Proteins are multifunctional large organic compounds that constitute an essential
component of a living system. Hence, control over their bioconjugation impacts science at …

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 …

Advances in chemoproteomic technology have revealed covalent interactions between
small molecules and protein nucleophiles, primarily cysteine, on a proteome-wide scale …

K-Ras is the most commonly mutated oncogene in human cancer. The recently approved
non-small cell lung cancer drugs sotorasib and adagrasib covalently capture an acquired …

Binding via reversible covalent bond formation presents a novel and powerful mechanism to
enhance the potency of synthetic inhibitors for therapeutically important proteins. Work on …

Peptide-based covalent probes can target shallow protein surfaces not typically addressable
using small molecules, yet there is a need for versatile approaches to convert native peptide …

Electrophilic small molecules that can reversibly modify proteins are of growing interest in
drug discovery. However, the ability to study reversible covalent probes in live cells can be …

Molecules that stabilize protein–protein interactions (PPIs) are invaluable as tool
compounds for biophysics and (structural) biology, and as starting points for molecular glue …

The covalent inhibition of a target protein has gained widespread attention in the field of
drug discovery. Most of the current covalent drugs utilize the high reactivity of cysteines …

Lysine-targeting irreversible covalent inhibitors have attracted growing interests in recent
years, especially in the fields of kinase research. Despite encouraging progress, few …