Functional E3 ligase hotspots and resistance mechanisms to small-molecule degraders

Abstract excerpt

Targeted protein degradation is a novel pharmacology established by drugs that recruit target proteins to E3 ubiquitin ligases. Based on the structure of the degrader and the target, different E3 interfaces are critically involved, thus forming defined ‘functional hotspots’. Understanding disruptive mutations in functional hotspots informs on the architecture of the assembly, and highlights residues susceptible...

Topics

Share this publication in a Topic to start or enrich a Post.

• Share to Peptidase Inhibition and Analysis
• Share to Protein Degradation and Inhibitors
• Share to Ubiquitin and proteasome pathways