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Issue 10, 2012
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Optimizing PK properties of cyclic peptides: the effect of side chain substitutions on permeability and clearance

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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.

Graphical abstract: Optimizing PK properties of cyclic peptides: the effect of side chain substitutions on permeability and clearance

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Publication details

The article was received on 20 Jul 2012, accepted on 16 Aug 2012 and first published on 31 Aug 2012


Article type: Concise Article
DOI: 10.1039/C2MD20203D
Citation: Med. Chem. Commun., 2012,3, 1282-1289
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    Optimizing PK properties of cyclic peptides: the effect of side chain substitutions on permeability and clearance

    A. C. Rand, S. S. F. Leung, H. Eng, C. J. Rotter, R. Sharma, A. S. Kalgutkar, Y. Zhang, M. V. Varma, K. A. Farley, B. Khunte, C. Limberakis, D. A. Price, S. Liras, A. M. Mathiowetz, M. P. Jacobson and R. S. Lokey, Med. Chem. Commun., 2012, 3, 1282
    DOI: 10.1039/C2MD20203D

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