Jump to main content
Jump to site search


Achieving enhanced cell penetration of short conformationally constrained peptides through amphiphilicity tuning

Author affiliations

Abstract

Due to their enhanced stability and cell permeability, cyclic cell-penetrating peptides have been widely used as delivery vectors for transporting cell-impermeable cargos into cells. In this study, we synthesized a panel of conformationally constrained peptides with either α-helix or β-hairpin conformations. We tuned the amphiphilicity of these constrained peptides with different distributions of charged or hydrophobic residues and compared their cellular uptake efficiencies in different cell lines. We found that the amphipathicity of these conformationally constrained peptides correlates well with their cellular uptake efficiency. We proposed that peptides with larger hydrophobic moments (HMs) have stronger binding affinities with the cell membrane which further accelerates the endocytosis process. This finding should provide an approach towards the design of more potent conformationally constrained cell-penetrating peptides for biomedical applications.

Graphical abstract: Achieving enhanced cell penetration of short conformationally constrained peptides through amphiphilicity tuning

Back to tab navigation

Supplementary files

Publication details

The article was received on 17 Aug 2017, accepted on 12 Sep 2017 and first published on 13 Sep 2017


Article type: Edge Article
DOI: 10.1039/C7SC03614K
Citation: Chem. Sci., 2017, Advance Article
  • Open access: Creative Commons BY license
  •   Request permissions

    Achieving enhanced cell penetration of short conformationally constrained peptides through amphiphilicity tuning

    Y. Tian, X. Zeng, J. Li, Y. Jiang, H. Zhao, D. Wang, X. Huang and Z. Li, Chem. Sci., 2017, Advance Article , DOI: 10.1039/C7SC03614K

    This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. Material from this article can be used in other publications provided that the correct acknowledgement is given with the reproduced material.

    Reproduced material should be attributed as follows:

    • For reproduction of material from NJC:
      [Original citation] - Published by The Royal Society of Chemistry (RSC) on behalf of the Centre National de la Recherche Scientifique (CNRS) and the RSC.
    • For reproduction of material from PCCP:
      [Original citation] - Published by the PCCP Owner Societies.
    • For reproduction of material from PPS:
      [Original citation] - Published by The Royal Society of Chemistry (RSC) on behalf of the European Society for Photobiology, the European Photochemistry Association, and RSC.
    • For reproduction of material from all other RSC journals:
      [Original citation] - Published by The Royal Society of Chemistry.

    Information about reproducing material from RSC articles with different licences is available on our Permission Requests page.

Search articles by author

Spotlight

Advertisements