2011 Fiscal Year Final Research Report
Development of antitumor agents targeting for prenoid-metabolizing enzymes
| Project/Area Number |
21790245
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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 |
General pharmacology
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| Research Institution | Gifu Pharmaceutical University |
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Principal Investigator |
ENDO Satoshi 岐阜薬科大学, 薬学部, 助教 (60433207)
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| Project Period (FY) |
2009 – 2011
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| Keywords | 酵素 |
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| Research Abstract |
Increment of prenylated small G proteins is a possible cause of abnormal growth and metastasis of carcinomas. Here, we found a novel metabolic pathway of prenoids and identified three human prenylaldehyde reductases as enzymes that involves the pathway. The enzymes highly express in a variety of carcinomas and have been suggested to be promoted to cancer cell proliferation. We succeeded development of the inhibitors that show potent and selective inhibitory effect against each enzymes by structure-based drug design. Moreover, the inhibitors significantly suppressed proliferation of cancer cells. Therefore, prenylaldehyde reductases are novel tumor-targeting molecules and their selective inhibitors are expected to be novel anticancer drugs.
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Research Products
(21 results)
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[Journal Article] Design, syn thesis and evaluation of caffeic ac id phenethyl ester-based inhibitors targeting a selectivity pocket in the active site of human aldo-keto reductase 1B102012
Author(s)
Midori Soda, Dawei Hu, Satoshi Endo, Mayuko Takemura, Jie Li, Ryogo Wa da, Syohei Ifuku, Hai-Tao Zhao, Oss ama El-Kabbani, Shozo Ohta, Keiko Y amamura, Naoki Toyooka, Akira Hara, and Toshiyuki Matsunaga
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Journal Title
Eur. J. Med. Chem.
Volume: 48
Pages: 321-329
DOI
Peer Reviewed
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[Journal Article] Kinetic studies of AKR1B10, human aldose reductase-like protein : Endogenous substrates and inhibition by steroids、Arch2009
Author(s)
Satoshi Endo, Toshiyuki Matsunaga, Hiroaki Mamiya, Chisato Ohta, Midori Soda, Yukio Kitade, Kazuo Tajima, Hai-Tao Zhao, Ossama El-Kabbani, Akira Hara
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Journal Title
Arch. Biochem. Biophys.
Volume: 487
Pages: 1-9
DOI
Peer Reviewed
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[Presentation] Design, Synthesis and Evaluation of Caffeic Acid Phenethyl Ester-Based Inhibitors Targeting a Selectivity Pocket in the Active Site of Human Aldo-Keto Reductase(AKR) 1B102011
Author(s)
Satoshi Endo, Toshiyuki Matsunaga, Midori Soda, Mayuko Takemura, Dawei Hu, Jie Li, Ryogo Wada, Syohei Ifuku, Naoki Toyooka, Hai-Tao Zhao, Ossama El-Kabbani and Akira
Organizer
8th AFMC International Medicinal Chemistry Symposium(AIMECS11)
Place of Presentation
東京
Year and Date
2011-11-30
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[Presentation] Roles of rat and human aldo-keto reductases in metabolism of farnesol and geranylgeraniol2010
Author(s)
Satoshi Endo, Toshiyuki Matsunaga, Chisato Ohta, Midori Soda, Ayano Kanamori, Yukio Kitade, Satoshi Ohno, Kazuo Tajima, Ossama El-Kabbani, Akira Hara
Organizer
ENZYMOLOGY AND MOLECULAR BIOLOGY OF CARBONYL METABOLISM FIFTEENTH INTERNATIONAL MEETING
Place of Presentation
LEXINGTON, KENTUCKY
Year and Date
20100709-10
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