title: Selective and Potent Proteomimetic Inhibitors of Intracellular Protein-Protein Interactions.
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.
authors.affiliation: School of Chemistry, University of Leeds, Woodhouse Lane, Leeds LS2 9JT (UK); Astbury Centre For Structural Molecular Biology, University of Leeds, Woodhouse Lane, Leeds LS2 9JT (UK).
authors.forename: Anna
authors.initials: A
authors.lastname: Barnard
authors.affiliation: School of Chemistry, University of Leeds, Woodhouse Lane, Leeds LS2 9JT (UK); Astbury Centre For Structural Molecular Biology, University of Leeds, Woodhouse Lane, Leeds LS2 9JT (UK).
authors.forename: Kérya
authors.initials: K
authors.lastname: Long
authors.affiliation: Leeds Institute of Biomedical and Clinical Sciences, Wellcome Trust Brenner Building, University of Leeds, St. James's University Hospital, Leeds LS9 7TF (UK).
authors.forename: Heather L
authors.initials: HL
authors.lastname: Martin
authors.affiliation: School of Chemistry, University of Leeds, Woodhouse Lane, Leeds LS2 9JT (UK); Astbury Centre For Structural Molecular Biology, University of Leeds, Woodhouse Lane, Leeds LS2 9JT (UK).
authors.forename: Jennifer A
authors.initials: JA
authors.lastname: Miles
authors.affiliation: Astbury Centre For Structural Molecular Biology, University of Leeds, Woodhouse Lane, Leeds LS2 9JT (UK); School of Molecular and Cellular Biology, University of Leeds, Woodhouse Lane, Leeds LS2 9JT (UK).
authors.forename: Thomas A
authors.initials: TA
authors.lastname: Edwards
authors.affiliation: Astbury Centre For Structural Molecular Biology, University of Leeds, Woodhouse Lane, Leeds LS2 9JT (UK); School of Molecular and Cellular Biology, University of Leeds, Woodhouse Lane, Leeds LS2 9JT (UK).
authors.forename: Darren C
authors.initials: DC
authors.lastname: Tomlinson
authors.affiliation: Astbury Centre For Structural Molecular Biology, University of Leeds, Woodhouse Lane, Leeds LS2 9JT (UK); School of Molecular and Cellular Biology, University of Leeds, Woodhouse Lane, Leeds LS2 9JT (UK).
authors.forename: Andrew
authors.initials: A
authors.lastname: Macdonald
authors.affiliation: School of Chemistry, University of Leeds, Woodhouse Lane, Leeds LS2 9JT (UK); Astbury Centre For Structural Molecular Biology, University of Leeds, Woodhouse Lane, Leeds LS2 9JT (UK).
authors.forename: Andrew J
authors.initials: AJ
authors.lastname: Wilson
keywords: Apoptose; Foldamere; Helikale Strukturen; Peptidomimetika; Protein‐Protein‐Wechselwirkungen