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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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Ye Y,Akers W,Xu B,Bloch S,Odonkor C,Achilefu S

doi

10.1016/j.bmcl.2012.07.044

subject

Has Abstract

pub_date

2012-09-01 00:00:00

pages

5405-9

issue

17

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(12)00920-1

journal_volume

22

pub_type

杂志文章

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