منابع مشابه
Isothiocyanatostilbenes as novel c-Met inhibitors
The hepatocyte growth factor receptor (HGFR or c-Met) is a driver of multiple cancer subtypes. While there are several c-Met inhibitors in development, few have been approved for clinical use, warranting the need for continued research and development of c-Met targeting therapeutic modalities. The research presented here demonstrates a particular class of compounds known as isothiocyanatostilbe...
متن کاملMET nucleotide variations and amplification in advanced ovarian cancer: characteristics and outcomes with c-Met inhibitors
PURPOSE MET alterations including amplifications and nucleotide variations have been associated with resistance to therapy and aggressive clinical behavior. EXPERIMENTAL DESIGN The medical records of patients presenting to the University of Texas MD Anderson Cancer Center Phase I Clinic with relapsed or metastatic ovarian cancers and known MET nucleotide variation or amplification status were...
متن کاملc-Myc alterations confer therapeutic response and acquired resistance to c-Met inhibitors in MET-addicted cancers.
Use of kinase inhibitors in cancer therapy leads invariably to acquired resistance stemming from kinase reprogramming. To overcome the dynamic nature of kinase adaptation, we asked whether a signal-integrating downstream effector might exist that provides a more applicable therapeutic target. In this study, we reported that the transcriptional factor c-Myc functions as a downstream effector to ...
متن کاملMET aberrations and c-MET inhibitors in patients with gastric and esophageal cancers in a phase I unit
We sought to investigate the demographics and tumor-associated features in patients with gastroesophageal (GE) malignancies referred to our Phase I Program who had formalin-fixed, paraffin-embedded tissue from archival or new biopsies tested for MET mutation and/or amplification. MET amplification was found in 5 of 76 (6.6%) patients (3/34 [8.8%] esophageal, 2/26 [7.7%] gastric and none in 22 g...
متن کاملDesign, synthesis and biological evaluation of c-Met kinase inhibitors bearing 2-oxo-1,2-dihydroquinoline scaffold.
A series of 2-oxo-1,2-dihydroquinoline-containing c-Met inhibitors were designed, synthesized and evaluated for their in vitro activities targeting c-Met. Most compounds showed high potency against c-Met with IC50 values in the single-digit nM range. Among these compounds, two target compounds, namely 1h and 1n, stood out as the most potent c-Met inhibitors with IC50s of 0.6 and 0.7nM, respecti...
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ژورنال
عنوان ژورنال: Infectious Agents and Cancer
سال: 2013
ISSN: 1750-9378
DOI: 10.1186/1750-9378-8-13