A Strategy to Assess the Cellular Activity of E3 Ligase Components against Neo-Substrates Using Electrophilic Probes
Time: 12:40 pm
day: Day 1 AM - Stream A
Details:
- COFFEE (Covalent Functionalization Followed by E3 Electroporation) tests neo-substrate degradation by chemically modified E3 ligase components
- Recombinant E3s are labelled with maleimide functionalized neo-substrate ligands, and then electroporated into cells
- Proof-of-concept degradation by electroporated JQ1- or dasatinib-labeled VHL. Discovery that SPSB2 and SKP1 can be redirected to degrade tyrosine kinases
