4.5 Article

EPSA: A Novel Supercritical Fluid Chromatography Technique Enabling the Design of Permeable Cyclic Peptides

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ACS MEDICINAL CHEMISTRY LETTERS
卷 5, 期 10, 页码 1167-1172

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AMER CHEMICAL SOC
DOI: 10.1021/ml500239m

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EPSA; cyclic peptides; permeability; polarity; intramolecular hydrogen bonding

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Most peptides are generally insufficiently permeable to be used as oral drugs. Designing peptides with improved permeability without reliable permeability monitoring is a challenge. We have developed a supercritical fluid chromatography technique for peptides, termed EPSA, which is shown here to enable improved permeability design. Through assessing the exposed polarity of a peptide, this technique can be used as a permeability surrogate.

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