A New Development of Molecular Design Utilizing Novel Hydrophobic Structures
| Project/Area Number |
26460151
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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 | Tohoku Medical and Pharmaceutical University |
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Principal Investigator |
ENDO Yasuyuki 東北医科薬科大学, 薬学部, 教授 (80126002)
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| Co-Investigator(Kenkyū-buntansha) |
猪股 浩平 東北医科薬科大学, 薬学部, 准教授 (60221785)
太田 公規 東北医科薬科大学, 薬学部, 講師 (90347906)
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| Co-Investigator(Renkei-kenkyūsha) |
TAN-NO Koichi 東北医科薬科大学, 薬学部, 教授 (20207260)
NAKAGAWASAI Osamu 東北医科薬科大学, 薬学部, 准教授 (50296018)
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| Project Period (FY) |
2014-04-01 – 2018-03-31
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| Project Status |
Completed (Fiscal Year 2017)
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| Budget Amount *help |
¥5,070,000 (Direct Cost: ¥3,900,000、Indirect Cost: ¥1,170,000)
Fiscal Year 2017: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
Fiscal Year 2016: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
Fiscal Year 2015: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2014: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
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| Keywords | 医薬分子設計 / 核内受容体 / エストロゲン受容体 / アンドロゲン受容体 / アゴニスト / アンタゴニスト / レチノイドX受容体 / i医薬分子設計 |
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| Outline of Final Research Achievements |
In this project, we focused design and synthesis of new estrogen receptor ligands and androgen receptor ligands utilizing a new hydrophobic structure such as boron cluster, carboranes. We have developed lead compounds for anti-osteoporosis drugs and anti-prostate cancer drugs which are effective for resistant cancer cells against conventional anticancer drugs. On the other hand, he present study has demonstrated that a new carborane compound BE360 has antidepressant and antidementia effects related by hippocampal cell proliferation. These results indicate that BE360 may have a valuable therapeutic potential against depression and neurodegenerative diseases such as AD.
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Report
(5 results)
Research Products
(48 results)
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[Journal Article] Structure-activity relations of rosmarinic acid derivatives for the amyloid beta aggregation inhibition and antioxidant properties2017
Author(s)
Taguchi Riho, Hatayama Koki, Takahashi Tomohito, Hayashi Takafumi, Sato Yuki, Sato Daisuke, Ohta Kiminori, Nakano Hiroto, Seki Chigusa, Endo Yasuyuki, Tokuraku Kiyotaka, Uwai Koji
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Journal Title
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume: 138
Pages: 1066-1075
DOI
Related Report
Peer Reviewed
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[Journal Article] BE360, a new selective estrogen receptor modulator, produces antidepressant and antidementia effects through the enhancement of hippocampal cell proliferation in olfactory bulbectomized mice.2016
Author(s)
Osamu Nakagawasai, Wataru Nemoto, Hiroshi Onogi, Takahiro Moriya, Jia-Rong Lin, Takayo Odaira, Fukie Yaoita, Takumi Ogawa, Kiminori Ohta, Yasuyuki Endo, Koichi Tan-No
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Journal Title
Behav Brain Res
Volume: 297
Pages: 315-322
DOI
Related Report
Peer Reviewed / Acknowledgement Compliant
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[Journal Article] BA321, a novel carborane analog that binds to androgen and estrogen receptors, acts as a new selective androgen receptor modulator of bone in male mice2016
Author(s)
Kenta Watanabe, Michiko Hirata Tsukasa Tominari, Chiho Matsumoto, Yasuyuki Endo, Gillian Murphy, Hideaki Nagase, Masaki Inada, Chisato Miyaura,
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Journal Title
Biochem. Biophys. Res. Commun.
Volume: 478
Issue: 1
Pages: 279-285
DOI
Related Report
Peer Reviewed
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[Presentation] Structural differences of the ligand binding pockets between estrogen receptor-alpha and beta2017
Author(s)
Koichi Kato, Kenichiro Fujii, Tomoki Nakayoshi, Yurie Watanabe, Shuichi Fukuyoshi, Kiminori Ohta, Yasuyuki Endo, Noriyuki Yamaotsu, Shuichi Hirono, Eiji Kurimoto, Akifumi Oda
Organizer
XXIX IUPAP Conference on Computational Physics, CCP20, Ｐａｒｉｓ17
Related Report
Int'l Joint Research
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