Studies on the interactions between ATR and its inhibitor Gomisin N and its application to a potentiator of antitumor agents.
Project/Area Number |
25293029
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Research Category |
Grant-in-Aid for Scientific Research (B)
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Allocation Type | Partial Multi-year Fund |
Section | 一般 |
Research Field |
Drug development chemistry
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Research Institution | Nigata University of Phermacy and Applied Life Sciences |
Principal Investigator |
Ishiguro Masaji 新潟薬科大学, 応用生物科学部, 教授 (10280687)
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Co-Investigator(Kenkyū-buntansha) |
NISHIDA Hiroshi 新潟薬科大学, 応用生物科学部, 教授 (60322541)
TAKAKU Hiroaki 新潟薬科大学, 応用生物科学部, 教授 (70350717)
TAMIYA Minoru 新潟薬科大学, 応用生物科学部, 助教 (10468960)
YAMAZAKI Harutake 新潟薬科大学, 応用生物科学部, 助教 (20456776)
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Project Period (FY) |
2013-04-01 – 2016-03-31
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Project Status |
Completed (Fiscal Year 2015)
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Budget Amount *help |
¥19,240,000 (Direct Cost: ¥14,800,000、Indirect Cost: ¥4,440,000)
Fiscal Year 2015: ¥4,550,000 (Direct Cost: ¥3,500,000、Indirect Cost: ¥1,050,000)
Fiscal Year 2014: ¥4,030,000 (Direct Cost: ¥3,100,000、Indirect Cost: ¥930,000)
Fiscal Year 2013: ¥10,660,000 (Direct Cost: ¥8,200,000、Indirect Cost: ¥2,460,000)
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Keywords | グミシンN / 五味子 / ATR / Phosphokinase / リグナン / 抗がん活性増強 / チェックポイント / ゴミシンN / ATR阻害 / 癌 / 生体分子 / 分子モデリング |
Outline of Final Research Achievements |
radioactive Gomisin N was prepared for examining the interaction site of Gomisin N in the binding at ATR. A binding mode of Gomisin N at the substrate-binding site of phosphokinase domain of ATR was examined by constructing the phosphokinase domain using a few crystal structures of phosphokinase-related proteins by homology modeling. Docking study of Gomisin N at the substrate binding site of of the domain suggested a characteristic site and new Gomisin-related new liganan derivatives were designed based on the interactions.
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Report
(4 results)
Research Products
(25 results)
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[Journal Article] Amino acid residues of bitter taste receptor TAS2R16 that determine sensitivity in primates to β-glycosides2016
Author(s)
Imai H, Suzuki-Hashido N, Ishimaru Y, Sakurai T, Yin W, Pan W, Ishiguro M, Masuda K, Abe K, Misaka T, and Hirai H.
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Journal Title
Biophysics and Physicobiology
Volume: in press
NAID
Related Report
Peer Reviewed / Acknowledgement Compliant
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[Presentation] ATR阻害剤ゴミシンNの全合成2014
Author(s)
田宮 実, 眞柄良平, 近 恵, 土屋裕徳, 熊倉美佳, 五十嵐久未, 中川悠貴, 石黒正路
Organizer
有機合成化学協会関東支部 新潟シンポジウム
Place of Presentation
新潟大学
Year and Date
2014-11-29
Related Report
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