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Recent advances in the development of covalent inhibitors

Hyunsoo Kim, Yoon Soo Hwang, Mingi Kim, Seung Bum Park

2021RSC Medicinal Chemistry101 citationsDOIOpen Access PDF

Abstract

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.

Topics & Concepts

Covalent bondDrug developmentCovalent bindingChemistryDrug discoveryNanotechnologyPharmacologyDrugMaterials scienceBiochemistryMedicineOrganic chemistryClick Chemistry and ApplicationsSynthesis and Biological EvaluationChemical Synthesis and Analysis
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