Over the past decade, covalent kinase inhibitors (CKI) have seen a resurgence in drug
discovery. Covalency affords a unique set of advantages as well as challenges relative to …

Cysteine is one of the least abundant amino acids in proteins of many organisms, which
plays a crucial role in catalysis, signal transduction, and redox regulation of gene …

The stabilization of protein–protein interactions (PPIs) has emerged as a promising strategy
in chemical biology and drug discovery. The identification of suitable starting points for …

Introduction Covalent drugs have been used for more than hundred years, but gathered
larger interest in the last two decades. There are currently over a 100 different electrophilic …

Highlights•Overview on available covalent warheads.•Design principles of covalent
fragment libraries.•Surrogate assay methodologies for testing reactivity.•Covalent screening …

The transcription factor TEAD, together with its coactivator YAP/TAZ, is a key transcriptional
modulator of the Hippo pathway. Activation of TEAD transcription by YAP has been …

Electrophilic biocompatible warheads, particularly cysteine-reactive acrylamides, have
enabled the development of covalent inhibitor drugs and chemical biology probes, but …

Abstract SARS-CoV-2 3CL protease is one of the key targets for drug development against
COVID-19. Most known SARS-CoV-2 3CL protease inhibitors act by covalently binding to …

Fragment based drug discovery has long been used for the identification of new ligands and
interest in targeted covalent inhibitors has continued to grow in recent years, with high …

Covalent inhibitors and other types of covalent modalities have seen a revival in the past two
decades, with a variety of new targeted covalent drugs having been approved in recent …