Kim Hyunsoo, Hwang Yoon Soo, Kim Mingi, Park Seung Bum
CRI Center for Chemical Proteomics, Department of Chemistry, Seoul National University Seoul 08826 Korea
Department of Biophysics and Chemical Biology, Seoul National University Seoul 08826 Korea.
RSC Med Chem. 2021 May 4;12(7):1037-1045. doi: 10.1039/d1md00068c. eCollection 2021 Jul 21.
The use of covalent inhibitors in the field of drug discovery has attracted considerable attention in the 2000s. As a result, more than 50 covalent drugs are currently on the market, and numerous covalent drug candidates are now under development. Therefore, interest in covalent drugs is expected to continue in the future. The purpose of this focused review is to provide an understanding of the development of covalent inhibitors by describing their inherent characteristics, possibilities, and limitations based on their mechanistic differences from noncovalent inhibitors. We also introduce the latest covalent warheads that can be applied to the development of potential covalent inhibitors.
在药物研发领域，共价抑制剂的应用在21世纪引起了广泛关注。因此，目前有50多种共价药物已上市，众多共价候选药物正在研发中。所以，预计未来对共价药物的兴趣仍将持续。本重点综述的目的是通过描述共价抑制剂与非共价抑制剂在作用机制上的差异，来阐述其内在特性、可能性和局限性，从而使读者了解共价抑制剂的发展情况。我们还介绍了可应用于潜在共价抑制剂研发的最新共价弹头。
