Title

Radiolabeling of RGD peptide and preliminary biological evaluation in mice bearing U87MG tumors

RIS ID

78199

Publication Details

Li, J., Shi, L., Jia, L., Jiang, D., Zhou, W., Hu, W., Qi, Y. & Zhang, L. (2012). Radiolabeling of RGD peptide and preliminary biological evaluation in mice bearing U87MG tumors. Bioorganic & Medicinal Chemistry, 21 (12), 3850-3855.

Abstract

2-[18F]Fluoroethyl azide ([18F]FEA) and terminal alkynyl modified propioloyl RGDfK were selected in this study. [18F]FEA was prepared by nucleophilic radiofluorination of 2-azidoethyl 4-toluenesulfonate with radiochemical yield of 71 ± 4% (n = 5, decay-corrected). We assessed the various conditions of the CuAAC reaction between [18F]FEA and propioloyl RGDfK, which included peptide concentration, reaction time, temperature and catalyst dosage. The 18F-labeled-RGD peptide ([18F]F-RGDfK) could be obtained in 60 min by a two-step radiochemical synthesis route, with total radiochemical yield of 60 ± 2% (n = 3, decay-corrected) through click chemistry. [18F]F-RGDfK showed high stability in phosphate buffered saline and new-born calf serum. Micro-PET imaging at 1 h post injection of [18F]F-RGDfK showed medium concentration of radioactivity in tumors while much decreased concentration in tumors in the blocking group. These results showed that [18F]F-RGDfK obtained by click chemistry maintained the affinity and specificity of the RGDfK peptide to integrin avb3. This study provided useful information for peptide radiofluorination by using click chemistry.

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Link to publisher version (DOI)

http://dx.doi.org/10.1016/j.bmc.2012.04.037