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Click-Addressable Cassette for Photoaffinity Labeling.
ACS Medicinal Chemistry Letters ( IF 3.5 ) Pub Date : 2018-01-24 , DOI: 10.1021/acsmedchemlett.7b00516
Bosheng Zhao 1 , Kevin Burgess 1
Affiliation  

A small molecule 1 was designed to contain an alkyne, a trifluoromethyl phenyldiazirine, and a free piperidine-NH for facile conjugation to protein binding ligands. This "cassette" 1 was synthesized via a relatively direct route involving only routine steps. In this proof-of-concept study, putative ligands for carbonic anhydrase IX and for TrkC were conjugated to 1. Photoaffinity labeling was performed using purified extracellular regions of both these protein-receptors, and using cells that express these receptors (isolation via a pull-down procedure), labeling of the protein was observed in all four experiments.

中文翻译:

用于光亲和性标签的可点击寻址的盒式磁带。

设计小分子1包含炔烃,三氟甲基苯基重氮和自由哌啶-NH,以便于与蛋白质结合配体结合。该“盒式磁带” 1是通过仅涉及常规步骤的相对直接的路线合成的。在此概念验证研究中,将碳酸酐酶IX和TrkC的假定配体与1偶联。使用这两种蛋白受体的纯化细胞外区域以及表达这些受体的细胞(通过拉动分离)进行光亲和标记。 -down程序),在所有四个实验中都观察到了蛋白质的标记。
更新日期:2018-01-30
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