Orthogonal functionalisation of α-helix mimetics

α-Helix mediated protein–protein interactions are of major therapeutic importance. As such, the design of inhibitors of this class of interaction is of significant interest. We present methodology to modify N-alkylated aromatic oligoamide α-helix mimetics using ‘click’ chemistry. The effect is shown...

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Autores principales: Barnard, Anna, Long, Kérya, Yeo, David J., Miles, Jennifer A., Azzarito, Valeria, Burslem, George M., Prabhakaran, Panchami, A. Edwards, Thomas, Wilson, Andrew J.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Royal Society of Chemistry 2014
Materias:
Chemistry
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4157654/
https://www.ncbi.nlm.nih.gov/pubmed/25065821
http://dx.doi.org/10.1039/c4ob00915k
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author Barnard, Anna
Long, Kérya
Yeo, David J.
Miles, Jennifer A.
Azzarito, Valeria
Burslem, George M.
Prabhakaran, Panchami
A. Edwards, Thomas
Wilson, Andrew J.
author_facet Barnard, Anna
Long, Kérya
Yeo, David J.
Miles, Jennifer A.
Azzarito, Valeria
Burslem, George M.
Prabhakaran, Panchami
A. Edwards, Thomas
Wilson, Andrew J.
author_sort Barnard, Anna
collection PubMed
description α-Helix mediated protein–protein interactions are of major therapeutic importance. As such, the design of inhibitors of this class of interaction is of significant interest. We present methodology to modify N-alkylated aromatic oligoamide α-helix mimetics using ‘click’ chemistry. The effect is shown to modulate the binding properties of a series of selective p53/hDM2 inhibitors.
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spelling pubmed-41576542014-09-10 Orthogonal functionalisation of α-helix mimetics Barnard, Anna Long, Kérya Yeo, David J. Miles, Jennifer A. Azzarito, Valeria Burslem, George M. Prabhakaran, Panchami A. Edwards, Thomas Wilson, Andrew J. Org Biomol Chem Chemistry α-Helix mediated protein–protein interactions are of major therapeutic importance. As such, the design of inhibitors of this class of interaction is of significant interest. We present methodology to modify N-alkylated aromatic oligoamide α-helix mimetics using ‘click’ chemistry. The effect is shown to modulate the binding properties of a series of selective p53/hDM2 inhibitors. Royal Society of Chemistry 2014-09-21 2014-07-28 /pmc/articles/PMC4157654/ /pubmed/25065821 http://dx.doi.org/10.1039/c4ob00915k Text en This journal is © The Royal Society of Chemistry 2014 http://creativecommons.org/licenses/by/3.0/ This is an Open Access article distributed under the terms of the Creative Commons Attribution 3.0 Unported License (http://creativecommons.org/licenses/by/3.0/) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Chemistry
Barnard, Anna
Long, Kérya
Yeo, David J.
Miles, Jennifer A.
Azzarito, Valeria
Burslem, George M.
Prabhakaran, Panchami
A. Edwards, Thomas
Wilson, Andrew J.
Orthogonal functionalisation of α-helix mimetics
title Orthogonal functionalisation of α-helix mimetics
title_full Orthogonal functionalisation of α-helix mimetics
title_fullStr Orthogonal functionalisation of α-helix mimetics
title_full_unstemmed Orthogonal functionalisation of α-helix mimetics
title_short Orthogonal functionalisation of α-helix mimetics
title_sort orthogonal functionalisation of α-helix mimetics
topic Chemistry
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4157654/
https://www.ncbi.nlm.nih.gov/pubmed/25065821
http://dx.doi.org/10.1039/c4ob00915k
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