title: Peptidomimetic therapeutics: scientific approaches and opportunities.
abstract: Natural endogenously occurring peptides exhibit desirable medicinal properties, but are often limited in application by rapid proteolysis and inadequate membrane permeability. However, editing naturally occurring peptide sequences to develop peptidomimetic analogs created a promising class of therapeutics that can augment or inhibit molecular interactions. Here, we discuss a variety of chemical modifications, including l to d isomerization, cyclization, and unnatural amino acid substitution, as well as design strategies, such as attachment to cell-penetrating peptides, which are used to develop peptidomimetics. We also provide examples of approved peptidomimetics and discuss several compounds in clinical trials.
authors.affiliation: Stanford University, Department of Chemical and Systems Biology, School of Medicine, Stanford, CA 94305, USA. Electronic address: nirqvit@stanford.edu.
authors.forename: Nir
authors.initials: N
authors.lastname: Qvit
authors.affiliation: Stanford University, Immunology Program, School of Medicine, Stanford, CA 94305, USA.
authors.forename: Samuel J S
authors.initials: SJS
authors.lastname: Rubin
authors.affiliation: Stanford University, Department of Chemical and Systems Biology, School of Medicine, Stanford, CA 94305, USA; Stanford University, Department of Anesthesiology, Perioperative and Pain Medicine, School of Medicine, Stanford, CA 94305, USA.
authors.forename: Travis J
authors.initials: TJ
authors.lastname: Urban
authors.affiliation: Stanford University, Department of Chemical and Systems Biology, School of Medicine, Stanford, CA 94305, USA.
authors.forename: Daria
authors.initials: D
authors.lastname: Mochly-Rosen
authors.affiliation: Stanford University, Department of Anesthesiology, Perioperative and Pain Medicine, School of Medicine, Stanford, CA 94305, USA.
authors.forename: Eric R
authors.initials: ER
authors.lastname: Gross
mesh_terms: D019943:Amino Acid Substitution; D000818:Animals; D015195:Drug Design; D006801:Humans; D010455:Peptides / Q000008:administration & dosage / Q000737:chemistry / Q000627:therapeutic use; D057786:Peptidomimetics
chemical_list: D010455:Peptides; D057786:Peptidomimetics