title: Modifying peptides to enhance permeability.
abstract: Recently, peptides have been validated to address intracellular targets and/or to be orally bioavailable. This review describes some of these scaffolds, offers insight in new cyclization methodologies thought to be beneficial to enhance permeability, and highlights modification on peptides thought to improve oral bioavailability. In this context, side chains and back-bone derivatization beneficial to encourage cellular uptake are presented. In addition, new methodologies supporting the assessment of permeability are discussed.
authors.affiliation: Novartis Institutes for Biomedical Research, CH-4056 Basel, Switzerland.
authors.forename: Thomas
authors.initials: T
authors.lastname: Vorherr
mesh_terms: D006801:Humans; D010455:Peptides / Q000737:chemistry / Q000378:metabolism*; D010539:Permeability
chemical_list: D010455:Peptides