Development of steroid hormone receptor modulators and their clinical application
| Project/Area Number |
16K08318
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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 |
Drug development chemistry
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| Research Institution | Ochanomizu University |
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Principal Investigator |
Tanatani Aya お茶の水女子大学, 基幹研究院, 准教授 (40361654)
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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 |
¥4,810,000 (Direct Cost: ¥3,700,000、Indirect Cost: ¥1,110,000)
Fiscal Year 2018: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
Fiscal Year 2017: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
Fiscal Year 2016: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
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| Keywords | 核内受容体 / アンドロゲン / プロゲステロン / アンタゴニスト / ビタミンD / リトコール酸 / セコステロイド / ステロイドホルモン / アンドロゲンアンタゴニスト / プロゲステロンアンタゴニスト / 蛍光性リガンド |
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| Outline of Final Research Achievements |
Steroid hormones exhibit various biological functions. A number of steroid hormone derivatives have been synthesized for the purpose of their clinical application towards cancer, autoimmune diseases, metabolic diseases, neurodegenerative diseases and so on. In this study, novel steroid hormone derivatives with unique structures were designed, and synthesized, and their biological activities were examined. Compounds bearing the coumarin moiety elicited the specific inhibitors (antagonists) of androgen or progesterone, depending on the substituents. In these compounds, the conformational properties of amide or sulfonamide bonds on the coumarin ring were significant for the activity and hormone selectivity. Then, the potent derivatives of vitamin D3 were developed, by using lithocholic acid as a lead compound.
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| Academic Significance and Societal Importance of the Research Achievements |
ステロイドホルモンやビタミンDは、様々な疾病に対する特効薬として用いられているものの、その多様な生物活性の理解や制御ができていないため、医薬応用が限られている。本研究では、これまでのステロイドホルモンやビタミンD活性を有する化合物とは構造や物性の異なる化合物を設計、合成し、高い活性を持つ化合物を見いだした。例えば、アンドロゲン抑制剤（アンタゴニスト）は、前立腺癌の治療薬として、ビタミンD誘導体は、がん、骨疾患、自己免疫疾患、生活習慣病などの治療薬への応用が期待される。今後、本研究で得られた知見と化合物をもとに、医薬応用へと展開したいと考えている。
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Report
(4 results)
Research Products
(33 results)
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[Journal Article] Crystal Engineering of N, N’-Diphenylurea Compounds Featuring Phenyl-Perfluorophenyl Interaction2017
Author(s)
Yamasaki, R.; Iida, M.; Ito, A.; Fukuda, K.; Tanatani, A.; Kagechika, H., Masu, H. Okamoto, I.
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Journal Title
Crystal Growth&Design
Volume: 47
Issue: 11
Pages: 5858-5866
DOI
Related Report
Peer Reviewed
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