New Glucocyclic RGD Dimers for Positron Emission Tomography Imaging of Tumor Integrin Receptors

Ji Woong Lee, Ji Ae Park, Yong Jin Lee, Un Chol Shin, Suhng Wook Kim, Byung Il Kim, Sang Moo Lim, Gwang Il An, Jung Young Kim, Kyo Chul Lee

Research output: Contribution to journalArticlepeer-review

5 Citations (Scopus)


Most studies of radiolabeled arginine-glycine-aspartic acid (RGD) peptides have shown in vitro affinity for integrin ανβ3, allowing for the targeting of receptor-positive tumors in vivo. However, major differences have been found in the pharmacokinetic profiles of different radiolabeled RGD peptide analogs. The purposes of this study were to prepare 64Cu-DOTA-gluco-E[c(RGDfK)]2 (R8), 64Cu-NOTA-gluco-E[c(RGDfK)]2 (R9), and 64Cu-NODAGA-gluco-E[c(RGDfK)]2 (R10) and compare their pharmacokinetics and tumor imaging properties using small-animal positron emission tomography (PET). All three compounds were produced with high specific activity within 10 minutes. The IC50 values were similar for all the substances, and their affinities were greater than that of c(RGDyK). R8, R9, and R10 were stable for 24 hours in human and mouse serums and showed high uptake in U87MG tumors with high tumor-to-blood ratios. Compared to the control, a cyclic RGD peptide dimer without glucosamine, R10, showed low uptake in the liver. Because of their good imaging qualities and improved pharmacokinetics, 64Cu-labeled dimer RGD conjugates (R8, R9, and R10) may have potential applications as PET radiotracers. R9 (NOTA) with highly in vivo stability consequentially showed an improved PET tumor uptake than R8 (DOTA) or R10 (NODAGA).

Original languageEnglish
Pages (from-to)209-216
Number of pages8
JournalCancer Biotherapy and Radiopharmaceuticals
Issue number6
Publication statusPublished - 2016 Aug

Bibliographical note

Funding Information:
This work was partially supported by NRF (grant nos. 2011-0030161 and 2011-0030162). The FutureChem (Korea) is acknowledged for the synthesis of peptides and MALDITOF measurements.

Publisher Copyright:
© 2016, Mary Ann Liebert, Inc.

Copyright 2017 Elsevier B.V., All rights reserved.


  • Cu
  • RGD
  • U87MG
  • bifunctional chelator
  • glucosamine
  • integrin receptor

ASJC Scopus subject areas

  • Oncology
  • Radiology Nuclear Medicine and imaging
  • Pharmacology
  • Cancer Research


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