Fluorescent amino acid initiated de novo cyclic peptides for the label-free assessment of cell permeability
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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.
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Journal ChemMedChem
Volume 16
Issue number 20
Pages 3185-3188
Available online
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Publisher website (DOI) 10.1002/cmdc.202100315
Europe PubMed Central 34236771
Pubmed 34236771
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