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Near-infrared fluorescent divalent RGD ligand for integrin ?v??-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 ?(v)?(3)-targeting. Compared with its monovalent counterpart cypate-c(RGDfK) (2), 1 exhibited remarkable improvements in integrin ?(v)?(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.

SUBMITTER: Ye Y

PROVIDER: S-EPMC3423536 | biostudies-literature | 2012 Sep

REPOSITORIES: biostudies-literature

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

Ye Yunpeng Y Akers Walter W Xu Baogang B Bloch Sharon S Odonkor Charles C Achilefu Samuel S

Bioorganic & medicinal chemistry letters 20120720 17

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 pla ...[more]

PMID: 22871580

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