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

Huang, Yiran; Deng, Yuqing; Zhang, Jianfu; Meng, Ling; Li, Xiaoyu

Huang, Yiran; Deng, Yuqing; Zhang, Jianfu; Meng, Ling; Li, Xiaoyu.

Afiliação

Huang Y; 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. xiaoyuli@hku.hk.

Chem Commun (Camb) ; 57(31): 3769-3772, 2021 Apr 21.

Article em En | MEDLINE | ID: mdl-33730131

ABSTRACT

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.

Assuntos

Marcadores de Afinidade/química; DNA/análise; Proteínas de Membrana/antagonistas & inibidores; Bibliotecas de Moléculas Pequenas/farmacologia; Células HeLa; Humanos; Interações Hidrofóbicas e Hidrofílicas; Ligantes; Estrutura Molecular; Bibliotecas de Moléculas Pequenas/química

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Texto completo: 1 Base de dados: MEDLINE Assunto principal: DNA / Marcadores de Afinidade / Bibliotecas de Moléculas Pequenas / Proteínas de Membrana Idioma: En Ano de publicação: 2021 Tipo de documento: Article

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