Peptidomimetics of Arg-Phe-NH2 as small molecule agonists of Mas-related gene C (MrgC) receptors |
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| Affiliation: | 1. Jiangsu Co-innovation Center for Prevention and Control of Important Animal Infectious Diseases and Zoonoses, Yangzhou, Jiangsu 225009, China;2. Jiangsu Key Laboratory of Zoonosis, Yangzhou University, Yangzhou, Jiangsu 225009, China;3. Ministry of Education Key Lab for Avian Preventive Medicine, Yangzhou University, Yangzhou, Jiangsu 225009, China;1. Department of Orthopedics, The 81st Hospital of PLA, Nanjing, Jiangsu, China;2. Department of Orthopedics, Jinling Hospital, Nanjing, Jiangsu, China;3. Department of Orthopedics, Chenggong Hospital affiliated to Xiamen University, Xiamen, Fujian, China;4. Linjin Biotechnology Research Center, Nanjing, Jiangsu, China |
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| 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. |
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| Keywords: | Mas-related gene (Mrg) receptors Agonist Peptidomimetic Arginine mimetic |
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