Functionalization of Small Rigid Platforms with Cyclic RGD Peptides for Targeting Tumors Overexpressing 伪v尾3-Integrins

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• 作者：Jessica Morlieras ; Sandrine Dufort ; Lucie Sancey ; Charles Truillet ; Anna Mignot ; Fabien Rossetti ; Mario Dentamaro ; Sophie Laurent ; Luce Vander Elst ; Robert N. Muller ; Rodolphe Antoine ; Philippe Dugourd ; St茅phane Roux ; Pascal Perriat ; Fran莽ois Lux ; Jean-Luc Coll ; Olivier Tillement
• 刊名：Bioconjugate Chemistry
• 出版年：2013
• 出版时间：September 18, 2013
• 年：2013
• 卷：24
• 期：9
• 页码：1584-1597
• 全文大小：637K
• 年卷期：v.24,no.9(September 18, 2013)
• ISSN：1520-4812

文摘

Gadolinium based Small Rigid Plaforms (SRPs) have previously demonstrated their efficiency for multimodal imaging and radiosensitization. Since the RGD sequence is well-known to be highly selective for 伪_v尾₃ integrins, a cyclic pentapeptide containing the RGD motif (cRGDfK) has been grafted onto the SRP surface. An appropriate protocol led to the grafting of two targeting ligands per nano-object. The resulting nanoparticles have demonstrated a strong association with 伪_v尾₃ integrins in comparison with cRADfK grafted SRPs as negative control. Flow cytometry and fluorescence microscopy have also been used to highlight the ability of the nanoparticles to target efficiently HEK293(尾3) and U87MG cells. Finally the grafted radiosensitizing nanoparticles were intravenously injected into Nude mice bearing subcutaneous U87MG tumors and the signal observed by optical imaging was twice as high for SRP-cRGDfK compared to their negative analogue.