Orthogonal ring-closing alkyne and olefin metathesis for the synthesis of small GTPase-targeting bicyclic peptides

Bicyclic peptides can inhibit biological targets hard to address with small molecules. Here, the authors combine two orthogonal ring-closing reactions to produce bicyclic peptides with improved bioactivity thereby providing a strategy that can greatly improve the structural diversity of such peptide...

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Main Authors: Philipp M. Cromm, Sebastian Schaubach, Jochen Spiegel, Alois Fürstner, Tom N. Grossmann, Herbert Waldmann
Format: Article
Language:English
Published: Nature Publishing Group 2016-04-01
Series:Nature Communications
Online Access:https://doi.org/10.1038/ncomms11300
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spelling doaj-6091ec26a2d4425d83166be139ae90e02021-05-11T11:00:51ZengNature Publishing GroupNature Communications2041-17232016-04-01711710.1038/ncomms11300Orthogonal ring-closing alkyne and olefin metathesis for the synthesis of small GTPase-targeting bicyclic peptidesPhilipp M. Cromm0Sebastian Schaubach1Jochen Spiegel2Alois Fürstner3Tom N. Grossmann4Herbert Waldmann5Department of Chemical Biology, Max-Planck-Institute of Molecular PhysiologyTechnische Universität Dortmund, Fakultät für Chemie and Chemische BiologieDepartment of Chemical Biology, Max-Planck-Institute of Molecular PhysiologyTechnische Universität Dortmund, Fakultät für Chemie and Chemische BiologieTechnische Universität Dortmund, Fakultät für Chemie and Chemische BiologieDepartment of Chemical Biology, Max-Planck-Institute of Molecular PhysiologyBicyclic peptides can inhibit biological targets hard to address with small molecules. Here, the authors combine two orthogonal ring-closing reactions to produce bicyclic peptides with improved bioactivity thereby providing a strategy that can greatly improve the structural diversity of such peptides.https://doi.org/10.1038/ncomms11300
collection DOAJ
language English
format Article
sources DOAJ
author Philipp M. Cromm
Sebastian Schaubach
Jochen Spiegel
Alois Fürstner
Tom N. Grossmann
Herbert Waldmann
spellingShingle Philipp M. Cromm
Sebastian Schaubach
Jochen Spiegel
Alois Fürstner
Tom N. Grossmann
Herbert Waldmann
Orthogonal ring-closing alkyne and olefin metathesis for the synthesis of small GTPase-targeting bicyclic peptides
Nature Communications
author_facet Philipp M. Cromm
Sebastian Schaubach
Jochen Spiegel
Alois Fürstner
Tom N. Grossmann
Herbert Waldmann
author_sort Philipp M. Cromm
title Orthogonal ring-closing alkyne and olefin metathesis for the synthesis of small GTPase-targeting bicyclic peptides
title_short Orthogonal ring-closing alkyne and olefin metathesis for the synthesis of small GTPase-targeting bicyclic peptides
title_full Orthogonal ring-closing alkyne and olefin metathesis for the synthesis of small GTPase-targeting bicyclic peptides
title_fullStr Orthogonal ring-closing alkyne and olefin metathesis for the synthesis of small GTPase-targeting bicyclic peptides
title_full_unstemmed Orthogonal ring-closing alkyne and olefin metathesis for the synthesis of small GTPase-targeting bicyclic peptides
title_sort orthogonal ring-closing alkyne and olefin metathesis for the synthesis of small gtpase-targeting bicyclic peptides
publisher Nature Publishing Group
series Nature Communications
issn 2041-1723
publishDate 2016-04-01
description Bicyclic peptides can inhibit biological targets hard to address with small molecules. Here, the authors combine two orthogonal ring-closing reactions to produce bicyclic peptides with improved bioactivity thereby providing a strategy that can greatly improve the structural diversity of such peptides.
url https://doi.org/10.1038/ncomms11300
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