- Negatively regulates integrin alpha-L/beta-2 (LFA-1) polarization and adhesion induced by T-cell receptor. (gliome.org)
- Sorafenib (Sor) can block receptor tyrosine kinases, which are involved in the development of new blood vessels, as well as cell proliferation as a result [ 22 ]. (biomedcentral.com)
Phospholipids1
- While most phospholipids have a saturated fatty acid on C-1 and an unsaturated fatty acid on C-2 of the glycerol backbone, the fatty acid distribution at the C-1 and C-2 positions of glycerol within phospholipids is continually in flux, owing to phospholipid degradation and the continuous phospholipid remodeling that occurs while these molecules are in membranes. (ymdb.ca)
Cells4
- In infected cells, type III phosphatidylinositol 4-kinases (PI4KIIIs) generate elevated levels of PI4P, which is then exchanged for cholesterol at replication organelles. (microbiologyresearch.org)
- Thus, we hypothesized that bioflavonoids may affect Ang II-induced MAP kinase activation in cultured rat aortic smooth muscle cells (RASMC). (aspetjournals.org)
- These results were further confirmed using brain microvascular endothelial cells expressing dominant negative forms of phosphatidylinositol 3-kinase. (asm.org)
- They regulate the excitability of cells and contribute to their resting membrane potential [ 1 , 2 ]. (ersjournals.com)
Inhibition1
- Broad-range inhibition of enterovirus replication by OSW-1, a natural compound targeting OSBP. (microbiologyresearch.org)
Mechanism1
- Here we provide biochemical and cellular evidence that artemisinins are potent inhibitors of Plasmodium falciparum phosphatidylinositol-3-kinase (PfPI3K), revealing an unexpected mechanism of action. (nature.com)
Molecular1
- Design of drug-resistant alleles of type-III phosphatidylinositol 4-kinases using mutagenesis and molecular modeling. (microbiologyresearch.org)
Membrane3
- The PI 3-kinase PI3KC2α regulates mouse platelet membrane structure and function independently of membrane lipid composition. (nih.gov)
- The strong dependence of PI 3-kinase function on membrane curvature suggests possible localization of PI 3-kinase activity at sites where clustering of receptors, for example, may locally deform the membrane, and suggests that once PI 3-kinase is localized and activated at surface sites, the reaction may become self-accelerating. (tamu.edu)
- Phosphatidylinositols are important lipids, both as a key membrane constituent and as a participant in essential metabolic processes, both directly and via a number of metabolites. (ymdb.ca)
Assay1
- 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide assay was executed for determination of effects of piperine on breast cancer cell viability. (ijpsonline.com)
Type1
- Other names in common use include phosphatidylinositol kinase (phosphorylating), phosphatidylinositol 4-kinase, phosphatidylinositol kinase, type II phosphatidylinositol kinase, PI kinase, and PI 4-kinase. (wikipedia.org)
Malignant2
- The most common malignant tumor, hepatocellular carcinoma (HCC), arises from well-differentiated hepatocytes [ 1 ]. (biomedcentral.com)
- Soft tissue sarcomas are a heterogeneous group of solid malignant tumours which represent ~1% of all new cancer cases in Europe and the United States ( 1 ). (spandidos-publications.com)
Activity1
- Enables 1-phosphatidylinositol-3-kinase activity. (nih.gov)
Vesicle1
- Similar measurements using PI 4-kinase showed a weak dependence on vesicle size. (tamu.edu)
Biological2
- Biological occurrences connected to tumor development are among HCC's distinguishing characteristics [ 4 ]. (biomedcentral.com)
- Seven different isomers are known, but the most important in both quantitative and biological terms are phosphatidylinositol 4-phosphate and phosphatidylinositol 4,5-bisphosphate. (ymdb.ca)
Liver1
- Hepatocellular carcinoma (HCC) is the most frequent primary malignancy of the liver and accounts for as many as 1 million deaths annually worldwide [ 1 - 4 ]. (hindawi.com)
Family1
- TWIK-related acid-sensitive potassium channel 1 (TASK-1 encoded by KCNK3) belongs to the family of two-pore domain potassium channels. (ersjournals.com)
Levels2
- Polyubiquitination of PfPI3K and its binding to PfKelch13 were reduced by the PfKelch13 mutation, which limited proteolysis of PfPI3K and thus increased levels of the kinase, as well as its lipid product phosphatidylinositol-3-phosphate (PI3P). (nature.com)
- Amy and Sor cotreatment resulted in the highest glutathione levels and induction of pro-autophagic genes AMPK, HGMB1, ATG5, Beclin 1, and LC3, suppressed the mTOR and BCL2 anti-apoptotic gene. (biomedcentral.com)
Expression1
- Evidence is presented for PI3P-dependent signalling in which transgenic expression of an additional kinase confers resistance. (nature.com)
Belongs1
- belongs to the class of organic compounds known as phosphatidylinositols. (ymdb.ca)
Brain1
- This is the first demonstration that Acanthamoeba -mediated brain microvascular endothelial cell death is dependent on phosphatidylinositol 3-kinase. (asm.org)
Common1
- Common themes to emerge from studies of picornavirus replication are the need for cholesterol and phosphatidylinositol 4-phosphate (PI4P). (microbiologyresearch.org)
Acid1
- PIs contain almost exclusively stearic acid at carbon 1 and arachidonic acid at carbon 2. (ymdb.ca)
Regulatory1
- Recent studies show that modulation of TASK-1 channels, either directly or indirectly by targeting their regulatory mechanisms, has the potential to control pulmonary arterial tone in humans. (ersjournals.com)