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Targeting the mTOR kinase domain: the second generation of mTOR inhibitors

Targeting the mTOR kinase domain: the second generation of mTOR inhibitors

http://www.wikidata.org/entity/Q24622194

about

Rab1A is an mTORC1 activator and a colorectal oncogene The PI3K/Akt/mTOR pathway in ovarian cancer: therapeutic opportunities and challenges mTOR kinase inhibitors as potential cancer therapeutic drugs mTOR-independent 4E-BP1 phosphorylation is associated with cancer resistance to mTOR kinase inhibitors.Judicious Toggling of mTOR Activity to Combat Insulin Resistance and Cancer: Current Evidence and Perspectives Targeting Strategies for Renal Cell Carcinoma: From Renal Cancer Cells to Renal Cancer Stem Cells Structure-activity relationships study of mTOR kinase inhibition using QSAR and structure-based drug design approaches ATP-competitive mTOR kinase inhibitors delay plant growth by triggering early differentiation of meristematic cells but no developmental patterning change.Maintaining glycogen synthase kinase-3 activity is critical for mTOR kinase inhibitors to inhibit cancer cell growth.Bacterial proteins and peptides in cancer therapy: today and tomorrow Ras/Raf/MEK/ERK and PI3K/PTEN/Akt/mTOR cascade inhibitors: how mutations can result in therapy resistance and how to overcome resistance.General aspects of colorectal cancer Combination of mTOR and EGFR kinase inhibitors blocks mTORC1 and mTORC2 kinase activity and suppresses the progression of colorectal carcinoma Rapamycin inhibits mSin1 phosphorylation independently of mTORC1 and mTORC2.Torin2 targets dysregulated pathways in anaplastic thyroid cancer and inhibits tumor growth and metastasis.Rapamycin induces Bad phosphorylation in association with its resistance to human lung cancer cells.mTOR Complex 2 Stabilizes Mcl-1 Protein by Suppressing Its Glycogen Synthase Kinase 3-Dependent and SCF-FBXW7-Mediated Degradation.High-dose rapamycin induces apoptosis in human cancer cells by dissociating mTOR complex 1 and suppressing phosphorylation of 4E-BP1.Aerobic glycolysis tunes YAP/TAZ transcriptional activity Role of DJ-1 siRNA in reverse sensitivity of breast cancer cells to chemotherapy and its possible mechanism.Structure-activity analysis of niclosamide reveals potential role for cytoplasmic pH in control of mammalian target of rapamycin complex 1 (mTORC1) signaling Expression profiling and functional analysis reveals that TOR is a key player in regulating photosynthesis and phytohormone signaling pathways in Arabidopsis.Aberrant amino acid signaling promotes growth and metastasis of hepatocellular carcinomas through Rab1A-dependent activation of mTORC1 by Rab1A PP2AC Level Determines Differential Programming of p38-TSC-mTOR Signaling and Therapeutic Response to p38-Targeted Therapy in Colorectal Cancer.Identification of a Non-Gatekeeper Hot Spot for Drug-Resistant Mutations in mTOR Kinase.N-Hydroxyphthalimide exhibits antitumor activity by suppressing mTOR signaling pathway in BT-20 and LoVo cells.The Enigma of Rapamycin Dosage.Activation of lysosomal function in the course of autophagy via mTORC1 suppression and autophagosome-lysosome fusion.5-Aminoimidazole-4-carboxamide-1-β-4-ribofuranoside (AICAR) enhances the efficacy of rapamycin in human cancer cells.Inhibition of S6 kinase suppresses the apoptotic effect of eIF4E ablation by inducing TGF-β-dependent G1 cell cycle arrest.Rationale-based therapeutic combinations with PI3K inhibitors in cancer treatment miR-99b-targeted mTOR induction contributes to irradiation resistance in pancreatic cancer.Incomplete inhibition of phosphorylation of 4E-BP1 as a mechanism of primary resistance to ATP-competitive mTOR inhibitors Targeting mTOR network in colorectal cancer therapy PI3K and Akt as molecular targets for cancer therapy: current clinical outcomes.Rapamycin passes the torch: a new generation of mTOR inhibitors.Homeostasis and the importance for a balance between AKT/mTOR activity and intracellular signaling.The mTOR signaling pathway in the brain: focus on epilepsy and epileptogenesis.Targeting oncogenic and epigenetic survival pathways in lymphoma.Therapeutic targeting of the mTOR-signalling pathway in cancer: benefits and limitations

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Targeting the mTOR kinase domain: the second generation of mTOR inhibitors

http://www.wikidata.org/entity/Q24622194

description

2011 nî lūn-bûn

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2011 թուականի Ապրիլին հրատարակուած գիտական յօդուած

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2011 թվականի ապրիլին հրատարակված գիտական հոդված

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2011年の論文

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2011年論文

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2011年論文

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2011年論文

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2011年論文

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2011年論文

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2011年论文

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name

Targeting the mTOR kinase domain: the second generation of mTOR inhibitors

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Targeting the mTOR kinase domain: the second generation of mTOR inhibitors

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Targeting the mTOR kinase domain: the second generation of mTOR inhibitors

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type

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Targeting the mTOR kinase domain: the second generation of mTOR inhibitors

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Targeting the mTOR kinase domain: the second generation of mTOR inhibitors

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Targeting the mTOR kinase domain: the second generation of mTOR inhibitors

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prefLabel

Targeting the mTOR kinase domain: the second generation of mTOR inhibitors

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Targeting the mTOR kinase domain: the second generation of mTOR inhibitors

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Targeting the mTOR kinase domain: the second generation of mTOR inhibitors

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J.DRUDIS.2011.02.008

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Drug Discovery Today

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Targeting the mTOR kinase domain: the second generation of mTOR inhibitors

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X F Steven Zheng

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Yan-Jie Zhang

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Yanwen Duan

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P2860

Active-site inhibitors of mTOR target rapamycin-resistant outputs of mTORC1 and mTORC2

First-in-class, first-in-human phase I results of targeted agents: highlights of the 2008 American society of clinical oncology meeting

Targeting the mTOR signaling network for cancer therapy

Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases

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

Defining the role of mTOR in cancer

Critical role for the p110alpha phosphoinositide-3-OH kinase in growth and metabolic regulation

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

An ATP-competitive mammalian target of rapamycin inhibitor reveals rapamycin-resistant functions of mTORC1

Identification and characterization of NVP-BEZ235, a new orally available dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor with potent in vivo antitumor activity

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