Multi-functionality and structure development of thalidomide
| Project/Area Number |
21790107
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| Research Category |
Grant-in-Aid for Young Scientists (B)
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| Allocation Type | Single-year Grants |
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| Research Field |
Drug development chemistry
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| Research Institution | The University of Tokyo |
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Principal Investigator |
YACHIDE Tomomi 東京大学, 分子細胞生物学研究所, 技術職員 (20401284)
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| Project Period (FY) |
2009 – 2012
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| Project Status |
Completed (Fiscal Year 2012)
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| Budget Amount *help |
¥5,200,000 (Direct Cost: ¥4,000,000、Indirect Cost: ¥1,200,000)
Fiscal Year 2012: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
Fiscal Year 2011: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2010: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2009: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
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| Keywords | ケミカルバイオロジー / サリドマイド / 構造展開 / 構造活性相関 / マルチテンプレート / 肝臓Ｘ受容体 / 核内受容体 / ヒダントイン誘導体 / ピューロマイシン感受性アミノペプチダーゼ / 肝臓X受容体 / エストロゲン受容体 / ペルオキシソーム増殖剤応答性受容体 / α-グルコシダーゼ / グリコーゲンホスホリラーゼ / 糖尿病 / 分化誘導 / チューブリン / シクロオキシゲナーゼ / 血管新生 |
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| Research Abstract |
I investigated the molecular mechanism of action of thalidomide andits metabolites, and cell signaling of biologically active derivatives of thalidomide. In addition, some biologically active compounds, such as nuclear receptor agonists/antagonists and enzyme inhibitors, have been created by structural development ofthalidomide and its derivatives. Based on these studies, I proved that thalidomide is usefulas a novel multi-template for development of various kinds of biologically activecompounds.
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Report
(4 results)
Research Products
(54 results)
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[Journal Article] Design, synthesis, and biological evaluation of novel transrepression-selective liver X receptor (LXR) ligands with 5,11-dihydro-5-methyl-11-methylene-6 Hdibenz[b,e]azepin-6-one skeleton.2012
Author(s)
Atsushi Aoyama, Kaori Endo-Umeda, Kenji Kishida, Kenji Ohgane, Tomomi Noguchi- Yachide, Hiroshi Aoyama, Minoru Ishikawa, Hiroyuki Miyachi, Makoto Makishima and Yuichi Hashimoto
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Journal Title
J. Med. Chem
Volume: 55
Pages: 7360-7377
Related Report
Peer Reviewed
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[Journal Article] Specific Inhibitors of Puromycin-Sensitive Aminopeptidase with a 3-(Halogenated Phenyl)-2,4(1H,3H)-quinazolinedione Skeleton2012
Author(s)
Matsumoto, Y., Noguchi-Yachide, T., Nakamura, M., Mita, Y., Numadate, A. and Hashimoto, Y.
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Journal Title
Heterocycles
Volume: 86
Issue: 2
Pages: 1449-1463
DOI
Related Report
Peer Reviewed
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