Novel Carboxamide-Based Allosteric MEK Inhibitors: Discovery and Optimization Efforts toward XL518 (GDC-0973) - Wikidata - wikimedia - TriplyDB

Novel Carboxamide-Based Allosteric MEK Inhibitors: Discovery and Optimization Efforts toward XL518 (GDC-0973)

Novel Carboxamide-Based Allosteric MEK Inhibitors: Discovery and Optimization Efforts toward XL518 (GDC-0973)

http://www.wikidata.org/entity/Q27684146

about

MEK inhibitors and their potential in the treatment of advanced melanoma: the advantages of combination therapy Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers Insights into the binding mode of MEK type-III inhibitors. A step towards discovering and designing allosteric kinase inhibitors across the human kinome PI3'-kinase inhibition forestalls the onset of MEK1/2 inhibitor resistance in BRAF-mutated melanoma.The BRAF kinase domain promotes the development of gliomas in vivo.MEK1/2 Inhibitors: Molecular Activity and Resistance Mechanisms.Phosphoproteome analysis of the MAPK pathway reveals previously undetected feedback mechanisms.Cobimetinib: First Global Approval.Quantitative Proteomics Reveals Fundamental Regulatory Differences in Oncogenic HRAS and Isocitrate Dehydrogenase (IDH1) Driven Astrocytoma.Cobimetinib Plus Vemurafenib: A Review in BRAF (V600) Mutation-Positive Unresectable or Metastatic Melanoma.Selumetinib for the treatment of metastatic uveal melanoma: past and future perspectives.Allosteric modulators of MEK1: drug design and discovery.Modular Assembly of Allosteric MEK Inhibitor Structural Elements Unravels Potency and Feedback-Modulation Handles.Novel approaches for targeting kinases: allosteric inhibition, allosteric activation and pseudokinases.Evaluation of Cytochrome P450 3A4-Mediated Drug-Drug Interaction Potential for Cobimetinib Using Physiologically Based Pharmacokinetic Modeling and Simulation.Selective, rapid and optically switchable regulation of protein function in live mammalian cells.THE CONCISE GUIDE TO PHARMACOLOGY 2017/18: Enzymes.PIK3CA-mutated melanoma cells rely on cooperative signaling through mTORC1/2 for sustained proliferation.Rapid Iododeboronation with and without Gold Catalysis: Application to Radiolabelling of Arenes.Current Development Status of MEK Inhibitors.A guanine derivative as a new MEK inhibitor produced by Streptomyces sp. MK63-43F2.Rhodium-catalyzed direct C-H amination of benzamides with aryl azides: a synthetic route to diarylamines.A CRISPR screen identifies MAPK7 as a target for combination with MEK inhibition in KRAS mutant NSCLC.

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Novel Carboxamide-Based Allosteric MEK Inhibitors: Discovery and Optimization Efforts toward XL518 (GDC-0973)

http://www.wikidata.org/entity/Q27684146

description

2012 nî lūn-bûn

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2012 թուականի Մայիսին հրատարակուած գիտական յօդուած

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2012 թվականի մայիսին հրատարակված գիտական հոդված

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2012年の論文

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2012年学术文章

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2012年学术文章

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2012年学术文章

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2012年学术文章

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2012年学术文章

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2012年學術文章

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name

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Novel Carboxamide-Based Allost ...... fforts toward XL518 (GDC-0973)

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Novel Carboxamide-Based Allost ...... fforts toward XL518 (GDC-0973)

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Novel Carboxamide-Based Allost ...... fforts toward XL518 (GDC-0973)

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ACS Medicinal Chemistry Letters

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Novel Carboxamide-Based Allost ...... fforts toward XL518 (GDC-0973)

@en

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Abigail R Kennedy

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

Anagha A Joshi

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Angie I Kim

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Charles M Blazey

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Csaba J Peto

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Elena S Koltun

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Jean-Claire L Manalo

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Jean-Francois Martini

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

Jeffry K Curtis

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

Joerg Bussenius

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

P2860

Raf family kinases: old dogs have learned new tricks

Nerve growth factor promotes breast cancer angiogenesis by activating multiple pathways.

The discovery of the benzhydroxamate MEK inhibitors CI-1040 and PD 0325901.

A phase II study of PD-0325901, an oral MEK inhibitor, in previously treated patients with advanced non-small cell lung cancer.

Ras in cancer and developmental diseases

Osteopontin stimulates preneoplastic cellular proliferation through activation of the MAPK pathway.

Basal subtype and MAPK/ERK kinase (MEK)-phosphoinositide 3-kinase feedback signaling determine susceptibility of breast cancer cells to MEK inhibition.

Intermittent administration of MEK inhibitor GDC-0973 plus PI3K inhibitor GDC-0941 triggers robust apoptosis and tumor growth inhibition.

Hyperactivation of NF-κB via the MEK signaling is indispensable for the inhibitory effect of cAMP on DNA damage-induced cell death.

Epidermal growth factor induces matrix metalloproteinase-1 (MMP-1) expression and invasion in glioma cell lines via the MAPK pathway.

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416-21

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scholarly article

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10.1021/ML300049D

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5

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3

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2012-05-10T00:00:00Z

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24900486

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Aagianik kimischri

allosteric inhibitor

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4025802

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