Unlocking Undruggable Chromatin Regulators to Advance First-in-Class PROTACs Through Preclinical Discovery & Optimisation
- Identifying ligands for a chromatin regulatory protein with limited prior tractability and validating functional degrader activity
- Optimising degrader architecture through iterative design to enhance potency, selectivity and degradation efficiency
- Outlining challenges and solutions in progressing an advanced preclinical degrader toward development candidate nomination