Peptidomimetics of Arg-Phe-NH2 as small molecule agonists of Mas-related gene C (MrgC) receptors

Niyada Hin, Jesse Alt, Sarah C. Zimmermann, Greg Delahanty, Dana V. Ferraris, Camilo Rojas, Fengxian Li, Qin Liu, Xinzhong Dong, Barbara S. Slusher, Takashi Tsukamoto

Research output: Contribution to journalArticlepeer-review

4 Scopus citations


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.

Original languageEnglish
Pages (from-to)5831-5837
Number of pages7
JournalBioorganic and Medicinal Chemistry
Issue number21
StatePublished - Nov 1 2014


  • Agonist
  • Arginine mimetic
  • Mas-related gene
  • Mrg) receptors
  • Peptidomimetic


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