The emerging use of covalent ligands as chemical probes and drugs would benefit from an
expanded repertoire of cysteine-reactive electrophiles for efficient and diverse targeting of …

Traditional biochemical target-based and phenotypic cell-based screening approaches to
drug discovery have produced the current covalent and non-covalent pharmacopoeia …

Protein-reactive electrophiles are critical to chemical proteomic applications including
activity-based protein profiling, site-selective protein modification, and covalent inhibitor …

Drug candidates are generally discovered using biochemical screens employing an isolated
target protein or by utilizing cell-based phenotypic assays. Both noncovalent and covalent …

Resurgent interest in covalent target engagement in drug discovery has demonstrated that
small molecules containing weakly reactive electrophiles can be safe and effective …

Despite the known propensity of small-molecule electrophiles to react with numerous
cysteine-active proteins, biological actions of individual signal inducers have emerged to be …

This Perspective delineates how redox signaling affects the activity of specific enzyme
isoforms and how this property may be harnessed for rational drug design. Covalent drugs …

Revolutionary proteomic strategies have enabled rapid profiling of the cellular targets of
electrophilic small molecules. However, precise means to directly interrogate how these …

Targeted covalent inhibitors have emerged as a powerful approach in the drug discovery
pipeline. Key to this process is the identification of signaling pathways (or receptors) specific …

Vinyl sulfones and sulfonamides are valued for their use as electrophilic warheads in
covalent protein inhibitors. Conversely, the S (VI) aza-isosteres thereof, vinyl sulfoximines …