title: Formylated polyamines as peptidomimetics.
abstract: A new construct for imitating a natural peptide ligand using a modified retro-inverso sequence is described. It is demonstrated through the synthesis of a peptidomimetic derived from the endogenous sequence of leucine enkephalin. The product was active at 400 nM and selective for μ-opioid receptors.
authors.affiliation: The Skaggs Institute for Chemical Biology and Department of Chemistry, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, CA 92037, USA.
authors.forename: Sacha
authors.initials: S
authors.lastname: Javor
authors.forename: Aaron
authors.initials: A
authors.lastname: Janowsky
authors.forename: Robert
authors.initials: R
authors.lastname: Johnson
authors.forename: Katherine
authors.initials: K
authors.lastname: Wolfrum
authors.forename: Mitra
authors.initials: M
authors.lastname: Tadayoni-Rebek
authors.forename: Julius
authors.initials: J
authors.lastname: Rebek
mesh_terms: D001682:Biological Availability; D006801:Humans; D015394:Molecular Structure; D057786:Peptidomimetics / Q000138:chemical synthesis* / Q000737:chemistry* / Q000493:pharmacokinetics; D011073:Polyamines / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics*; D017450:Receptors, Opioid, mu / Q000737:chemistry
chemical_list: D057786:Peptidomimetics; D011073:Polyamines; D017450:Receptors, Opioid, mu