PROTAC degraders with ligands recruiting MDM2 E3 ubiquitin ligase: an updated perspective

Abstract excerpt

Mouse double minute 2 (MDM2) is an oncogenic E3 ligase that effectively degrades the tumor suppressor p53. In the past two decades, many MDM2 inhibitors that disrupt MDM2-p53 binding have been discovered and developed. Given that MDM2 and p53 form an auto-regulatory loop, in which p53 undergoes targeted degradation as a substrate of MDM2, and p53 targets MDM2 for transcriptional upregulation, these MDM2...

Topics

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

• Share to Multiple Myeloma Research and Treatments
• Share to Protein Degradation and Inhibitors
• Share to Ubiquitin and proteasome pathways