Near-infrared fluorescent divalent RGD ligand for integrin αvβ₃-targeted optical imaging.

Bioorg Med Chem Lett

Department of Radiology, Optical Radiology Laboratory, Washington University School of Medicine, 4525 Scott Avenue, Saint Louis, MO 63108, USA.

Published: September 2012

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.

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http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3423536PMC
http://dx.doi.org/10.1016/j.bmcl.2012.07.044DOI Listing

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