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Wiley, Angewandte Chemie International Edition, 10(54), p. 2960-2965, 2015

DOI: 10.1002/anie.201410810

Wiley, Angewandte Chemie, 10(127), p. 3003-3008, 2015

DOI: 10.1002/ange.201410810

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Selective and Potent Proteomimetic Inhibitors of Intracellular Protein–Protein Interactions**

Journal article published in 2015 by Anna Barnard, Kérya Long, Heather L. Martin ORCID, Jennifer A. Miles ORCID, Andrew J. Wilson, Thomas Alfred Edwards, Darren C. Tomlinson, Andrew Macdonald, Wilson Andrew
This paper is available in a repository.
This paper is available in a repository.

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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.