Today for our weekend series, we want to highlight an article published only 2 weeks ago on the development of targeted covalent drugs. 

Before we start, we want to remind you about our great product – 40 Covalent Modifiers Sets, developed for each specific warhead.

This quite successful section of Medicinal Chemistry began its rapid development back in the 1990s with the disclosure of the first targeted covalent inhibitor. Even though the efforts of the scientists are super promising, this field still faces quite important challenges like the off-target toxicity of such compounds.  

Today’s review covers the concept of targeted covalent inhibition to diseases, discusses traditional and interdisciplinary strategies of cysteine-focused covalent drug discovery, and exhibits newly disclosed electrophilic warheads majorly targeting the cysteine residue. Of course, the authors also discuss the successful applications of covalent drugs.

You can find the full text of this great work here.