title: Near-infrared fluorescent divalent RGD ligand for integrin αvβ₃-targeted optical imaging.
abstract: A new near-infrared fluorescent compound containing two cyclic RGD motifs, cypate-[c(RGDfK)](2) (1), was synthesized based on a carbocyanine fluorophore bearing two carboxylic acid groups (cypate) for integrin α(v)β(3)-targeting. Compared with its monovalent counterpart cypate-c(RGDfK) (2), 1 exhibited remarkable improvements in integrin α(v)β(3) binding affinity and tumor uptake in nude mice of A549. The results suggest that cypate-linked divalent ligands can serve as an important molecular platform for exploring receptor-targeted optical imaging and treatment of various diseases.
authors.affiliation: Department of Radiology, Optical Radiology Laboratory, Washington University School of Medicine, 4525 Scott Avenue, Saint Louis, MO 63108, USA.
authors.forename: Yunpeng
authors.initials: Y
authors.lastname: Ye
authors.forename: Walter
authors.initials: W
authors.lastname: Akers
authors.forename: Baogang
authors.initials: B
authors.lastname: Xu
authors.forename: Sharon
authors.initials: S
authors.lastname: Bloch
authors.forename: Charles
authors.initials: C
authors.lastname: Odonkor
authors.forename: Samuel
authors.initials: S
authors.lastname: Achilefu
mesh_terms: D000818:Animals; D002232:Carbocyanines / Q000737:chemistry / Q000378:metabolism; D045744:Cell Line, Tumor; D005456:Fluorescent Dyes / Q000737:chemistry* / Q000378:metabolism; D006801:Humans; D039302:Integrin alphaVbeta3 / Q000032:analysis* / Q000378:metabolism; D051379:Mice; D008819:Mice, Nude; D009369:Neoplasms / Q000175:diagnosis* / Q000378:metabolism; D009842:Oligopeptides / Q000737:chemistry* / Q000378:metabolism; D061848:Optical Imaging / Q000379:methods*
chemical_list: D002232:Carbocyanines; D005456:Fluorescent Dyes; D039302:Integrin alphaVbeta3; D009842:Oligopeptides; C047981:arginyl-glycyl-aspartic acid