ARQ 197, a novel and selective inhibitor of the human c-Met receptor tyrosine kinase with antitumor activity

The met proto-oncogene is functionally linked with tumorigenesis and metastatic progression. Validation of the receptor tyrosine kinase c-Met as a selective anticancer target has awaited the emergence of selective c-Met inhibitors. Herein, we report ARQ 197 as the first non-ATP-competitive small mol...

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Veröffentlicht in:	Molecular cancer therapeutics 2010-06, Vol.9 (6), p.1544-1553
Hauptverfasser:	Munshi, Neru, Jeay, Sébastien, Li, Youzhi, Chen, Chang-Rung, France, Dennis S, Ashwell, Mark A, Hill, Jason, Moussa, Magdi M, Leggett, David S, Li, Chiang J
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Apoptosis - drug effects Caspases - metabolism Cell Line, Tumor Cell Proliferation - drug effects Humans Immunosuppression Mice Mice, Nude Neoplasms - enzymology Neoplasms - pathology Phosphorylation - drug effects Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - pharmacology Proto-Oncogene Proteins c-met - antagonists & inhibitors Pyrroles - chemistry Pyrroles - pharmacology Pyrrolidinones - chemistry Pyrrolidinones - pharmacology Quinolines - chemistry Quinolines - pharmacology Signal Transduction - drug effects Xenograft Model Antitumor Assays
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