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一种用于癌细胞成像的新型上皮细胞黏附分子(EpCAM)适配体-荧光共轭物的应变促进炔-叠氮环加成(SPAAC)反应。

A strain-promoted alkyne-azide cycloaddition (SPAAC) reaction of a novel EpCAM aptamer-fluorescent conjugate for imaging of cancer cells.

作者信息

Subramanian Nithya, Sreemanthula Jagadeesh Babu, Balaji Baghavathi, Kanwar Jagat R, Biswas Jyotirmay, Krishnakumar Subramanian

机构信息

Department of Nanobiotechnology, Kamalnayan Bajaj Research Institute, Vision Research Foundation, Chennai, India.

出版信息

Chem Commun (Camb). 2014 Oct 14;50(80):11810-3. doi: 10.1039/c4cc02996h.

Abstract

For the first time, a novel EpCAM aptamer (SYL3C)-DIBO-AF594 fluorescent conjugate was synthesised by bioorthogonal chemistry utilizing a strain promoted alkyne-azide cycloaddition (copper free click) reaction (SPAAC). The ligation efficiency of SPAAC was improved by freeze-thaw cycles. The obtained conjugate showed target specific binding and aided in the imaging of various EpCAM positive cancer cell lines like MCF7, MDAMB453, Weri-RB1 and PC3.

摘要

首次通过利用应变促进的炔-叠氮环加成(无铜点击)反应(SPAAC)的生物正交化学合成了一种新型的上皮细胞粘附分子(EpCAM)适配体(SYL3C)-二苯并环辛炔(DIBO)-AF594荧光共轭物。通过冻融循环提高了SPAAC的连接效率。所获得的共轭物表现出靶向特异性结合,并有助于对多种EpCAM阳性癌细胞系(如MCF7、MDAMB453、Weri-RB1和PC3)进行成像。

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