2018 Fiscal Year Final Research Report
Chemical biological studies
| Project/Area Number |
15K01810
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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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| Research Field |
Biomolecular chemistry
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| Research Institution | Chubu University |
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Principal Investigator |
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| Co-Investigator(Kenkyū-buntansha) |
禹 済泰 中部大学, 応用生物学部, 教授 (20272693)
饒村 修 中部大学, 工学部, 准教授 (20365175)
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| Project Period (FY) |
2015-04-01 – 2019-03-31
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| Keywords | プロテインホスファターゼ / 天然低分子物質 / 生理活性物質 |
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| Outline of Final Research Achievements |
Metal-dependent protein phosphatases (PPMs) are Mg2+/Mn2+-dependent enzymes that specifically phosphorylate Ser and Thr residues, and at least 17 different PPM genes are present in the mammalian genome. Although they are central players in disease pathogenesis, only few inhibitors of PPM phosphatases have been reported and more potent and selective small molecules regulating these enzymes are expected to be developed. In this study, the docking simulation was performed for several small molecules identified as activators of PPM1A and PPM1B to elucidate their binding sites within these phosphatases. Furthermore, we investigated the effects of these compounds on osteoclast differentiation among RAW264 cells and lipid accumulation in 3T3-L1 adipocytes.
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| Free Research Field |
生化学・分子生物学
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| Academic Significance and Societal Importance of the Research Achievements |
PPM1AおよびPPM1Bの活性化物質としてこれまでに同定されたglabridinとpisiferdiolが、細胞におけるこれらの酵素の生理機能を解明する上で、分子プローブとして有効であることが示された。また本研究により、これらの化合物によってPPM1AやPPM1Bの活性を制御することが、骨粗鬆症、肥満、糖尿病などの疾患の治療や予防に有効である可能性が示されたため、これらの酵素を標的とした薬剤や食品機能性成分の開発が期待される。
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