Discovery of GSK2126458, a Highly Potent Inhibitor of PI3K and the Mammalian Target of Rapamycin - Wikidata - thesis-toulmin - TriplyDB

Discovery of GSK2126458, a Highly Potent Inhibitor of PI3K and the Mammalian Target of Rapamycin

Discovery of GSK2126458, a Highly Potent Inhibitor of PI3K and the Mammalian Target of Rapamycin

http://www.wikidata.org/entity/Q27684091

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Discovery of 1-(4-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2(1H)-one as a highly potent, selective mammalian target of rapamycin (mTOR) inhibitor for the treatment of cancer Targeting the mTOR kinase domain: the second generation of mTOR inhibitors Recent development of ATP-competitive small molecule phosphatidylinostitol-3-kinase inhibitors as anticancer agents Judicious Toggling of mTOR Activity to Combat Insulin Resistance and Cancer: Current Evidence and Perspectives mTOR inhibitors in cancer therapy Biological characterization of 3-(2-amino-ethyl)-5-[3-(4-butoxyl-phenyl)-propylidene]-thiazolidine-2,4-dione (K145) as a selective sphingosine kinase-2 inhibitor and anticancer agent Predicting mTOR inhibitors with a classifier using recursive partitioning and Naïve Bayesian approaches Anticancer compound plumbagin and its molecular targets: a structural insight into the inhibitory mechanisms using computational approaches Relationships between signaling pathway usage and sensitivity to a pathway inhibitor: examination of trametinib responses in cultured breast cancer lines Potentiation of Growth Inhibitory Responses of the mTOR Inhibitor Everolimus by Dual mTORC1/2 Inhibitors in Cultured Breast Cancer Cell Lines Acquired resistance to BRAF inhibitors mediated by a RAF kinase switch in melanoma can be overcome by cotargeting MEK and IGF-1R/PI3K Recent advances in the use of PI3K inhibitors for glioblastoma multiforme: current preclinical and clinical development Recent advances in the discovery of small molecule mTOR inhibitors.Small-molecule inhibitors of the PI3K signaling network Blocking the mTOR pathway: a drug discovery perspective.The concept of privileged structures in rational drug design: focus on acridine and quinoline scaffolds in neurodegenerative and protozoan diseases.mTOR kinase: a possible pharmacological target in the management of chronic pain.Comparison of the effects of the PI3K/mTOR inhibitors NVP-BEZ235 and GSK2126458 on tamoxifen-resistant breast cancer cells.Discovery of a Potent Class of PI3Kα Inhibitors with Unique Binding Mode via Encoded Library Technology (ELT).Biological evaluation and docking studies of recently identified inhibitors of phosphoinositide-3-kinases.Docking studies on isoform-specific inhibition of phosphoinositide-3-kinases.Development of a test that measures real-time HER2 signaling function in live breast cancer cell lines and primary cells.Discovering new mTOR inhibitors for cancer treatment through virtual screening methods and in vitro assays.Factors Influencing the Central Nervous System Distribution of a Novel Phosphoinositide 3-Kinase/Mammalian Target of Rapamycin Inhibitor GSK2126458: Implications for Overcoming Resistance with Combination Therapy for Melanoma Brain Metastases.The effects of anticancer drugs TSA and GSK on spermatogenesis in male mice Nimbolide, a neem limonoid inhibits Phosphatidyl Inositol-3 Kinase to activate Glycogen Synthase Kinase-3β in a hamster model of oral oncogenesis.Auranofin-mediated inhibition of PI3K/AKT/mTOR axis and anticancer activity in non-small cell lung cancer cells.Torin2 Suppresses Ionizing Radiation-Induced DNA Damage Repair Exploration of a potent PI3 kinase/mTOR inhibitor as a novel anti-fibrotic agent in IPF Phosphatidylinositol 3-kinase (PI3K) inhibitors as cancer therapeutics.Estrogen receptor-positive breast cancer molecular signatures and therapeutic potentials (Review).Class I phosphatidylinositol 3-kinase inhibitors for cancer therapy.Endothelin-1 suppresses insulin-stimulated Akt phosphorylation and glucose uptake via GPCR kinase 2 in skeletal muscle cells.Current and future directions in mammalian target of rapamycin inhibitors development.Targeting phosphatidylinositol 3 kinase (PI3K)-Akt beyond rapalogs.Recent advances in the discovery of small-molecule ATP competitive mTOR inhibitors: a patent review.Progress in the preclinical discovery and clinical development of class I and dual class I/IV phosphoinositide 3-kinase (PI3K) inhibitors.Pyrazolo[3,4-b]pyridine kinase inhibitors: a patent review (2008--present).Furthering the design and the discovery of small molecule ATP-competitive mTOR inhibitors as an effective cancer treatment.Analysis of phosphoinositide 3-kinase inhibitors by bottom-up electron-transfer dissociation hydrogen/deuterium exchange mass spectrometry.

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Discovery of GSK2126458, a Highly Potent Inhibitor of PI3K and the Mammalian Target of Rapamycin

http://www.wikidata.org/entity/Q27684091

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2010 nî lūn-bûn

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2010 թուականի Ապրիլին հրատարակուած գիտական յօդուած

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2010 թվականի ապրիլին հրատարակված գիտական հոդված

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2010年の論文

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2010年学术文章

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2010年学术文章

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2010年学术文章

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2010年学术文章

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2010年学术文章

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2010年學術文章

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Discovery of GSK2126458, a Hig ...... Mammalian Target of Rapamycin

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Discovery of GSK2126458, a Hig ...... Mammalian Target of Rapamycin

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Discovery of GSK2126458, a Hig ...... Mammalian Target of Rapamycin

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Discovery of GSK2126458, a Hig ...... Mammalian Target of Rapamycin

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Discovery of GSK2126458, a Hig ...... Mammalian Target of Rapamycin

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Discovery of GSK2126458, a Hig ...... Mammalian Target of Rapamycin

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Discovery of GSK2126458, a Hig ...... Mammalian Target of Rapamycin

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ACS Medicinal Chemistry Letters

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Discovery of GSK2126458, a Hig ...... Mammalian Target of Rapamycin

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Amita M Chaudhari

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Carla A Donatelli

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Chiu-Mei Sung

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Christian S Sherk

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Christine M Gardiner

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Cynthia A Parrish

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Dashyant Dhanak

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David Sutton

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Eric Garver

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Glenn S Van Aller

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Phosphorylation and regulation of Akt/PKB by the rictor-mTOR complex

A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling

Structural Determinants of Phosphoinositide 3-Kinase Inhibition by Wortmannin, LY294002, Quercetin, Myricetin, and Staurosporine

The structure of a human p110alpha/p85alpha complex elucidates the effects of oncogenic PI3Kalpha mutations

The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer

Phosphatidylinositol 3-kinase mutations identified in human cancer are oncogenic

High frequency of mutations of the PIK3CA gene in human cancers

Signaling by distinct classes of phosphoinositide 3-kinases

PDGF-dependent tyrosine phosphorylation stimulates production of novel polyphosphoinositides in intact cells

The evolution of phosphatidylinositol 3-kinases as regulators of growth and metabolism

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