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 αvβ3-targeting. Compared with its monovalent counterpart cypate-c(RGDfK) (2), 1 exhibited remarkable improvements in integrin αvβ3 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.
Original language | English |
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Pages (from-to) | 5405-5409 |
Number of pages | 5 |
Journal | Bioorganic and Medicinal Chemistry Letters |
Volume | 22 |
Issue number | 17 |
DOIs | |
State | Published - Sep 1 2012 |
Keywords
- Cypate
- Divalent ligand
- Integrin αβ
- Optical imaging
- RGD peptide