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 |
Section | 一般 |
Research Field |
Biomolecular chemistry
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Research Institution | Chubu University |
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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Project Status |
Completed (Fiscal Year 2018)
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Budget Amount *help |
¥4,810,000 (Direct Cost: ¥3,700,000、Indirect Cost: ¥1,110,000)
Fiscal Year 2017: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
Fiscal Year 2016: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2015: ¥2,470,000 (Direct Cost: ¥1,900,000、Indirect Cost: ¥570,000)
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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 / 阻害剤 / 破骨細胞 / シグナル伝達 |
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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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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Report
(5 results)
Research Products
(60 results)
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[Journal Article] Targeted disruption of the mouse protein phosphatase ppm1l gene leads to structural abnormalities in the brain.2016
Author(s)
Kusano R, Fujita K, Shinoda Y, Nagaura Y, Kiyonari H, Abe T, Watanabe T, Matsui Y, Fukaya M, Sakagami H, Sato T, Funahashi JI, Ohnishi M, Tamura S, Kobayashi T.
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Journal Title
FEBS Lett.
Volume: 590
Pages: 3606-3615
Related Report
Peer Reviewed / Int'l Joint Research
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[Presentation] 卵巣切除マウスにおけるマルトビオン酸の骨密度改善効果2018
Author(s)
西尾彩花, 鵜飼容子, 山口青夏, 中川大, 渡辺章夫, 米澤貴之, 禹 済泰, 末廣大樹, 阿部秀飛, 深見健, 大西素子
Organizer
食品科学工学会第65回大会
Related Report
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[Presentation] Baccharin, Artepillin C, and Drupanin enhance adipocyte differentiation in 3T3-L1 cells2016
Author(s)
Je-Tae Woo, Yusuke Deguchi, Akio Watanabe, Jairo Kenupp Bastos, Maria Palmira Daflon Gremiao, Franciane Marquele de Oliveira, Andresa Aparecida Berretta, Byung-Yoon Cha, Takayuki Yonezawa
Organizer
Propolis Conference 2016
Place of Presentation
Glasgow, UK
Year and Date
2016-06-17
Related Report
Int'l Joint Research
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