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Advances in Development of Phosphatidylinositol 3-Kinase Inhibitors

Current Medicinal Chemistry, 2009
Phosphatidylinositol 3-kinases (PI3Ks) are a class of lipid kinases that phosphorylate phosphatidylinositol 4,5-bisphosphate (PIP2) at the 3-OH of the inositol ring to generate phosphatidylinositol 3,4,5-trisphosphate (PIP3), which in turn activates Akt and the downstream effectors like mTOR, and therefore play important roles in cell growth, survival,
Dexin, Kong, Takao, Yamori
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Phosphatidylinositol-3-Kinase Inhibition in Follicular Lymphoma

Hematology/Oncology Clinics of North America, 2020
Chemoimmunotherapy is the standard frontline treatment for symptomatic or high tumor burden follicular lymphoma. Better understanding of the molecular mechanisms of lymphomagenesis has led to the development of drugs targeting these pathways. The phosphatidylinositol-3-kinase pathway is an important signaling pathway in B-cell lymphomas. Three drugs in
Ryan C, Lynch, Ajay K, Gopal
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Cancer-specific mutations in phosphatidylinositol 3-kinase

Trends in Biochemical Sciences, 2007
Cancer-specific mutations in the catalytic subunit of phosphatidylinositol 3-kinase (PI3K) p110 alpha occur in diverse tumors in frequencies that can exceed 30%. The majority of these mutations map to one of three hot spots in the gene, and the rest are distributed over much of the PI3K coding sequence.
Peter K, Vogt   +3 more
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Exercise activates the phosphatidylinositol 3-kinase pathway

Molecular Brain Research, 2005
Physical exercise is known to enhance psychological well-being and coping capacity. Voluntary physical exercise in rats also robustly and rapidly up-regulates hippocampal brain-derived neurotrophic factor (BDNF) mRNA levels, which are potentiated following a regimen of chronic antidepressant treatment. Increased BDNF levels are associated with enhanced
Michael J, Chen   +1 more
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Potent Phosphatidylinositol 3-Kinase Inhibitors and Their Biology

Current Drug Discovery Technologies, 2014
The Phosphoinositide 3-kinase (PI3k) is an important regulator of intracellular signalling pathways, like cell proliferation, migration, survival, and angiogenesis upon activation by growth factor or receptors. The PI3k's pathway is frequently up-regulated in human cancers, thus inhibition of PI3k's is a promising approach for cancer therapy.
Mukesh Chandra, Joshi   +2 more
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The inhibition of phosphatidylinositol 3-kinase by quercetin and analogs

Biochemical and Biophysical Research Communications, 1992
Phosphatidylinositol (PtdIns) 3-kinase is an enzyme involved in cellular responses to growth factors. Quercetin (2-(3,4-dihydroxyphenyl)-3,5,7-trihydroxy-4H-1-benzopyrano-4-one), a naturally occuring bioflavinoid, was found to inhibit PtdIns 3-kinase with an IC50 of 1.3 micrograms/ml (3.8 microM); inhibition appears to be directed towards the ATP ...
W F, Matter, R F, Brown, C J, Vlahos
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Phosphatidylinositol 3’ kinase: one of the effectors of Ras

Philosophical Transactions of the Royal Society of London. Series B: Biological Sciences, 1996
Abstract Ras proteins are proto-oncogene products that are critical components of signalling pathways leading from cell surface receptors to control of cellular proliferation, morphology and differentiation. The ability of Ras to activate the MAP kinase pathway through interaction with the serine/threonine kinase Raf is now well ...
Pablo Rodriguez-Viciana   +4 more
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Ras activation of phosphatidylinositol 3-kinase and akt

2001
Publisher Summary This chapter describes the Ras activation of phosphatidylinositol 3-Kinase. The interaction between Ras proteins and PI 3-kinase can be studied in vitro, using either soluble Pl 3-kinase and immobilized Ras [e.g., purified untagged Ras covalently coupled to Affi-Gel 10 beads or glutathione S-transferase (GST)-Ras bound to ...
P, Rodriguez-Viciana, J, Downward
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Regulation of granulocyte apoptosis by phosphatidylinositol 3-kinase

Biochemical Society Transactions, 2004
Granulocytes are critical components of the innate immune system whose lifespan is limited by an intrinsic, constitutive, apoptotic pathway. However, the lifespan of these cells can be extended at an inflammatory locus through interaction with survival factors.
C A, Lindemans, P J, Coffer
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Phosphatidylinositol 3-Kinase Pathway

2014
The phosphatidylinositol 3-kinase (PI3K) pathway is one of the signalling pathways activated following the interaction of a growth factor with a tyrosine kinase receptor (TKR). It follows a parallel path to the MAP kinase pathway, and similarly, it operates after binding a phosphotyrosine residue of the receptor to an adapter protein.
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