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

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	Radiolabeling of RGD peptide and preliminary biological evaluation in mice bearing U87MG tumors
	Li, JB(李建波); Shi, LL; Jia, LN(贾丽娜); Jiang, DW(江大卫); Zhou, W(周伟); Hu, WQ(胡伟清); Qi, YJ(漆玉金); Zhang, L(张岚)
	2012
Source Publication	BIOORGANIC & MEDICINAL CHEMISTRY
ISSN	0968-0896
Volume	20 Issue:12
Abstract	2-[F-18]Fluoroethyl azide ([F-18]FEA) and terminal alkynyl modified propioloyl RGDfK were selected in this study. [F-18]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 [F-18]FEA and propioloyl RGDfK, which included peptide concentration, reaction time, temperature and catalyst dosage. The F-18-labeled-RGD peptide ([F-18]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. [F-18]F-RGDfK showed high stability in phosphate buffered saline and new-born calf serum. Micro-PET imaging at 1 h post injection of [F-18]F-RGDfK showed medium concentration of radioactivity in tumors while much decreased concentration in tumors in the blocking group. These results showed that [F-18]F-RGDfK obtained by click chemistry maintained the affinity and specificity of the RGDfK peptide to integrin alpha(v)beta(3). This study provided useful information for peptide radiofluorination by using click chemistry. (C) 2012 Elsevier Ltd. All rights reserved.
Language	英语
Funding Project	应物所项目组
WOS ID	WOS:000304486500019
Citation statistics	Cited Times:10[WOS] [WOS Record] [Related Records in WOS]
Document Type	期刊论文
Identifier	http://ir.sinap.ac.cn/handle/331007/13275
Collection	中科院上海应用物理研究所2011-2019年
Recommended Citation GB/T 7714	Li, JB,Shi, LL,Jia, LN,et al. Radiolabeling of RGD peptide and preliminary biological evaluation in mice bearing U87MG tumors[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2012,20(12).
APA	Li, JB.,Shi, LL.,Jia, LN.,Jiang, DW.,Zhou, W.,...&Zhang, L.(2012).Radiolabeling of RGD peptide and preliminary biological evaluation in mice bearing U87MG tumors.BIOORGANIC & MEDICINAL CHEMISTRY,20(12).
MLA	Li, JB,et al."Radiolabeling of RGD peptide and preliminary biological evaluation in mice bearing U87MG tumors".BIOORGANIC & MEDICINAL CHEMISTRY 20.12(2012).

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