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

Authors :
Philipp M. Cromm
Sebastian Schaubach
Jochen Spiegel
Alois Fürstner
Tom N. Grossmann
Herbert Waldmann
Source :
Nature Communications, Vol 7, Iss 1, Pp 1-7 (2016)
Publication Year :
2016
Publisher :
Nature Portfolio, 2016.

Abstract

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.

Subjects

Subjects :
Science

Details

Language :
English
ISSN :
20411723
Volume :
7
Issue :
1
Database :
Directory of Open Access Journals
Journal :
Nature Communications
Publication Type :
Academic Journal
Accession number :
edsdoj.6091ec26a2d4425d83166be139ae90e0
Document Type :
article
Full Text :
https://doi.org/10.1038/ncomms11300