Targeting A Non-Traditional Residue to Reprogram E3 Ligase Function & Degradation Profiles

  • Targeting a non-traditional nucleophilic residues such as histidine to expand the scope of covalent drug discovery beyond cysteine-centric approaches
  • Inducing covalent-driven conformational changes that remodel E3 ligase surfaces and enable recruitment of entirely new substrate
  • Reprogramming degradation profiles by engagement of a non-classical degron