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Updated: Jun 17, 2026
Preparing a 68Ga-labeled Arginine Glycine Aspartate (RGD)-peptide for Angiogenesis
Published on: January 7, 2019
Radiolabeling RGD peptide and preliminary biodistribution evaluation in mice bearing S180 tumors
Yufei Ma1, Junfeng Yu, Yanjiang Han
1Shanghai Institute of Applied Physics (SINAP), Chinese Academy of Sciences, PR China.
Objective:
To prepare the rhenium-188 (188Re)-arginine-glycine-aspartic acid (RGD) peptide in a convenient manner and to evaluate its potential as an agent for alphavbeta3 integrin receptor-positive tumors.
Methods:
Radiolabeled RGD was obtained by conjugating the His group at the end of peptide with fac-[188Re(H2O)3(CO)3]+. Chelating efficiency of fac-[188Re(H2O)3(CO)3]+ and radiolabeling efficiency of radiolabeled peptide were measured by thin-layer chromatography and high-performance liquid chromatography. In-vitro stability of the radio-complex was determined in phosphate-buffered saline (0.05 mol/l, pH 7.4), new-born calf serum, His or Cys solution at 37 degrees C or room temperature and analyzed by thin-layer chromatography. A biodistribution study was carried out in mice bearing S180 tumors.
Results:
188Re-RGD was obtained with a more than 95% of radiolabeling efficiency, and showed high stability in phosphate-buffered saline, new-born calf serum, His and Cys solution. Furthermore, this radio-complex was cleared rapidly from the blood and showed specific tumor uptake in mice bearing S180 tumors.
Conclusion:
188Re-RGD was prepared by a simple method. Preliminary biodistribution results showed its potential as an agent for cancer therapy and encouraged further investigation.
