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• W2024607730 abstract "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 conditions. These simple cyclic peptides demonstrate that oral bioavailability is achievable for peptides that fall outside of rule-of-five guidelines without the need for N-methylation or modified amino acids." @default.
• W2024607730 created "2016-06-24" @default.
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• W2024607730 date "2014-08-07" @default.
• W2024607730 modified "2023-10-16" @default.
• W2024607730 title "Cyclic Penta- and Hexaleucine Peptides without <i>N</i>-Methylation Are Orally Absorbed" @default.
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• W2024607730 doi "https://doi.org/10.1021/ml5002823" @default.
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