title: Peptidomimetics of Arg-Phe-NH2 as small molecule agonists of Mas-related gene C (MrgC) receptors.
abstract: A series of Arg-Phe-NH2 peptidomimetics containing an Arg mimetic were synthesized and tested as agonists of human MrgX1, rat MrgC, and mouse MrgC11 receptors. As predicted from the previously established species specificity, these peptidomimetics were found to be devoid of MrgX1 agonist activity. In contrast, these compounds acted as agonists of MrgC and/or MrgC11 with varying degrees of potency. These new peptidomimetics should complement the existing small molecule human MrgX1 agonists and enhance our ability to assess the therapeutic utility of targeting Mrg receptors in rodent models.
authors.affiliation: Brain Science Institute, Johns Hopkins University, Baltimore, MD 21205, United States.
authors.forename: Niyada
authors.initials: N
authors.lastname: Hin
authors.affiliation: Brain Science Institute, Johns Hopkins University, Baltimore, MD 21205, United States.
authors.forename: Jesse
authors.initials: J
authors.lastname: Alt
authors.affiliation: Department of Neurology, Johns Hopkins University, Baltimore, MD 21205, United States.
authors.forename: Sarah C
authors.initials: SC
authors.lastname: Zimmermann
authors.affiliation: Brain Science Institute, Johns Hopkins University, Baltimore, MD 21205, United States.
authors.forename: Greg
authors.initials: G
authors.lastname: Delahanty
authors.affiliation: Brain Science Institute, Johns Hopkins University, Baltimore, MD 21205, United States.
authors.forename: Dana V
authors.initials: DV
authors.lastname: Ferraris
authors.affiliation: Brain Science Institute, Johns Hopkins University, Baltimore, MD 21205, United States.
authors.forename: Camilo
authors.initials: C
authors.lastname: Rojas
authors.affiliation: Center for the Study of Itch and Departments of Anesthesiology and Anatomy & Neurobiology, Washington University School of Medicine, St Louis, MO 63110, United States.
authors.forename: Fengxian
authors.initials: F
authors.lastname: Li
authors.affiliation: Center for the Study of Itch and Departments of Anesthesiology and Anatomy & Neurobiology, Washington University School of Medicine, St Louis, MO 63110, United States.
authors.forename: Qin
authors.initials: Q
authors.lastname: Liu
authors.affiliation: The Solomon H. Snyder Department of Neuroscience, Johns Hopkins University, Baltimore, MD 21205, United States.
authors.forename: Xinzhong
authors.initials: X
authors.lastname: Dong
authors.affiliation: Brain Science Institute, Johns Hopkins University, Baltimore, MD 21205, United States; Department of Neurology, Johns Hopkins University, Baltimore, MD 21205, United States.
authors.forename: Barbara S
authors.initials: BS
authors.lastname: Slusher
authors.affiliation: Brain Science Institute, Johns Hopkins University, Baltimore, MD 21205, United States; Department of Neurology, Johns Hopkins University, Baltimore, MD 21205, United States. Electronic address: ttsukamoto@jhmi.edu.
authors.forename: Takashi
authors.initials: T
authors.lastname: Tsukamoto
mesh_terms: D000818:Animals; D057809:HEK293 Cells; D006801:Humans; D051379:Mice; D009479:Neuropeptides / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism; D057786:Peptidomimetics / Q000494:pharmacology; D011485:Protein Binding / Q000187:drug effects; D051381:Rats; D043562:Receptors, G-Protein-Coupled / Q000819:agonists* / Q000235:genetics / Q000378:metabolism; D054852:Small Molecule Libraries / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D014162:Transfection
chemical_list: D009479:Neuropeptides; D057786:Peptidomimetics; D043562:Receptors, G-Protein-Coupled; D054852:Small Molecule Libraries; C470192:Mrgprx1 protein, mouse; C000591603:Mrgprc protein, rat; C510803:mas-related gene-X1 receptor, human; C058047:arginylphenylalaninamide
keywords: Agonist; Arginine mimetic; Mas-related gene (Mrg) receptors; Peptidomimetic