Covalent binders in drug discovery.

Authors :: Vasudevan A
Argiriadi MA
Baranczak A
Friedman MM
Gavrilyuk J
Hobson AD
Hulce JJ
Osman S
Wilson NS
Source :: Progress in medicinal chemistry [Prog Med Chem] 2019; Vol. 58, pp. 1-62. Date of Electronic Publication: 2019 Mar 11.
Publication Year :: 2019
Abstract: Covalent modulation of protein function can have multiple utilities including therapeutics, and probes to interrogate biology. While this field is still viewed with scepticism due to the potential for (idiosyncratic) toxicities, significant strides have been made in terms of understanding how to tune electrophilicity to selectively target specific residues. Progress has also been made in harnessing the potential of covalent binders to uncover novel biology and to provide an enhanced utility as payloads for Antibody Drug Conjugates. This perspective covers the tenets and applications of covalent binders.<br /> (© 2019 Elsevier B.V. All rights reserved.)