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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
Summary
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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