Today George is here with a very hot article on covalent drugs!
Covalent drugs have been used to treat diseases for more than a century, but tools that facilitate the rational design of covalent drugs have emerged more recently. The purposeful addition of reactive functional groups to existing ligands can enable potent and selective inhibition of target proteins, as demonstrated by the covalent epidermal growth factor receptor (EGFR) and Bruton’s tyrosine kinase (BTK) inhibitors used to treat various cancers.
The authors talk about evolving toolbox of covalent Drug Discovery techniques facilitates success in this field. The full text is available here!
We also want to remind you about our Covalent Modifiers Sets! It is a collection of 40 compound sets comprised of molecules that have a covalent warhead. They are divided into sets by the type of functional group for your convenience.
The sets are available here!