| Project/Area Number |
16K19537
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| Research Category |
Grant-in-Aid for Young Scientists (B)
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| Allocation Type | Multi-year Fund |
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| Research Field |
Metabolomics
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| Research Institution | Kobe University |
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Principal Investigator |
Sugawara Kenji 神戸大学, 医学部附属病院, 医員 (70645217)
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| Project Period (FY) |
2016-04-01 – 2019-03-31
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| Project Status |
Completed (Fiscal Year 2018)
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| Budget Amount *help |
¥3,900,000 (Direct Cost: ¥3,000,000、Indirect Cost: ¥900,000)
Fiscal Year 2018: ¥1,170,000 (Direct Cost: ¥900,000、Indirect Cost: ¥270,000)
Fiscal Year 2017: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2016: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
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| Keywords | インスリン分泌 / ケミカルプロテオミクス / 糖尿病 |
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| Outline of Final Research Achievements |
Compound X identified by in silico search and phenotypic screening has a novel insulinotropic effect in a glucose-dependent manner in pancreatic β cells. In this study, we aimed to elucidate the novel mechanism of insulin secretion by chemical proteomic approach utilizing compound X.
First, according to the structure-activity relationship information on compound X, we synthesized a highly active derivative compound. This compound had an ester group which is chemically active. Therefore, it has been shown that this novel compound is useful for chemical modification. Then, we identified an appropriate linker with no effect on insulin secretion. Finally, compound X was added to linker and tag compound to successfully synthesize a chemical probe for chemical proteomic approach.
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| Academic Significance and Societal Importance of the Research Achievements |
本研究において、化合物XのSAR情報からデザイン・合成に成功したインスリン分泌増強作用を有する新規化合物は、グルコース濃度依存的かつ直接的に膵β細胞を刺激することから、2型糖尿病患者に対するより高い有効性を備える薬剤開発への展開を可能とする。さらに本研究で合成した化学プローブを用いたケミカルプロテオミクス解析により化合物Xの標的分子が同定可能となり、β細胞における新規インスリン分泌増強経路の解明に向けた応用研究の基盤となる。
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