title: Functionalization of small rigid platforms with cyclic RGD peptides for targeting tumors overexpressing αvβ3-integrins.
abstract: 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 αvβ3 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 αvβ3 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(β3) 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.
authors: Laboratoire de Physico-Chimie des Matériaux Luminescents, UMR 5620 CNRS - Université Claude Bernard Lyon 1, 69622 Villeurbanne Cedex, France.
authors: Jessica
authors: J
authors: Morlieras
authors: Sandrine
authors: S
authors: Dufort
authors: Lucie
authors: L
authors: Sancey
authors: Charles
authors: C
authors: Truillet
authors: Anna
authors: A
authors: Mignot
authors: Fabien
authors: F
authors: Rossetti
authors: Mario
authors: M
authors: Dentamaro
authors: Sophie
authors: S
authors: Laurent
authors: Luce
authors: L
authors: Vander Elst
authors: Robert N
authors: RN
authors: Muller
authors: Rodolphe
authors: R
authors: Antoine
authors: Philippe
authors: P
authors: Dugourd
authors: Stéphane
authors: S
authors: Roux
authors: Pascal
authors: P
authors: Perriat
authors: François
authors: F
authors: Lux
authors: Jean-Luc
authors: JL
authors: Coll
authors: Olivier
authors: O
authors: Tillement
mesh_terms: D000818:Animals; D045744:Cell Line, Tumor; D005260:Female; D057809:HEK293 Cells; D006801:Humans; D039302:Integrin alphaVbeta3 / Q000378:metabolism*; D051379:Mice; D008819:Mice, Nude; D057054:Molecular Imaging / Q000379:methods; D053758:Nanoparticles / Q000737:chemistry / Q000378:metabolism; D009369:Neoplasms / Q000175:diagnosis*; D061848:Optical Imaging / Q000379:methods; D010456:Peptides, Cyclic / Q000737:chemistry / Q000378:metabolism
chemical_list: D039302:Integrin alphaVbeta3; D010456:Peptides, Cyclic; C507169:cyclic arginine-glycine-aspartic acid peptide