| Literature DB >> 25288495 |
Niyada Hin1, Jesse Alt1, Sarah C Zimmermann2, Greg Delahanty1, Dana V Ferraris1, Camilo Rojas1, Fengxian Li3, Qin Liu3, Xinzhong Dong4, Barbara S Slusher5, Takashi Tsukamoto6.
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.Entities:
Keywords: Agonist; Arginine mimetic; Mas-related gene (Mrg) receptors; Peptidomimetic
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Year: 2014 PMID： 25288495 PMCID： PMC4254045 DOI： 10.1016/j.bmc.2014.09.025
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641