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Targeted Protein Degradation in Drug Discovery
Substoichiometric E3 ligase recruitment
Structure and biophysical approaches
Dissociation kinetics correlate with initial rate of degradation
Advantages of Targeted Protein Degradation
Bump-Hole Strategy
RNA-seq analysis
Evaluation in vivo
Q&A session
Closing Remarks
Introduction
Theoretical Advantages of Targeted Protein Degradation
Degraders Are Agnostic to the Liggins Mode of Action
Paradoxical Ref Activation
Seven Is Tissue Selectivity Based on E3 Ligase Expression
Degraders Can Lead to Bystander Degradation of Alternative Targets
Areas To Watch in the Future
Why Do You Think Protein Degraders Are Mainly Applied to Oncology
Can Protein Degraders Be Used for Targeting Proteins from Pathogens
Do You Think the Degraders That Target the Oncogenes or Driver Genes Such as Egfr or Btk Have More Chance of Success