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Updated: May 17, 2026

Construction of Cyclic Cell-Penetrating Peptides for Enhanced Penetration of Biological Barriers
Published on: September 19, 2022
Optimizing PK properties of cyclic peptides: the effect of side chain substitutions on permeability and clearance()
Arthur C Rand1, Siegfried S F Leung, Heather Eng
1Department of Chemistry, University of California Santa Cruz, California, USA.
Abstract:
A series of cyclic peptides were designed and prepared to investigate the physicochemical properties that affect oral bioavailabilty of this chemotype in rats. In particular, the ionization state of the peptide was examined by the incorporation of naturally occurring amino acid residues that are charged in differing regions of the gut. In addition, data was generated in a variety of in vitro assays and the usefulness of this data in predicting the subsequent oral bioavailability observed in the rat is discussed.
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