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Computational Design of Phosphatidylinositol 3-Kinase Inhibitors

ASSAY and Drug Development Technologies, 2022
One of the most sought-after therapeutic targets for treating human cancers is the phosphoinositide 3-kinase; PI3k is an integral part of the PI3K/protein kinase B signaling arcade. This pathway is frequently activated in malignancies. Drug resistance and dose-limiting adverse effects are currently associated challenges with the existing anticancer ...
Isha Rani, Anju Goyal, M. Sharma
openaire   +2 more sources

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
openaire   +2 more sources

Activation of phosphatidylinositol 3-kinase, protein kinase B, and p70 S6 kinases in lipopolysaccharide-stimulated Raw 264.7 cells: differential effects of rapamycin, Ly294002, and wortmannin on nitric oxide production.

Journal of Immunology, 1998
Phosphatidylinositol 3-kinase (PI 3-kinase) and protein kinase B are critical players in cell proliferation and survival. Their downstream effector protein kinase, p70 S6 kinase, has an established role in protein translation.
Bill Salh   +4 more
semanticscholar   +1 more source

Phosphorylation of Unnatural Phosphatidylinositols with Phosphatidylinositol 3-Kinase

Tetrahedron, 2000
Phosphatidylinositol analogs (PIC2–PIC18) having a series of saturated fatty acid (C2–C18) at sn-2 position were synthesized and subjected to the phosphorylation reaction with phosphatidylinositol 3-kinase (PI 3-kinase). The reactivity of PIC8 with PI 3-kinase turned out to be comparable to that of natural PI, although PIC18 was not phosphorylated ...
Naoko Morisaki   +6 more
openaire   +1 more source

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
openaire   +2 more sources

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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Phosphatidylinositol 3′ Kinase Signaling in Mammary Tumorigenesis

Journal of Mammary Gland Biology and Neoplasia, 2001
Suppression of apoptosis is now recognized as a key contributory element to tumorigenesis in animal models and human cancer. The phosphatidylinositol 3' kinase pathway plays a seminal role in cell death suppression or "survival signaling." Over the past 5 years, the molecular mechanisms by which this pathway exerts its death suppressive effects have ...
M P, Scheid, J R, Woodgett
openaire   +2 more sources

New phosphatidylinositol 3-kinase inhibitors for cancer

Expert Opinion on Investigational Drugs, 2011
Cancer treatment is moving away from conventional cytotoxic drugs and towards agents that target specific proteins important to cancer development or survival. The PI3K signaling axis is an important pathway involved in myriad human malignancies. Inhibition of this axis is a promising therapeutic approach for several cancers.This article reviews ...
Daniel W, Bowles, Antonio, Jimeno
openaire   +2 more sources

Expression of Phosphatidylinositol-3 Kinase in Lung Cancer

Bulletin of Experimental Biology and Medicine, 2000
The expression of phosphatidylinositol-3 kinase in tumors and homologous tissues from 29 patients with lung cancer, 5 patients with lung metastases of various tumors, and some non-tumorous pulmonary diseases was studied by Western blot analysis.
E S, Gershtein   +4 more
openaire   +2 more sources

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