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

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 presentat...

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Detalles Bibliográficos
Autores principales: Barnard, Anna, Long, Kérya, Martin, Heather L, Miles, Jennifer A, Edwards, Thomas A, Tomlinson, Darren C, Macdonald, Andrew, Wilson, Andrew J
Formato: Online Artículo Texto
Lenguaje:English
Publicado: WILEY-VCH Verlag 2015
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4506525/
https://www.ncbi.nlm.nih.gov/pubmed/25651514
http://dx.doi.org/10.1002/anie.201410810
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author Barnard, Anna
Long, Kérya
Martin, Heather L
Miles, Jennifer A
Edwards, Thomas A
Tomlinson, Darren C
Macdonald, Andrew
Wilson, Andrew J
author_facet Barnard, Anna
Long, Kérya
Martin, Heather L
Miles, Jennifer A
Edwards, Thomas A
Tomlinson, Darren C
Macdonald, Andrew
Wilson, Andrew J
author_sort Barnard, Anna
collection PubMed
description 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.
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spelling pubmed-45065252015-07-22 Selective and Potent Proteomimetic Inhibitors of Intracellular Protein–Protein Interactions** Barnard, Anna Long, Kérya Martin, Heather L Miles, Jennifer A Edwards, Thomas A Tomlinson, Darren C Macdonald, Andrew Wilson, Andrew J Angew Chem Int Ed Engl Communications 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. WILEY-VCH Verlag 2015-03-02 2015-02-04 /pmc/articles/PMC4506525/ /pubmed/25651514 http://dx.doi.org/10.1002/anie.201410810 Text en © 2015 The Authors. Published by Wiley-VCH Verlag GmbH & Co. KGaA. http://creativecommons.org/licenses/by/3.0/ This is an open access article under the terms of the Creative Commons Attribution License, which permits use, distribution and reproduction in any medium, provided the original work is properly cited.
spellingShingle Communications
Barnard, Anna
Long, Kérya
Martin, Heather L
Miles, Jennifer A
Edwards, Thomas A
Tomlinson, Darren C
Macdonald, Andrew
Wilson, Andrew J
Selective and Potent Proteomimetic Inhibitors of Intracellular Protein–Protein Interactions**
title Selective and Potent Proteomimetic Inhibitors of Intracellular Protein–Protein Interactions**
title_full Selective and Potent Proteomimetic Inhibitors of Intracellular Protein–Protein Interactions**
title_fullStr Selective and Potent Proteomimetic Inhibitors of Intracellular Protein–Protein Interactions**
title_full_unstemmed Selective and Potent Proteomimetic Inhibitors of Intracellular Protein–Protein Interactions**
title_short Selective and Potent Proteomimetic Inhibitors of Intracellular Protein–Protein Interactions**
title_sort selective and potent proteomimetic inhibitors of intracellular protein–protein interactions**
topic Communications
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4506525/
https://www.ncbi.nlm.nih.gov/pubmed/25651514
http://dx.doi.org/10.1002/anie.201410810
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