2022 Fiscal Year Final Research Report
Development of peptidic NMUR1 antagonist and the application to suppression of type 2 inflammation
| Project/Area Number |
20K06974
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Multi-year Fund |
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| Section | 一般 |
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| Review Section |
Basic Section 47010:Pharmaceutical chemistry and drug development sciences-related
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| Research Institution | Kyoto Pharmaceutical University |
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Principal Investigator |
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| Project Period (FY) |
2020-04-01 – 2023-03-31
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| Keywords | ペプチドモジュレータ / ニューロメジンU / 抗炎症 / 抗肥満 |
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| Outline of Final Research Achievements |
Neuromedin U (NMU), which is well known as an anti-obesity peptide, is related to type 2 inflammation by the activation of mast cells, eosinophils and innate lymphoma cell 2 via NMU receptor 1 (NMUR1). To suppress the inflammation, development of NMUR1 antagonists would be one of the promising approach. In this study, a structure activity relationship study based on conventional NMU receptor modulators in our laboratory afforded a first peptide antagonist CPN-351 to human NMUR1. Also, a first partial agonist to human NMU receptor 2 (NMUR2) is successfully discovered. These new findings are valuable for understanding the molecular mechanism in the regulation of NMU receptor function.
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| Free Research Field |
ペプチド科学、生体機能化学
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| Academic Significance and Societal Importance of the Research Achievements |
本研究をもって、NMU受容体モジュレータとして、アゴニスト、パーシャルアゴニスト、アンタゴニストをNMUR1、NMUR2に対して全て揃えることができ、各受容体に立脚した機能解析や創薬を展開することができる基盤が整備された。NMUは肥満やエネルギー代謝調節のみならず、２型炎症、プロラクチン分泌などにも関わり、これを制御することによる健康増進を念頭にした研究を加速させることができる成果が得られたものである。
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