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Transforming targeted cancer therapy with PROTACs: A forward-looking perspective
William Farnaby1, Manfred Koegl2, Darryl B McConnell2
1Division of Biological Chemistry and Drug Discovery, School of Life Sciences, University of Dundee, UK.
Current Opinion in Pharmacology
|April 2, 2021
Summary
Proteolysis Targeting Chimeras (PROTACs) offer new cancer therapy strategies by degrading disease-causing proteins. While promising for broadening drug targets and overcoming resistance, challenges remain for their full clinical application.
Area of Science:
- Oncology
- Molecular Biology
- Drug Discovery
Background:
- Small-molecule targeted protein degraders are revolutionizing cancer research.
- Proteolysis Targeting Chimeras (PROTACs) are bifunctional molecules enabling targeted protein degradation.
Purpose of the Study:
- To provide a concise perspective on the opportunities and challenges of PROTACs in cancer therapy.
- To highlight studies supporting PROTAC potential and assess current limitations.
Main Methods:
- Review of high-profile studies on PROTAC applications in cancer.
- Assessment of PROTACs' ability to broaden drug target scope, address resistance, and enhance selectivity.
- Discussion of future opportunities for bifunctional degrader molecules.
Main Results:
- PROTACs show potential for expanding drug target scope and overcoming resistance.
- Evidence supports PROTACs' ability to enhance target selectivity and tissue specificity.
- The full potential of PROTACs in specific cancer contexts is still under development.
Conclusions:
- PROTACs represent a significant advancement in targeted protein degradation for cancer therapy.
- Further research is needed to overcome current challenges and fully realize PROTACs' therapeutic benefits.
- The unique bifunctional nature of PROTACs presents exciting future opportunities in oncology.
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