A great read for this weekend – a fresh featured article by George! 

Today we are going to cover a hot topic – the development of covalent chemical probes for protein kinases.

Don’t forget that Chemspace has a great collection of Covalent Modifiers. This set contains screening compounds that possess a covalent warhead and is divided into lysine- and cysteine-targeted modifiers. 

But why are these compounds so important? In addition to prolonging pharmacological effects beyond the clearance of a drug, covalent targeting offers benefits such as superior potency, increased selectivity, and limited competitivity with natural substrates and co-factors.  

This potential is widely used for the design of chemical probes – crucial tools to study the function of unexplored proteins in biological systems. One of the applications of such probes is targeting protein kinases, which is a very fruitful strategy for exploring the human kinome. 

The article we want to feature today showcases the properties and generations of covalent kinase inhibitors, specifically the ones targeting cysteine and lysine residues in an irreversible or reversible-covalent manner.*

*doi.org/10.1016/j.crchbi.2022.100040