Synthetic studies on ligand molecules
| Project/Area Number |
15K07421
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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 |
Bioorganic chemistry
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| Research Institution | Institute of Physical and Chemical Research |
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Principal Investigator |
Takahashi Shunya 国立研究開発法人理化学研究所, 環境資源科学研究センター, 専任研究員 (00202151)
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| Project Period (FY) |
2015-04-01 – 2018-03-31
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| Project Status |
Completed (Fiscal Year 2017)
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| Budget Amount *help |
¥4,940,000 (Direct Cost: ¥3,800,000、Indirect Cost: ¥1,140,000)
Fiscal Year 2017: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2016: ¥2,080,000 (Direct Cost: ¥1,600,000、Indirect Cost: ¥480,000)
Fiscal Year 2015: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
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| Keywords | 分子リガンド / 天然物合成 / 生理活性天然物 / 酵素阻害剤 / 細胞毒性物質 / 機能性分子リガンド / グリコシダーゼ阻害剤 / p-テルフェニル化合物 / プロリルオリゴペプチダーゼ / リガンド分子 / ジベンゾフラン骨格 / p-テルフェニル / ディ－ルズ・アルダー反応 / ４級炭素 / Suzuki-Miyauraカップリング |
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| Outline of Final Research Achievements |
A ligand molecule that binds to a target protein is expected to be a useful tool for clarifying a variety of biofunctions. Bioactive natural products have been utilized as a model for designing a novel ligand molecule. In this project, p-terphenyls, steroids, and sugars are selected as the models, and basic studies based on the natural product synthesis were performed. Efficient methods for the syntheses of bioactive p-terphenyls such as polyozellin and kehokorins A-E were developed, thus leading to the structural revision of polyozellin and studies of the structure-activity relationship. Bioassay of newly designed p-terphenyls carrying a biotinyl unit was also examined with the aim of searching the target. For preparation of a ligand molecule utilizing an anticancer steroid as a model, chemical reactions of androsterone were investigated. A novel branched sugar was designed as a glycosidase inhibitor and was synthesized from D-glucose.
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Report
(4 results)
Research Products
(10 results)
