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

Abstract：

:2-[(18)F]Fluoroethyl azide ([(18)F]FEA) and terminal alkynyl modified propioloyl RGDfK were selected in this study. [(18)F]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 [(18)F]FEA and propioloyl RGDfK, which included peptide concentration, reaction time, temperature and catalyst dosage. The (18)F-labeled-RGD peptide ([(18)F]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. [(18)F]F-RGDfK showed high stability in phosphate buffered saline and new-born calf serum. Micro-PET imaging at 1 h post injection of [(18)F]F-RGDfK showed medium concentration of radioactivity in tumors while much decreased concentration in tumors in the blocking group. These results showed that [(18)F]F-RGDfK obtained by click chemistry maintained the affinity and specificity of the RGDfK peptide to integrin α(v)β(3). This study provided useful information for peptide radiofluorination by using click chemistry.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Li J,Shi L,Jia L,Jiang D,Zhou W,Hu W,Qi Y,Zhang L

doi

10.1016/j.bmc.2012.04.037

subject

Has Abstract

pub_date

2012-06-15 00:00:00

pages

3850-5

issue

12

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(12)00321-5

journal_volume

20

pub_type

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