Selective and Potent Proteomimetic Inhibitors of Intracellular Protein–Protein Interactions |
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| Authors: | Dr. Anna Barnard Dr. Kérya Long Dr. Heather L. Martin Dr. Jennifer A. Miles Dr. Thomas A. Edwards Dr. Darren C. Tomlinson Dr. Andrew Macdonald Prof. Andrew J. Wilson |
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| Affiliation: | 1. School of Chemistry, University of Leeds, Woodhouse Lane, Leeds LS2 9JT (UK);2. Astbury Centre For Structural Molecular Biology, University of Leeds, Woodhouse Lane, Leeds LS2 9JT (UK);3. Leeds Institute of Biomedical and Clinical Sciences, Wellcome Trust Brenner Building, University of Leeds, St. James's University Hospital, Leeds LS9 7TF (UK);4. School of Molecular and Cellular Biology, University of Leeds, Woodhouse Lane, Leeds LS2 9JT (UK) |
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| Abstract: | Inhibition of protein–protein interactions (PPIs) represents a major challenge in chemical biology and drug discovery. α‐Helix mediated PPIs may be amenable to modulation using generic chemotypes, termed “proteomimetics”, which can be assembled in a modular manner to reproduce the vectoral presentation of key side chains found on a helical motif from one partner within the PPI. In this work, it is demonstrated that by using a library of N‐alkylated aromatic oligoamide helix mimetics, potent helix mimetics which reproduce their biophysical binding selectivity in a cellular context can be identified. |
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| Keywords: | apoptosis foldamers helical structures peptidomimetics protein– protein interactions |
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