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: 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: Anna
authors: A
authors: Barnard
authors: Kérya
authors: K
authors: Long
authors: Heather L
authors: HL
authors: Martin
authors: Jennifer A
authors: JA
authors: Miles
authors: Thomas A
authors: TA
authors: Edwards
authors: Darren C
authors: DC
authors: Tomlinson
authors: Andrew
authors: A
authors: Macdonald
authors: Andrew J
authors: AJ
authors: Wilson
mesh_terms: D045744:Cell Line, Tumor; D006801:Humans; D018716:Molecular Mimicry; D011506:Proteins / Q000737:chemistry*
chemical_list: D011506:Proteins
keywords: apoptosis; foldamers; helical structures; peptidomimetics; protein-protein interactions
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