In-cell click labelling of small molecules to determine subcellular localisation

Journal of Chemical Biology

Emily J. S. Graham²  Paul Targett-Adams²  Florian Wakenhut²  Peter Dodd¹  Owen Everson¹  Jared Millbank²  Matthew D. Selby¹  Thien-Duc Tran²  George M. Burslem¹  David Beal¹  Lyn H. Jones¹ 

[1] Chemical Biology Group, Sandwich Chemistry, Pfizer, Ramsgate Road, Sandwich, Kent CT13 9NJ UK;New Opportunities Unit, Pfizer, Ramsgate Road, Sandwich, Kent CT13 9NJ UK

关键词: Hepatitis C virus;    Click chemistry;    Labelling;    Small molecules;   

DOI  :  10.1007/s12154-010-0047-1

学科分类：分子生物学，细胞生物学和基因

来源: Springer

【 摘 要 】

Small molecule fluorometric boron dipyrromethene probes were developed to bind hepatitis C virus-encoded NS5A protein and aid subcellular distribution studies. These molecules did not co-locate with NS5A, therefore alternative ‘silent’ azide reporters were used to obtain a more relevant picture of their distribution. Following pre-incubation with replicon cells, click chemistry was used to append a fluorophore to the azide that confirmed the co-localisation of the small molecule with the NS5A protein, thus providing greater insight into the antiviral mode of action of this chemotype.

【 授权许可】

Unknown