A two-step strategy to radiolabel choline phospholipids with Tc-99m in   S180 cell membranes via strain-promoted cyclooctyne-azide cycloaddition   reaction

doi:10.1016/j.bmcl.2016.10.026

CORC > 北京大学 > 化学与分子工程学院

	A two-step strategy to radiolabel choline phospholipids with Tc-99m in S180 cell membranes via strain-promoted cyclooctyne-azide cycloaddition reaction
	Chen, Qingxin ; Chu, Taiwei
刊名	BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
	2016
关键词	Tumor imaging AECho ADIBO-BPA Tc-99m(CO)(3)-labeling Pretargeting SPAAC FREE CLICK CHEMISTRY POSITRON-EMISSION-TOMOGRAPHY IN-VIVO METABOLIC INCORPORATION ENVELOPED VIRUS HOST-CELLS LIVE MICE CANCER ANTIBODY RADIOIMMUNOTHERAPY
DOI	10.1016/j.bmcl.2016.10.026
英文摘要	As tumor markers, the radiolabeling of choline (Cho)-containing phospholipids in cellular membranes with Tc-99m is a challenge. The conventional strategy to combine the metallic radionuclide with Cho by large ligand damages the bioactivity of Cho, resulting in low tumor-to-nontumor ratios. Pretargeting strategy based on strain-promoted cyclooctyne-azide cycloaddition (SPAAC) reaction was applied to solve this general problem. Functional click synthons were synthesized as pretargeting components: azidoethyl-choline (AECho) serves as tumor marker and azadibenzocyclooctyne (ADIBO) conjugated to bis(2-pieolyl) amine (BPA) ligand (ADIBO-BPA) as Tc-99m(CO)(3)-labeling and azido-binding group. Both in vitro cell experiment and in vivo biodistribution experiment indicate that it is versatile to radiolabel Cho in cellular membranes via this two-step pretargeting strategy. We believe that this pretargeting strategy can indeed enhance the target-specificity and also reduce background signals to optimize imaging quality. (C) 2016 Elsevier Ltd. All rights reserved.; National Natural Science Foundation of China [21371017, 81371592]; SCI(E); PubMed; ARTICLE; twchu@pku.edu.cn; 22; 5472-5475; 26
语种	英语
内容类型	期刊论文
源URL	[http://ir.pku.edu.cn/handle/20.500.11897/457286]
专题	化学与分子工程学院
推荐引用方式 GB/T 7714	Chen, Qingxin,Chu, Taiwei. A two-step strategy to radiolabel choline phospholipids with Tc-99m in S180 cell membranes via strain-promoted cyclooctyne-azide cycloaddition reaction[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2016.
APA	Chen, Qingxin,&Chu, Taiwei.(2016).A two-step strategy to radiolabel choline phospholipids with Tc-99m in S180 cell membranes via strain-promoted cyclooctyne-azide cycloaddition reaction.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS.
MLA	Chen, Qingxin,et al."A two-step strategy to radiolabel choline phospholipids with Tc-99m in S180 cell membranes via strain-promoted cyclooctyne-azide cycloaddition reaction".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2016).