Cyclic Penta- and Hexaleucine Peptides without N-Methylation Are Orally Absorbed.

@article{Hill2014CyclicPA,
  title={Cyclic Penta- and Hexaleucine Peptides without N-Methylation Are Orally Absorbed.},
  author={Timothy A. Hill and R. H. Lohman and Huy N. Hoang and Daniel Stefek Frank Nielsen and Conor C. G. Scully and W. Mei Kok and Ligong Liu and Andrew J. Lucke and Martin J. Stoermer and Christina I Schroeder and Stephanie Chaousis and Barbara Colless and Paul V Bernhardt and David J Edmonds and David A. Griffith and Charles J. Rotter and Roger B. Ruggeri and David A. Price and Spiros Liras and David J. Craik and David P. Fairlie},
  journal={ACS medicinal chemistry letters},
  year={2014},
  volume={5 10},
  pages={1148-51}
}
Development of peptide-based drugs has been severely limited by lack of oral bioavailability with less than a handful of peptides being truly orally bioavailable, mainly cyclic peptides with N-methyl amino acids and few hydrogen bond donors. Here we report that cyclic penta- and hexa-leucine peptides, with no N-methylation and five or six amide NH protons, exhibit some degree of oral bioavailability (4-17%) approaching that of the heavily N-methylated drug cyclosporine (22%) under the same… CONTINUE READING

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