| Literature DB >> 26267536 |
Roberto Ronca1, Arianna Giacomini2, Emanuela Di Salle2, Daniela Coltrini2, Katiuscia Pagano3, Laura Ragona3, Sara Matarazzo2, Sara Rezzola2, Daniele Maiolo4, Rubben Torrella5, Elisabetta Moroni5, Roberta Mazzieri6, Giulia Escobar7, Marco Mor8, Giorgio Colombo5, Marco Presta9.
Abstract
The fibroblast growth factor (FGF)/FGF receptor (FGFR) system plays a crucial role in cancer by affecting tumor growth, angiogenesis, drug resistance, and escape from anti-angiogenic anti-vascular endothelial growth factor therapy. The soluble pattern recognition receptor long-pentraxin 3 (PTX3) acts as a multi-FGF antagonist. Here we demonstrate that human PTX3 overexpression in transgenic mice driven by the Tie2 promoter inhibits tumor growth, angiogenesis, and metastasis in heterotopic, orthotopic, and autochthonous FGF-dependent tumor models. Using pharmacophore modeling of the interaction of a minimal PTX3-derived FGF-binding pentapeptide with FGF2, we identified a small-molecule chemical (NSC12) that acts as an extracellular FGF trap with significant implications in cancer therapy.Entities:
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Year: 2015 PMID： 26267536 DOI： 10.1016/j.ccell.2015.07.002
Source DB: PubMed Journal: Cancer Cell ISSN： 1535-6108 Impact factor: 31.743