Drug Overcomes Protein Degrader Resistance
Research
Angewandte Chemie has published a study led by Dr. Cristina Mayor-Ruiz and Dr. Antoni Riera describing RBS-10, a small molecule that selectively kills cells resistant to targeted protein degraders by being bio-activated through the enzyme NQO1. Chemoproteomic profiling pinpointed NQO1 as the specific vulnerability in these resistant cells.
Because resistance remains a major obstacle to the clinical use of degrader compounds, pairing them with NQO1-activated agents such as RBS-10 offers a way to exploit that metabolic liability. In doing so, it may help sustain anti-tumor activity and broaden the range of proteins that can be effectively targeted.
More information: New drug reveals a key mechanism to overcome resistance to protein degraders
