Preclinical validation of the small molecule drug quininib as a novel therapeutic for colorectal cancer

Colorectal cancer (CRC) is a leading cause of cancer deaths. Molecularly targeted therapies ( e.g . bevacizumab) have improved survival rates but drug resistance ultimately develops and newer therapies are required. We identified quininib as a small molecule drug with anti-angiogenic activity using...

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Veröffentlicht in:	Scientific reports 2016-10, Vol.6 (1), p.34523-34523, Article 34523
Hauptverfasser:	Murphy, Adrian G., Casey, Rory, Maguire, Aoife, Tosetto, Miriam, Butler, Clare T., Conroy, Emer, Reynolds, Alison L., Sheahan, Kieran, O’Donoghue, Diarmuid, Gallagher, William M., Fennelly, David, Kennedy, Breandán N., O’Sullivan, Jacintha
Format:	Artikel
Sprache:	eng
Schlagworte:	13 13/21 38 38/77 59 59/5 64 64/116 64/60 692/4028/67/1059/153 692/4028/67/1504/1885/1393 96 96/98 Angiogenesis Angiogenesis Inhibitors - therapeutic use Animal models Animals Antineoplastic Agents - therapeutic use Bevacizumab Blood Vessels - drug effects Cell adhesion & migration Cell Line Cell migration Cell survival Colorectal cancer Colorectal carcinoma Colorectal Neoplasms - complications Colorectal Neoplasms - drug therapy Colorectal Neoplasms - metabolism Colorectal Neoplasms - pathology Drug resistance Embryos Endothelial Cells - drug effects Explants Gene Expression HT29 Cells Humanities and Social Sciences Humans Inflammation Mediators - metabolism Interleukin 6 Interleukin 8 Interleukin-6 - secretion Interleukin-8 - secretion Mice, Inbred BALB C Molecular weight Monoclonal antibodies Monocyte chemoattractant protein 1 multidisciplinary Neovascularization, Pathologic - complications Neovascularization, Pathologic - metabolism Phenols Phenols - therapeutic use Quinolines - therapeutic use Science Secretions Survival Targeted cancer therapy Tumor necrosis factor Tumors Vascular endothelial growth factor Vascular Endothelial Growth Factor A - secretion Xenograft Model Antitumor Assays Xenografts Zebrafish
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Zusammenfassung:	Colorectal cancer (CRC) is a leading cause of cancer deaths. Molecularly targeted therapies ( e.g . bevacizumab) have improved survival rates but drug resistance ultimately develops and newer therapies are required. We identified quininib as a small molecule drug with anti-angiogenic activity using in vitro , ex vivo and in vivo screening models. Quininib (2-[( E )-2-(Quinolin-2-yl) vinyl] phenol), is a small molecule drug (molecular weight 283.75 g/mol), which significantly inhibited blood vessel development in zebrafish embryos (p
ISSN:	2045-2322 2045-2322
DOI:	10.1038/srep34523