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Recent Advances in CBP/EP300 Degraders
Leonardo Palaferri1, Iván Cheng-Sánchez2, Cristina Nevado3
1University of Zurich, Department of Chemistry, CH-8057 Zurich, Switzerland. leonardo.palaferri@chem.uzh.ch.
Targeted protein degradation (TPD) utilizes novel PROTACs and MGDs to eliminate proteins. New degraders targeting CBP/EP300 show promise as anticancer agents by disrupting transcription.
Area of Science:
- Biochemistry
- Molecular Biology
- Drug Discovery
Background:
- Targeted protein degradation (TPD) offers advantages over traditional inhibitors.
- Proteolysis targeting chimeras (PROTACs) and molecular glue degraders (MGDs) are leading TPD modalities.
- These degraders utilize the ubiquitin-proteasome system (UPS) for protein elimination.
Purpose of the Study:
- To review the latest advancements in developing degraders for CBP/EP300.
- To highlight the therapeutic potential of CBP/EP300 degraders in cancer treatment.
Main Methods:
- Review of current literature on CBP/EP300 degraders.
- Analysis of the mechanisms of action for PROTACs and MGDs targeting CBP/EP300.
Main Results:
- CBP/EP300 are critical for transcription and are targets for novel degraders.
- Synthetic bifunctional compounds effectively degrade CBP/EP300.
- These degraders demonstrate significant potential as anticancer agents.
Conclusions:
- CBP/EP300 degraders represent a promising new frontier in cancer therapy.
- These compounds serve as valuable chemical tools for biological research.
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