(1238-C) Biophysical and Biochemical Evaluation of WD-Repeat-Containing Protein 5 (WDR5) Degraders

Abstract: The dysregulation of WDR5 expression and function has been implicated in the development of cancer, particularly through its interaction with the MYC oncogene. Here we detail the biophysical, biochemical, and structural evaluation of five WDR5 degraders via the recruitment of VHL. We assess binary and ternary binding affinities and discuss this data in the context of in vivo degradation efficiency.