Structure and Dynamics of CRLomes: Implications for Targeted Protein Degradation

Time: 3:30 pm
day: Day Two


• Some of the most commonly used ligands for assembling PROTACs work through cullin-RING ubiquitin ligases (CRLs)
• Active CRLs are composed of a core catalytic unit (cullin+RING domain protein+adaptor protein) assembled with one member
of a large family of different substrate receptors that in aggregate are present in excess over the core catalytic unit
• Assembly of different receptors with the core catalytic unit is regulated by a reversible cycle of Nedd8 conjugation/
deconjugation of the cullin and the substrate receptor exchange factors Cand1 and Cand2
• Discussing the architecture and dynamics of the network of CRL4 enzymes