Assay Development Towards the Optimization of Effective Degraders

Time: 4:00 pm
day: Day One


• Targeted protein degradation (TPD) is an emerging novel therapeutic modality with the potential to tackle traditionally difficult to target (undruggable) disease-causing proteins
• Highly efficacious degraders (PROTAC) induce rapid and selective degradation of the POI with high potency (DC50) and high maximal degradation (Dmax). To optimize such parameters a sensitive bioluminescence protein quantitation system for the POI was established using Promega’s Nano-Glo HiBiT Detection System
• Further analysis revealed differential degradation of isoforms and the need for further development of cellular degradation assay approaches to fully understand these difference