Amide-to-Ester Substitution as a Strategy for Optimising PROTAC Permeability & Cellular Activity

Time: 11:30 am
day: Day 2 AM - Stream B


*Remote Presentation* 

  • Bifunctional PROTAC degraders belong to “beyond Rule of 5” chemical space, and criteria for predicting their drug-like properties are underdeveloped
  • A simple, yet unconventional, amide-to-ester substitution in BET degraders leads to increased cellular activity
  • Increases in PROTAC activity is due to increases in cellular permeability and not due to enhancement of ternary complex formation