Targeting the Untouchables: Covalent Peptides That Target Elusive Transcription Factors
June 27, 2025
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9 min
Researchers at the University of Bath have developed a novel method to create irreversible inhibitors for transcription factors, specifically targeting cJun, a protein associated with melanoma and various cancers. By utilizing a peptide library and adding a reactive 'warhead,' they successfully designed HW33, which forms a permanent bond with cJun's cysteine site, making it more potent and selective. This innovative approach showcases the potential for new treatments for difficult-to-target proteins, contributing to advancements in cancer therapies and other diseases.
1. Developed irreversible inhibitors targeting cJun for melanoma treatment. 2. Used a peptide library and introduced a 'warhead' for bond permanence. 3. HW33 effectively decreased cJun levels in melanoma cells. 4. Emphasized specificity and reduced off-target effects in drug design. 5. Method applicable to other transcription factors and potentially various diseases. 6. Challenges include cell entry, stability, and specificity of the inhibitors. 7. Future improvements may enhance therapeutic delivery systems.
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