Influence of Macrocyclization on Allosteric, Juxtamembrane-Derived, Stapled Peptide Inhibitors of the Epidermal Growth Factor Receptor (EGFR)

[Image: see text] The hydrocarbon-stapled peptide E1(S) allosterically inhibits the kinase activity of the epidermal growth factor receptor (EGFR) by blocking a distant but essential protein–protein interaction: a coiled coil formed from the juxtamembrane segment (JM) of each member of the dimeric p...

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Autores principales: Sinclair, Julie K.-L., Schepartz, Alanna
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2014
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4168776/
https://www.ncbi.nlm.nih.gov/pubmed/25207804
http://dx.doi.org/10.1021/ol502426b
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author Sinclair, Julie K.-L.
Schepartz, Alanna
author_facet Sinclair, Julie K.-L.
Schepartz, Alanna
author_sort Sinclair, Julie K.-L.
collection PubMed
description [Image: see text] The hydrocarbon-stapled peptide E1(S) allosterically inhibits the kinase activity of the epidermal growth factor receptor (EGFR) by blocking a distant but essential protein–protein interaction: a coiled coil formed from the juxtamembrane segment (JM) of each member of the dimeric partnership.1 Macrocyclization is not required for activity: the analogous unstapled (but alkene-bearing) peptide is equipotent in cell viability, immunoblot, and bipartite display experiments to detect coiled coil formation on the cell surface.
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spelling pubmed-41687762015-09-10 Influence of Macrocyclization on Allosteric, Juxtamembrane-Derived, Stapled Peptide Inhibitors of the Epidermal Growth Factor Receptor (EGFR) Sinclair, Julie K.-L. Schepartz, Alanna Org Lett [Image: see text] The hydrocarbon-stapled peptide E1(S) allosterically inhibits the kinase activity of the epidermal growth factor receptor (EGFR) by blocking a distant but essential protein–protein interaction: a coiled coil formed from the juxtamembrane segment (JM) of each member of the dimeric partnership.1 Macrocyclization is not required for activity: the analogous unstapled (but alkene-bearing) peptide is equipotent in cell viability, immunoblot, and bipartite display experiments to detect coiled coil formation on the cell surface. American Chemical Society 2014-09-10 2014-09-19 /pmc/articles/PMC4168776/ /pubmed/25207804 http://dx.doi.org/10.1021/ol502426b Text en Copyright © 2014 American Chemical Society Terms of Use (http://pubs.acs.org/page/policy/authorchoice_termsofuse.html)
spellingShingle Sinclair, Julie K.-L.
Schepartz, Alanna
Influence of Macrocyclization on Allosteric, Juxtamembrane-Derived, Stapled Peptide Inhibitors of the Epidermal Growth Factor Receptor (EGFR)
title Influence of Macrocyclization on Allosteric, Juxtamembrane-Derived, Stapled Peptide Inhibitors of the Epidermal Growth Factor Receptor (EGFR)
title_full Influence of Macrocyclization on Allosteric, Juxtamembrane-Derived, Stapled Peptide Inhibitors of the Epidermal Growth Factor Receptor (EGFR)
title_fullStr Influence of Macrocyclization on Allosteric, Juxtamembrane-Derived, Stapled Peptide Inhibitors of the Epidermal Growth Factor Receptor (EGFR)
title_full_unstemmed Influence of Macrocyclization on Allosteric, Juxtamembrane-Derived, Stapled Peptide Inhibitors of the Epidermal Growth Factor Receptor (EGFR)
title_short Influence of Macrocyclization on Allosteric, Juxtamembrane-Derived, Stapled Peptide Inhibitors of the Epidermal Growth Factor Receptor (EGFR)
title_sort influence of macrocyclization on allosteric, juxtamembrane-derived, stapled peptide inhibitors of the epidermal growth factor receptor (egfr)
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4168776/
https://www.ncbi.nlm.nih.gov/pubmed/25207804
http://dx.doi.org/10.1021/ol502426b
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