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Application of the All-Hydrocarbon Stapling Technique in the Design of Membrane-Active Peptides

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...

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Main Authors: Huy Xuan, Luong, Hai Thi Phuong, Bui, Truong, Thanh Tung
Format: Bài trích
Language:English
Published: ACS Publications 2022
Subjects:
Hydrocarbons
Hydrophobicity
Online Access:https://pubs.acs.org/doi/10.1021/acs.jmedchem.1c01744
https://dlib.phenikaa-uni.edu.vn/handle/PNK/5873
https://doi.org/10.1021/acs.jmedchem.1c01744
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spelling oai:localhost:PNK-58732022-08-17T05:54:54Z Application of the All-Hydrocarbon Stapling Technique in the Design of Membrane-Active Peptides Huy Xuan, Luong Hai Thi Phuong, Bui Truong, Thanh Tung Hydrocarbons Hydrophobicity 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. 2022-07-13T01:59:46Z 2022-07-13T01:59:46Z 2022 Bài trích https://pubs.acs.org/doi/10.1021/acs.jmedchem.1c01744 https://dlib.phenikaa-uni.edu.vn/handle/PNK/5873 https://doi.org/10.1021/acs.jmedchem.1c01744 en ACS Publications
institution Digital Phenikaa
collection Digital Phenikaa
language English
topic Hydrocarbons
Hydrophobicity
spellingShingle Hydrocarbons
Hydrophobicity
Huy Xuan, Luong
Hai Thi Phuong, Bui
Truong, Thanh Tung
Application of the All-Hydrocarbon Stapling Technique in the Design of Membrane-Active Peptides
description 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.
format Bài trích
author Huy Xuan, Luong
Hai Thi Phuong, Bui
Truong, Thanh Tung
author_facet Huy Xuan, Luong
Hai Thi Phuong, Bui
Truong, Thanh Tung
author_sort Huy Xuan, Luong
title Application of the All-Hydrocarbon Stapling Technique in the Design of Membrane-Active Peptides
title_short Application of the All-Hydrocarbon Stapling Technique in the Design of Membrane-Active Peptides
title_full Application of the All-Hydrocarbon Stapling Technique in the Design of Membrane-Active Peptides
title_fullStr Application of the All-Hydrocarbon Stapling Technique in the Design of Membrane-Active Peptides
title_full_unstemmed Application of the All-Hydrocarbon Stapling Technique in the Design of Membrane-Active Peptides
title_sort application of the all-hydrocarbon stapling technique in the design of membrane-active peptides
publisher ACS Publications
publishDate 2022
url https://pubs.acs.org/doi/10.1021/acs.jmedchem.1c01744
https://dlib.phenikaa-uni.edu.vn/handle/PNK/5873
https://doi.org/10.1021/acs.jmedchem.1c01744
_version_ 1751856316381396992
score 8.891145

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