Long-Pentraxin 3 Derivative as a Small-Molecule FGF Trap for Cancer Therapy

Ronca, Roberto, Giacomini, Arianna, Di Salle, Emanuela, Coltrini, Daniela, Pagano, Katiuscia, Ragona, Laura, Matarazzo, Sara, Rezzola, Sara, Maiolo, Daniele, Torrella, Rubben, Moroni, Elisabetta, Mazzieri, Roberta, Escobar, Giulia, Mor, Marco, Colombo, Giorgio and Presta, Marco (2015) Long-Pentraxin 3 Derivative as a Small-Molecule FGF Trap for Cancer Therapy. Cancer Cell, 28 2: 225-239. doi:10.1016/j.ccell.2015.07.002

Author Ronca, Roberto
Giacomini, Arianna
Di Salle, Emanuela
Coltrini, Daniela
Pagano, Katiuscia
Ragona, Laura
Matarazzo, Sara
Rezzola, Sara
Maiolo, Daniele
Torrella, Rubben
Moroni, Elisabetta
Mazzieri, Roberta
Escobar, Giulia
Mor, Marco
Colombo, Giorgio
Presta, Marco
Title Long-Pentraxin 3 Derivative as a Small-Molecule FGF Trap for Cancer Therapy
Journal name Cancer Cell   Check publisher's open access policy
ISSN 1535-6108
Publication date 2015-08-10
Year available 2015
Sub-type Article (original research)
DOI 10.1016/j.ccell.2015.07.002
Open Access Status Not Open Access
Volume 28
Issue 2
Start page 225
End page 239
Total pages 5
Place of publication Cambridge, MA United States
Publisher Cell Press
Collection year 2016
Language eng
Formatted 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.
Q-Index Code C1
Q-Index Status Confirmed Code
Institutional Status UQ

Document type: Journal Article
Sub-type: Article (original research)
Collections: Official 2016 Collection
UQ Diamantina Institute Publications
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Citation counts: Scopus Citation Count Cited 12 times in Scopus Article | Citations
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Created: Tue, 25 Aug 2015, 16:27:20 EST by Roberta Mazzieri on behalf of UQ Diamantina Institute