Fluorescent amino acid initiated de novo cyclic peptides for the label‐free assessment of cell permeability
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Published version
Supporting information
Author(s)
Type
Journal Article
Abstract
The major obstacle in applying peptides to intracellular targets is their low inherent cell permeability. Standard approaches to attach a fluorophore (e.g. FITC, TAMRA) can change the physicochemical properties of the parent peptide and influence their ability to penetrate and localize in cells. We report a label-free strategy for evaluating the cell permeability of cyclic peptide leads. Fluorescent tryptophan analogues 4-cyanotryptophan (4CNW) and beta-(1-azulenyl)-L-alanine (AzAla) were incorporated into in vitro translated macrocyclic peptides by initiator reprogramming. We then demonstrate these efficient blue fluorescent emitters are good tools for monitoring peptide penetration into cells.
Date Issued
2021-10-15
Date Acceptance
2021-07-08
Citation
ChemMedChem, 2021, 16 (20), pp.3185-3188
ISSN
1860-7179
Publisher
Wiley
Start Page
3185
End Page
3188
Journal / Book Title
ChemMedChem
Volume
16
Issue
20
Copyright Statement
© 2021 The Authors. ChemMedChem published by Wiley-VCH GmbH. This is an open access article under the terms of the Creative Commons Attribution
License, which permits use, distribution and reproduction in any medium,
provided the original work is properly cited.
License, which permits use, distribution and reproduction in any medium,
provided the original work is properly cited.
License URL
Identifier
https://chemistry-europe.onlinelibrary.wiley.com/doi/10.1002/cmdc.202100315
Subjects
Science & Technology
Life Sciences & Biomedicine
Chemistry, Medicinal
Pharmacology & Pharmacy
RaPID
peptides
label-free
cell permeability
fluorescence imaging
RaPID
cell permeability
fluorescence imaging
label-free
peptides
Medicinal & Biomolecular Chemistry
0304 Medicinal and Biomolecular Chemistry
0305 Organic Chemistry
1115 Pharmacology and Pharmaceutical Sciences
Publication Status
Published
Date Publish Online
2021-07-28