The term “undruggable” refers to proteins or other biological targets that have been
historically challenging to target with conventional drugs or therapeutic strategies because …

Genomic technologies have led to massive gains in our understanding of human gene
function and disease relevance. Chemical biologists are a primary beneficiary of this …

Caspases are a highly conserved family of cysteine-aspartyl proteases known for their
essential roles in regulating apoptosis, inflammation, cell differentiation, and proliferation …

β-catenin (CTNNB1) is an oncogenic transcription factor that is important in cell–cell
adhesion and transcription of cell proliferation and survival genes that drive the …

Molecules that are able to induce proximity between two proteins are finding ever increasing
applications in chemical biology and drug discovery. The ability to introduce an electrophile …

Cysteine chemoproteomic screening platforms are widely utilized for chemical probe and
drug discovery campaigns. Chemoproteomic compound screens, which use a mass …

Core regulatory circuitry refers to the network of lineage-specific transcription factors
regulating expression of both their own coding genes, and that of other transcription factors …

We describe exciting recent advances in fusion-driven sarcoma etiology, from an
epigenetics perspective. By exploring the current state of the field, we identify and describe …

Cysteine residues play key roles in protein structure and function and can serve as targets
for chemical probes and even drugs. Chemoproteomic studies have revealed that …

In this issue, Won et al. 1 report a covalent ligand binding the pioneer transcription factor
FOXA1, altering its function and remodeling chromatin. This important finding highlights the …