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MDM2-PROTAC versus MDM2 Inhibitors: Beyond p53 Reactivation

Sylvain Peuget1, Galina Selivanova1

  • 1Department of Microbiology, Tumor and Cell Biology, Karolinska Institutet, Stockholm, Sweden.

Cancer Discovery
|May 4, 2023
PubMed
Abstract

Insights

Researchers discovered a potent PROTAC drug that degrades MDM2, activating p53 and causing cancer cell death. This PROTAC effectively kills cancer cells with mutated or absent p53, offering a new therapeutic strategy.

Area of Science:

  • Oncology
  • Molecular Biology
  • Drug Discovery

Background:

  • The p53 tumor suppressor is frequently inactivated in cancer.
  • MDM2 is an E3 ubiquitin ligase that targets p53 for degradation.
  • Targeting MDM2 offers a potential strategy to restore p53 function.

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