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Title: 
Application of the All-Hydrocarbon Stapling Technique in the Design of Membrane-Active Peptides
Authors: 
Huy Xuan, Luong
Hai Thi Phuong, Bui
Truong, Thanh Tung
Issue Date: 
2022
Publisher: 
ACS Publications
Abstract: 
The threats of drug resistance and new emerging pathogens have led to an urgent need to develop alternative treatment therapies. Recently, considerable research efforts have focused on membrane-active peptides (MAPs), a category of peptides in drug discovery with antimicrobial, anticancer, and cell penetration activities that have demonstrated their potential to be multifunctional agents. Nonetheless, natural MAPs have encountered various disadvantages, which mainly include poor bioavailability, the lack of a secondary structure in short peptides, and high production costs for long peptide sequences. Hence, an “all-hydrocarbon stapling system” has been applied to these peptides and proven to effectively stabilize the helical conformations, improving proteolytic resistance and increasing both the potency and the cell permeability. In this review, we summarized and categorized the advances made using this powerful technique in the development of stapled MAPs. Furthermore, outstanding issues and suggestions for future design within each subcategory were thoroughly discussed.
URI: 
https://pubs.acs.org/doi/10.1021/acs.jmedchem.1c01744
https://dlib.phenikaa-uni.edu.vn/handle/PNK/5873
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