Montaño et al. generate an integrated proteomic and cysteine reactivity resource for the NCI-60 cancer cell line panel, offering quantitative data on over 12,000 proteins and 36,000 cysteines to enabl...

Isocyanides have been applied in bioorthogonal reactions as triggers for uncaging reactions. However, emerging evidence suggests that they may label proteins covalently. We synthesised a fluorophore-conjugated isocyanide and analysed its protein reactivity. Our results suggest that isocyanides cannot be considered

The enzyme PCMT1 was found to install a C-terminal cyclic imide modification on proteins that marks them for degradation by CRBN, uncovering a conserved protein turnover pathway with implications in m...

The proteomics pioneer notes that the field has made tremendous technological strides over the decades but its clinical impact remains muted.

Peptide drugs are a powerful modality in modern drug discovery. Synthetic methods that enable the late-stage diversification of native peptides through amino acid-specific modifications are thus in high demand. In this work, we demonstrate the epimerization-free, chemoselective late-stage diversification of tryptophan-containing native peptides through nitrogen atom insertion in solution. The direct application of this rapid and straightforward method to structurally complex peptide drugs underscores the broader potential of atom insertion reactions in drug discovery beyond small molecules.

vCATCH is a volumetric tissue labeling technique enabling cellular-resolution mapping of covalent drug targets throughout the entire mammalian body.