用于确定亚细胞定位的小分子细胞内点击标记
In-cell click labelling of small molecules to determine subcellular localisation.
作者信息
Jones Lyn H, Beal David, Selby Matthew D, Everson Owen, Burslem George M, Dodd Peter, Millbank Jared, Tran Thien-Duc, Wakenhut Florian, Graham Emily J S, Targett-Adams Paul
出版信息
J Chem Biol. 2011 Apr;4(2):49-53. doi: 10.1007/s12154-010-0047-1. Epub 2010 Nov 18.
Abstract
UNLABELLED
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.
ELECTRONIC SUPPLEMENTARY MATERIAL
The online version of this article (doi:10.1007/s12154-010-0047-1) contains supplementary material, which is available to authorized users.
摘要
未标记
开发了小分子荧光硼二吡咯亚甲基探针，用于结合丙型肝炎病毒编码的NS5A蛋白并辅助亚细胞分布研究。这些分子并未与NS5A共定位，因此使用了替代性的“沉默”叠氮化物报告基团来更准确地了解它们的分布情况。在用复制子细胞进行预孵育后，利用点击化学将荧光团连接到叠氮化物上，证实了小分子与NS5A蛋白的共定位，从而更深入地了解了这种化学类型的抗病毒作用模式。
电子补充材料
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3
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