Selective and Potent Proteomimetic Inhibitors of Intracellular Protein–Protein Interactions1. Issue 10 (4th February 2015)

• Record Type: Journal Article
• Authors: Barnard, Anna; Long, Kérya; Martin, Heather L.; Miles, Jennifer A.; Edwards, Thomas A.; Tomlinson, Darren C.; Macdonald, Andrew; Wilson, Andrew J.
• Is Part Of: Angewandte Chemie international edition. Volume 54:Issue 10(2015)
• Page Start: 2960
• Page End: 2965
• Publication Date: 2015-02-04
• Subjects: Chemistry -- Periodicals; 540
• DOI: 10.1002/anie.201410810
• Languages: English
• ISSNs: 1433-7851

Abstract

<abstract abstract-type="main" xml:lang="en"> <title>Abstract</title> <p>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.</p> </abstract>