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通过 DNA 编程亲和标记,直接针对活细胞上的膜蛋白进行配体筛选。

Direct ligand screening against membrane proteins on live cells enabled by DNA-programmed affinity labelling.

机构信息

Department of Chemistry and State Key Laboratory of Synthetic Chemistry, The University of Hong Kong, Pokfulam Road, Hong Kong SAR, China, Laboratory for Synthetic Chemistry and Chemical Biology, Health@InnoHK, Innovation and Technology Commission, Hong Kong, SAR, China.

出版信息

Chem Commun (Camb). 2021 Apr 21;57(31):3769-3772. doi: 10.1039/d1cc00961c. Epub 2021 Mar 17.

DOI:10.1039/d1cc00961c
PMID:33730131
Abstract

Membrane proteins are important drug targets; however, ligand discovery for membrane proteins is highly challenging due to their hydrophobic nature. We show that membrane proteins may be specifically labelled with a DNA tag by DNA-programmed affinity labelling (DPAL), thereby enabling the screening of chemical compounds against membrane proteins directly on live cells.

摘要

膜蛋白是重要的药物靶点;然而,由于其疏水性,膜蛋白的配体发现极具挑战性。我们表明,膜蛋白可以通过 DNA 编程亲和标记 (DPAL) 进行特异性标记,从而可以直接在活细胞上针对膜蛋白筛选化学化合物。

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