Format

Send to

Choose Destination
Medchemcomm. 2012 Oct;3(10):1282-1289.

Optimizing PK properties of cyclic peptides: the effect of side chain substitutions on permeability and clearance().

Author information

1
Department 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.

Supplemental Content

Full text links

Icon for Royal Society of Chemistry Icon for PubMed Central
Loading ...
Support Center