title: [Conformation-activity relations of dermorphin and its pentapeptide analogs].
abstract: Low-energy peptide backbone structures of dermorphin (DM), amide of its N-terminal pentapeptide (DM 1-5) and DM 1-5 analogues with substitutions of Gly4 for Leu, D-Gln, Aal or Tal were determined by energy calculations. The above analogues were shown to possess different affinities toward opiate receptors of mu-type. The comparison of low-energy backbone structures of DM, DM 1-5 and its analogues resulted in development of the dermorphin "biologically active" conformation being characteristic of its binding with mu-type receptors. The specific binding of dermorphin to this receptor apparently depends on the conformation of the whole N-terminal pentapeptide.
authors.forename: M D
authors.initials: MD
authors.lastname: Shenderovich
authors.forename: I T
authors.initials: IT
authors.lastname: Liepinia
authors.forename: G V
authors.initials: GV
authors.lastname: Nikiforovich
authors.forename: N V
authors.initials: NV
authors.lastname: Sumbatian
authors.forename: G A
authors.initials: GA
authors.lastname: Korshunova
authors.forename: Iu P
authors.initials: IuP
authors.lastname: Shvachkin
mesh_terms: D000595:Amino Acid Sequence; D008969:Molecular Sequence Data; D009842:Oligopeptides / Q000378:metabolism*; D018847:Opioid Peptides; D011487:Protein Conformation; D011957:Receptors, Opioid / Q000378:metabolism; D017450:Receptors, Opioid, mu; D013329:Structure-Activity Relationship
chemical_list: D009842:Oligopeptides; D018847:Opioid Peptides; D011957:Receptors, Opioid; D017450:Receptors, Opioid, mu; C030058:dermorphin
vernacular_title: Konformatsionno-funktsional'nye otnosheniia dermorfina i ego pentapeptidnykh analogov.