ERK Mutations and Amplification Confer Resistance to ERK-Inhibitor Therapy
نویسندگان
چکیده
منابع مشابه
ERK mutations confer resistance to mitogen-activated protein kinase pathway inhibitors.
The use of targeted therapeutics directed against BRAF(V600)-mutant metastatic melanoma improves progression-free survival in many patients; however, acquired drug resistance remains a major medical challenge. By far, the most common clinical resistance mechanism involves reactivation of the MAPK (RAF/MEK/ERK) pathway by a variety of mechanisms. Thus, targeting ERK itself has emerged as an attr...
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The MAPK pathway is frequently activated in many human cancers, particularly melanomas. A single-nucleotide mutation in BRAF resulting in the substitution of glutamic acid for valine (V(600E)) causes constitutive activation of the downstream MAPK pathway. Selective BRAF and MEK inhibitor therapies have demonstrated remarkable antitumor responses in BRAF(V600) (E)-mutant melanoma patients. Howev...
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Running Title: ERK signal suppression and sensitivity to FGFR inhibitor
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Ran-binding protein M (RanBPM) is a nucleocytoplasmic protein of yet unknown function. We have previously shown that RanBPM inhibits expression of the anti-apoptotic factor Bcl-2 and promotes apoptosis induced by DNA damage. Here we show that the effects of RanBPM on Bcl-2 expression occur through a regulation of the ERK signaling pathway. Transient and stable down-regulation of RanBPM stimulat...
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ژورنال
عنوان ژورنال: Clinical Cancer Research
سال: 2018
ISSN: 1078-0432,1557-3265
DOI: 10.1158/1078-0432.ccr-17-3674