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Click Chemistry in Peptide-Based Drug Design
Journal article   Open access   Peer reviewed

Click Chemistry in Peptide-Based Drug Design

Huiyuan Li, Rachna Aneja and Irwin Chaiken
Molecules (Basel, Switzerland), v 18(8), pp 9797-9817
Aug 2013
PMID: 23959192
url
https://doi.org/10.3390/molecules18089797View
Published, Version of Record (VoR) Open

Abstract

triazoles click chemistry peptides Review application drug discovery
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.

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Web of Science research areas
Biochemistry & Molecular Biology
Chemistry, Multidisciplinary
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