Enhanced inhibition of ERK signaling by a novel allosteric MEK inhibitor, CH5126766, that suppresses feedback reactivation of RAF activity. - Wikidata - wikimedia - TriplyDB

Enhanced inhibition of ERK signaling by a novel allosteric MEK inhibitor, CH5126766, that suppresses feedback reactivation of RAF activity.

Enhanced inhibition of ERK signaling by a novel allosteric MEK inhibitor, CH5126766, that suppresses feedback reactivation of RAF activity.

http://www.wikidata.org/entity/Q33971120

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Disruption of CRAF-mediated MEK activation is required for effective MEK inhibition in KRAS mutant tumors Combination Therapies to Inhibit the RAF/MEK/ERK Pathway in Melanoma: We are not Done Yet Network-level effects of kinase inhibitors modulate TNF-α-induced apoptosis in the intestinal epithelium Molecular pathways: targeting NRAS in melanoma and acute myelogenous leukemia.Change or die: targeting adaptive signaling to kinase inhibition in cancer cells.The dual RAF/MEK inhibitor CH5126766/RO5126766 may be a potential therapy for RAS-mutated tumor cells.Drugging the undruggable RAS: Mission possible?Dual inhibition of allosteric mitogen-activated protein kinase (MEK) and phosphatidylinositol 3-kinase (PI3K) oncogenic targets with a bifunctional inhibitor Dual PI3K/mTOR Inhibitors Induce Rapid Overactivation of the MEK/ERK Pathway in Human Pancreatic Cancer Cells through Suppression of mTORC2.Evaluation of efficacy of a new MEK inhibitor, RO4987655, in human tumor xenografts by [(18)F] FDG-PET imaging combined with proteomic approaches.MEK1/2 Inhibitors: Molecular Activity and Resistance Mechanisms.ERBB activation modulates sensitivity to MEK1/2 inhibition in a subset of driver-negative melanoma Allosteric MEK1/2 inhibitor refametinib (BAY 86-9766) in combination with sorafenib exhibits antitumor activity in preclinical murine and rat models of hepatocellular carcinoma.[18 F]FDG-PET imaging is an early non-invasive pharmacodynamic biomarker for a first-in-class dual MEK/Raf inhibitor, RO5126766 (CH5126766), in preclinical xenograft models.Mechanism and consequences of RAF kinase activation by small-molecule inhibitors "RAF" neighborhood: protein-protein interaction in the Raf/Mek/Erk pathway.Intrinsic and acquired resistance to MEK1/2 inhibitors in cancer.Targeting RAS-mutant cancers: is ERK the key?Oncogene addiction: pathways of therapeutic response, resistance, and road maps toward a cure.Sorafenib-based combined molecule targeting in treatment of hepatocellular carcinoma.Selumetinib for the treatment of metastatic uveal melanoma: past and future perspectives.Modular Assembly of Allosteric MEK Inhibitor Structural Elements Unravels Potency and Feedback-Modulation Handles.Computational study on the unbinding pathways of B-RAF inhibitors and its implication for the difference of residence time: insight from random acceleration and steered molecular dynamics simulations.Vertical inhibition of the MAPK pathway enhances therapeutic responses in NRAS-mutant melanoma.Molecular-targeting therapies against quantitative abnormalities in gene expression with malignant tumors.Sustained ERK inhibition maximizes responses of BrafV600E thyroid cancers to radioiodine.Fluorine Scanning by Nonselective Fluorination: Enhancing Raf/MEK Inhibition while Keeping Physicochemical Properties.Optimizing the Physicochemical Properties of Raf/MEK Inhibitors by Nitrogen Scanning.Non-canonical PI3K-Cdc42-Pak-Mek-Erk Signaling Promotes Immune-Complex-Induced Apoptosis in Human Neutrophils.Inhibition of MEK1 Signaling Pathway in the Liver Ameliorates Insulin Resistance.Inhibition of the PI3K/AKT/mTOR pathway activates autophagy and compensatory Ras/Raf/MEK/ERK signalling in prostate cancer Redifferentiation of Radioiodine Refractory Differentiated Thyroid Cancer for Reapplication of I-131 Therapy.Allele-Specific Mechanisms of Activation of MEK1 Mutants Determine Their Properties.Blockage of the mevalonate pathway overcomes the apoptotic resistance to MEK inhibitors with suppressing the activation of Akt in cancer cells.Galectin-3-Mediated Glial Crosstalk Drives Oligodendrocyte Differentiation and (Re)myelination

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P2860

Enhanced inhibition of ERK signaling by a novel allosteric MEK inhibitor, CH5126766, that suppresses feedback reactivation of RAF activity.

http://www.wikidata.org/entity/Q33971120

description

2013 nî lūn-bûn

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2013 թուականի Մայիսին հրատարակուած գիտական յօդուած

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2013 թվականի մայիսին հրատարակված գիտական հոդված

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2013年の論文

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2013年論文

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2013年論文

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2013年論文

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2013年論文

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2013年論文

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Enhanced inhibition of ERK sig ...... reactivation of RAF activity.

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Enhanced inhibition of ERK sig ...... reactivation of RAF activity.

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Enhanced inhibition of ERK sig ...... reactivation of RAF activity.

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Enhanced inhibition of ERK sig ...... reactivation of RAF activity.

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0008-5472.CAN-12-3937

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Cancer Research

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Enhanced inhibition of ERK sig ...... reactivation of RAF activity.

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Eric W Joseph

http://www.w3.org/2001/XMLSchema#string

Hiroshi Sakamoto

http://www.w3.org/2001/XMLSchema#string

Hitoshi Iikura

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Kazuhiro Ohara

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Mikio Arisawa

http://www.w3.org/2001/XMLSchema#string

Naoki Harada

http://www.w3.org/2001/XMLSchema#string

Neal Rosen

http://www.w3.org/2001/XMLSchema#string

Nobuo Shimma

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Nobuya Ishii

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Poulikos I Poulikakos

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P2860

The RAF inhibitor PLX4032 inhibits ERK signaling and tumor cell proliferation in a V600E BRAF-selective manner

Kinase-dead BRAF and oncogenic RAS cooperate to drive tumor progression through CRAF

Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma

Improved survival with vemurafenib in melanoma with BRAF V600E mutation

RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth

Safety, pharmacokinetic, pharmacodynamic, and efficacy data for the oral MEK inhibitor trametinib: a phase 1 dose-escalation trial.

PD 098059 is a specific inhibitor of the activation of mitogen-activated protein kinase kinase in vitro and in vivo

RAF inhibitors transactivate RAF dimers and ERK signalling in cells with wild-type BRAF

Improved survival with MEK inhibition in BRAF-mutated melanoma

Sprouty1 and Sprouty2 provide a control mechanism for the Ras/MAPK signalling pathway.

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4050-4060

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10.1158/0008-5472.CAN-12-3937

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13

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236692957

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23667175

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allosteric inhibitor

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4115369

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