激酶
光亲和标记
生物化学
计算生物学
酶
鉴定(生物学)
药物发现
生物
结合位点
化学
植物
作者
Dimitris Korovesis,Hester A. Beard,Christel Mérillat,Steven H. L. Verhelst
出处
期刊:ChemBioChem
[Wiley]
日期:2021-02-05
卷期号:22 (13): 2206-2218
被引量:7
标识
DOI:10.1002/cbic.202000874
摘要
Abstract Protein kinases, one of the largest enzyme superfamilies, regulate many physiological and pathological processes. They are drug targets for multiple human diseases, including various cancer types. Probes for the photoaffinity labelling of kinases are important research tools for the study of members of this enzyme superfamily. In this review, we discuss the design principles of these probes, which are mainly derived from inhibitors targeting the ATP pocket. Overall, insights from crystal structures guide the placement of photoreactive groups and detection tags. This has resulted in a wide variety of probes, of which we provide a comprehensive overview. We also discuss several areas of application of these probes, including the identification of targets and off‐targets of kinase inhibitors, mapping of their binding sites, the development of inhibitor screening assays, the imaging of kinases, and identification of protein binding partners.
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