Utilizing PROTACs to Degrade Kinases with Increased Selectivity, Improved Efficacy or PK/PD Disconnect Using Multiple Examples

Time: 1:30 pm
day: Day One


  • Highlighting the advantages of using a degrader vs. catalytic site inhibitors and determining high specificity to minimize off-target effects
  • Optimizing the linkers and E3 ligand for maximal binding, optimize residency time and improving the durability of kinase inhibitor therapeutics
  • Discovering and characterizing a highly cooperative FAK-GSK215-VHL ternary complex