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Improvement on Permeability of Cyclic Peptide/Peptidomimetic: Backbone N-Methylation as A Useful Tool

Li, Yang, Li, Wang, Xu, Zhengshuang·2021·Marine Drugs
DOI 10.3390/md19060311
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Abstract

Peptides have a three-dimensional configuration that can adopt particular conformations for binding to proteins, which are well suited to interact with larger contact surface areas on target proteins. However, low cell permeability is a major challenge in the development of peptide-related drugs. In recent years, backbone N-methylation has been a useful tool for manipulating the permeability of cyclic peptides/peptidomimetics. Backbone N-methylation permits the adjustment of molecule’s conformational space. Several pathways are involved in the drug absorption pathway; the relative importance of each N-methylation to total permeation is likely to differ with intrinsic properties of cyclic peptide/peptidomimetic. Recent studies on the permeability of cyclic peptides/peptidomimetics using the backbone N-methylation strategy and synthetic methodologies will be presented in this review.

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Metadata

Authors
Li, Y., Li, W., & Xu, Z.
Venue
Marine Drugs
Publisher
MDPI AG
Published
2021-05-27
Volume
19
Issue
6
Pages
311
ISSN
1660-3397
DOI
10.3390/md19060311
Cited by
59
References
6
Language
en
Licence
creativecommons.org/licenses/by/4.0/ (vor)
Funders
  • Shenzhen Science and Technology Innovation Commission (JCYJ20170412151002616)
  • National Natural Science Foundation of China (25172007)

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