1. Near-infrared fluorescent divalent RGD ligand for integrin αvβ₃-targeted optical imaging.
- Author
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Ye Y, Akers W, Xu B, Bloch S, Odonkor C, and Achilefu S
- Subjects
- Animals, Carbocyanines chemistry, Carbocyanines metabolism, Cell Line, Tumor, Fluorescent Dyes metabolism, Humans, Integrin alphaVbeta3 metabolism, Mice, Mice, Nude, Neoplasms metabolism, Oligopeptides metabolism, Fluorescent Dyes chemistry, Integrin alphaVbeta3 analysis, Neoplasms diagnosis, Oligopeptides chemistry, Optical Imaging methods
- 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., (Copyright © 2012 Elsevier Ltd. All rights reserved.)
- Published
- 2012
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