Friday, October 14, 2022

Recent advances in the development of covalent inhibitors

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

RSC Med. Chem., 2021, 12, 1037-1045

https://doi.org/10.1039/D1MD00068C

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.

Discovery of a Tunable Heterocyclic Electrophile 4-Chloro-pyrazolopyridine That Defines a Unique Subset of Ligandable Cysteines

Hong-Rae Kim, David P. Byun, Kalyani Thakur, Jennifer Ritchie, Yixin Xie, Ronald Holewinski, Kiall F. Suazo, Mckayla Stevens, Hope Liechty, ...