Assay Development and Screening
Biochemical & Biophysical Assays
Targeted protein degradation, through the use of heterobifunctional degraders that act as catalytic activators for an E3 ligase and target protein, has the potential to transform drug discovery. This talk will discuss the key structure:activity relationships that underpin degrader optimization, including the interpretation and interplay of both thermodynamic and kinetic elements that drive the catalytic turnover of targeted proteins. These data will be placed in context with an enzymology framework to characterize cellular degradation data the extension of these insights to pharmacodynamic modeling and predictions.