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Construction of ligand assay systems by protein-based semisynthetic biosensors.
Current Opinion in Chemical Biology ( IF 7.8 ) Pub Date : 2019-03-12 , DOI: 10.1016/j.cbpa.2019.02.011
Seiji Sakamoto 1 , Shigeki Kiyonaka 1 , Itaru Hamachi 1
Affiliation  

Proteins as causative agents of diseases such as cancers, diabetes and neurological disorders are attractive drug targets. For developing chemicals selectively acting on key disease-causing proteins, one useful concept is the direct conversion of such target proteins into biosensors. This approach provides ligand-binding assay systems based on protein-based biosensors, which can quantitatively evaluate interactions between the protein and a specific ligand in many environments. Site-specific chemical modifications are used widely for the creation of protein-based semisynthetic biosensors in vitro. Notably, a few bio-orthogonal approaches capable of selectively modifying drug-targets have been developed, allowing conversion of specific target proteins into semisynthetic biosensors in live cells. These biosensors can be used for quantitative drug binding analyses in native environments. In this review, we discuss recent efforts for the construction of ligand assay systems using semisynthetic protein-based biosensors and their application to quantitative analysis and high-throughput screening of small molecules for drug discovery.

中文翻译:

通过基于蛋白质的半合成生物传感器构建配体测定系统。

蛋白质是诸如癌症,糖尿病和神经系统疾病等疾病的病原体,是有吸引力的药物靶标。为了开发选择性作用于关键致病蛋白质的化学物质,一个有用的概念是将此类目标蛋白质直接转化为生物传感器。这种方法提供了基于蛋白质的生物传感器的配体结合测定系统,可以在许多环境中定量评估蛋白质与特定配体之间的相互作用。特定于位点的化学修饰已广泛用于体外创建基于蛋白质的半合成生物传感器。值得注意的是,已经开发了一些能够选择性修饰药物靶标的生物正交方法,从而可以将特定的靶蛋白转化为活细胞中的半合成生物传感器。这些生物传感器可用于天然环境中的定量药物结合分析。在这篇综述中,我们讨论了使用基于半合成蛋白质的生物传感器构建配体测定系统的最新工作,以及它们在定量分析和小分子药物高通量筛选中的应用。
更新日期:2019-11-01
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