Hin Niyada, Alt Jesse, Zimmermann Sarah C, Delahanty Greg, Ferraris Dana V, Rojas Camilo, Li Fengxian, Liu Qin, Dong Xinzhong, Slusher Barbara S, Tsukamoto Takashi
Brain Science Institute, Johns Hopkins University, Baltimore, MD 21205, United States.
Department of Neurology, Johns Hopkins University, Baltimore, MD 21205, United States.
Bioorg Med Chem. 2014 Nov 1;22(21):5831-7. doi: 10.1016/j.bmc.2014.09.025. Epub 2014 Sep 19.
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.
合成了一系列含有精氨酸模拟物的精氨酸-苯丙氨酸-氨基肽模拟物，并将其作为人MrgX1、大鼠MrgC和小鼠MrgC11受体的激动剂进行测试。正如根据先前确定的物种特异性所预测的那样，发现这些肽模拟物没有MrgX1激动剂活性。相反，这些化合物作为MrgC和/或MrgC11的激动剂，具有不同程度的效力。这些新的肽模拟物应补充现有的小分子人MrgX1激动剂，并增强我们在啮齿动物模型中评估靶向Mrg受体的治疗效用的能力。
