Click Chemistry in Peptide-Based Drug Design

Molecules

Huiyuan Li¹  Rachna Aneja¹ 

[1] Department of Biochemistry and Molecular Biology, College of Medicine, Drexel University, 245 N 15th Street, New College Building, Room 11102, Philadelphia, PA 19102, USA;

关键词: click chemistry;    triazoles;    application;    peptides;    drug discovery;   

DOI  :  10.3390/molecules18089797

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2013 by the authors; licensee MDPI, Basel, Switzerland.