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Molecules 2013, 18(8), 9797-9817; doi:10.3390/molecules18089797

Click Chemistry in Peptide-Based Drug Design

Department of Biochemistry and Molecular Biology, College of Medicine, Drexel University, 245 N 15th Street, New College Building, Room 11102, Philadelphia, PA 19102, USA
* Author to whom correspondence should be addressed.
Received: 15 July 2013 / Revised: 9 August 2013 / Accepted: 12 August 2013 / Published: 16 August 2013
(This article belongs to the Special Issue Advances in Click Chemistry)
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Click chemistry is an efficient and chemoselective synthetic method for coupling molecular fragments under mild reaction conditions. Since the advent in 2001 of methods to improve stereochemical conservation, the click chemistry approach has been broadly used to construct diverse chemotypes in both chemical and biological fields. In this review, we discuss the application of click chemistry in peptide-based drug design. We highlight how triazoles formed by click reactions have been used for mimicking peptide and disulfide bonds, building secondary structural components of peptides, linking functional groups together, and bioconjugation. The progress made in this field opens the way for synthetic approaches to convert peptides with promising functional leads into structure-minimized and more stable forms.
Keywords: click chemistry; triazoles; application; peptides; drug discovery click chemistry; triazoles; application; peptides; drug discovery
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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Li, H.; Aneja, R.; Chaiken, I. Click Chemistry in Peptide-Based Drug Design. Molecules 2013, 18, 9797-9817.

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