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

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• 作者：Jianbo Li^a ; ^b ; Lingli Shi^a ; ^b ; Lina Jia^a ; ^b ; Dawei Jiang^a ; ^b ; Wei Zhou^a ; Weiqing Hu^a ; Yujin Qi^a ; Lan Zhang^a ; ^{zhanglan@sinap.ac.cn}
• 关键词：Click reaction ; Fluorion-18 ; Radiolabeling ; RGD peptide ; Micro-PET imaging
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：2012
• 出版时间：15 June, 2012
• 年：2012
• 卷：20
• 期：12
• 页码：3850-3855
• 全文大小：482 K

文摘

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 ¡À 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 ¡À 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 ¦Á_v¦Â₃. This study provided useful information for peptide radiofluorination by using click chemistry.