Radiolabeling RGD peptide and preliminary biodistribution evaluation in mice bearing S180 tumors.

Abstract:

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.

journal_name

Nucl Med Commun

authors

Ma Y,Yu J,Han Y,Shen H,Li Z,Zhou W,Yin D

doi

10.1097/MNM.0b013e3283334e48

subject

Has Abstract

pub_date

2010-02-01 00:00:00

pages

147-51

issue

2

eissn

0143-3636

issn

1473-5628

journal_volume

31

pub_type

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