Click chemistry in peptide-based drug design

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...

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Bibliographic Details
Published inMolecules Vol. 18; no. 8; pp. 9797 - 9817
Main Authors Li, Huiyuan, Aneja, Rachna, Chaiken, Irwin
Format Journal Article Book Review
LanguageEnglish
Published Switzerland MDPI AG 16.08.2013
MDPI
Subjects
application
click chemistry
Click Chemistry - methods
Drug Design
drug discovery
Molecular Structure
peptides
Peptides - chemistry
Review
triazoles
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Summary: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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ISSN:1420-3049
1420-3049
DOI:10.3390/molecules18089797