Selective and Potent Proteomimetic Inhibitors of Intracellular Protein-Protein Interactions.

Autor:	Barnard A; 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)., Long K; 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)., Martin HL; Leeds Institute of Biomedical and Clinical Sciences, Wellcome Trust Brenner Building, University of Leeds, St. James's University Hospital, Leeds LS9 7TF (UK)., Miles JA; 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)., Edwards TA; 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)., Tomlinson DC; 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)., Macdonald A; 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)., Wilson AJ; 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).
Jazyk:	angličtina
Zdroj:	Angewandte Chemie (Weinheim an der Bergstrasse, Germany) [Angew Chem Weinheim Bergstr Ger] 2015 Mar 02; Vol. 127 (10), pp. 3003-3008. Date of Electronic Publication: 2015 Jan 30.
DOI:	10.1002/ange.201410810
Abstrakt:	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.
Databáze:	MEDLINE
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