title: EPSA: A Novel Supercritical Fluid Chromatography Technique Enabling the Design of Permeable Cyclic Peptides.
abstract: 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.
authors.affiliation: Worldwide Medicinal Chemistry, Pfizer Global Research & Development, Groton Laboratories, Eastern Point Road, Groton, Connecticut 06340, United States.
authors.forename: Gilles H
authors.initials: GH
authors.lastname: Goetz
authors.affiliation: Worldwide Medicinal Chemistry, Pfizer Global Research & Development, Groton Laboratories, Eastern Point Road, Groton, Connecticut 06340, United States.
authors.forename: Laurence
authors.initials: L
authors.lastname: Philippe
authors.affiliation: Worldwide Medicinal Chemistry, Pfizer Global Research & Development, Groton Laboratories, Eastern Point Road, Groton, Connecticut 06340, United States.
authors.forename: Michael J
authors.initials: MJ
authors.lastname: Shapiro
keywords: EPSA; cyclic peptides; intramolecular hydrogen bonding; permeability; polarity