Abstract. Approved inhibitors of KRASG12C prevent oncogenic activation by sequestering the inactive, GDP-bound (OFF) form rather than directly binding and inhibiting the active, GTP-bound (ON) form. T...

Oncogene - Discovery of a molecular glue for EGFR degradation

Jochem et al. present DegMS, a proteomic approach to selectively investigate protein degradation that combines stable isotope-labeling, click-chemistry, and mass spectrometry. Resilience to compensato...

Small molecules promoting protein–protein interactions produce a range of therapeutic outcomes. Molecular glue degraders exemplify this concept due to their compact drug-like structures and ability to...

Curated daily chemistry problems. Six attempts to solve the questions, on topics from named reactions to total synthesis.

Molecular glue degraders (MGDs) are small molecules that harness the ubiquitin-proteasome system to induce degradation of target proteins lacking conventional druggable pockets. Given the challenges i...

Development of a targeted protein degradation platform, methylarginine targeting chimera (MrTAC), enables arginine methylation-driven degradation of intracellular proteins in lysosomes.