KRC-327, a selective novel inhibitor of c-Met receptor tyrosine kinase with anticancer activity

Highlights ► KRC-327 is a highly selective small-molecule inhibitor targeting the catalytic activity of c-Met. ► KRC-327 showed a prominent inhibitory effect on the c-Met activation and its signaling pathway in human cancer cells. ► KRC-327 inhibited proliferation and Migration of HGF-stimulated can...

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Veröffentlicht in:	Cancer letters 2013-05, Vol.331 (2), p.158-166
Hauptverfasser:	Park, Byung Hee, Jung, Kyung Hee, Yun, Sun-Mi, Hong, Sang-Won, Ryu, Jae Wook, Jung, Heejung, Ha, Jae Du, Lee, Jongkook, Hong, Soon-Sun
Format:	Artikel
Sprache:	eng
Schlagworte:	AKT protein animal models anticarcinogenic activity Antineoplastic Agents - pharmacology c-Met Cancer carcinogenesis Cell cycle Cell growth Cell Line, Tumor Drug Screening Assays, Antitumor drugs Fluorescent Antibody Technique Hematology, Oncology and Palliative Medicine hepatocyte growth factor HGF Humans Isoquinolines - pharmacology Kinases KRC-327 metastasis Neoplasms - pathology Phosphorylation Protein Kinase Inhibitors - pharmacology Pyridazines - pharmacology Receptor Protein-Tyrosine Kinases - antagonists & inhibitors Receptor Protein-Tyrosine Kinases - metabolism transcription factors tyrosine
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Zusammenfassung:	Highlights ► KRC-327 is a highly selective small-molecule inhibitor targeting the catalytic activity of c-Met. ► KRC-327 showed a prominent inhibitory effect on the c-Met activation and its signaling pathway in human cancer cells. ► KRC-327 inhibited proliferation and Migration of HGF-stimulated cancer cells. ► KRC-327 significantly delayed tumor growth by targeting c-Met signaling pathway. ► KRC-327 may be a potential anticanceragentto target c-Metpathway in various c-Met activated cancers.
ISSN:	0304-3835 1872-7980
DOI:	10.1016/j.canlet.2012.12.025