Cyclic, Cell-Penetrating Peptides Tailor-Made for the Creation of Peptide Libraries with Intrinsic Cell Permeability

12 June 2020, Version 1
This content is a preprint and has not undergone peer review at the time of posting.


The discovery of high-affinity peptides to many intracellular targets has become feasible through the development of diverse macrocyclic peptide libraries. But lack of cell permeability is a key feature hampering the use of these peptides as therapeutics. Here, we develop a set of small, cyclic peptide carriers that efficiently carry cargoes into the cytosol. These peptides are cyclized via side-chain alkylation, which makes them ideal for the creation of diverse mRNA or phage-displayed libraries with intrinsic cell permeability.


cell penetrating peptide
drug delivery
in vitro selection
cyclic peptides
Peptide Cyclization
cysteine alkylation

Supplementary materials

ChemRxiv version 6-8-20


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