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

Yunpeng Ye, Walter Akers, Baogang Xu, Sharon Bloch, Charles Odonkor, Samuel Achilefu

Research output: Contribution to journalArticlepeer-review

7 Scopus citations


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 languageEnglish (US)
Pages (from-to)5405-5409
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Issue number17
StatePublished - Sep 1 2012
Externally publishedYes


  • Cypate
  • Divalent ligand
  • Integrin αβ
  • Optical imaging
  • RGD peptide

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry


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