Development of small molecules that stabilize i-motif DNA structures composed in the C-rich regions.
| Project/Area Number |
26560444
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| Research Category |
Grant-in-Aid for Challenging Exploratory Research
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| Allocation Type | Multi-year Fund |
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| Research Field |
Chemical biology
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| Research Institution | Tokyo University of Agriculture and Technology |
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Principal Investigator |
Nagasawa Kazuo 東京農工大学, 工学(系)研究科(研究院), 教授 (10247223)
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| Co-Investigator(Renkei-kenkyūsha) |
HIROKAWA Takatsugu 独立行政法人産業技術総合研究所, 創薬分子プロファイリング研究センター, 研究員 (20357867)
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| Project Period (FY) |
2014-04-01 – 2016-03-31
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| Project Status |
Completed (Fiscal Year 2015)
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| Budget Amount *help |
¥3,640,000 (Direct Cost: ¥2,800,000、Indirect Cost: ¥840,000)
Fiscal Year 2015: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
Fiscal Year 2014: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
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| Keywords | アイモチーフ / DNA高次構造 / リガンド / シトシン / インシリコ / グアニン四重鎖 / i-motif |
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| Outline of Final Research Achievements |
i-Motif is one of a non-B DNA structure, which is believed to construct in the C-rich regions in DNA. Since the no i-motif stabilizing compounds have been reported, no information about the function of i-motif has been obtained. In this research we aimed to develop i-mtoif selective interacting molecules, i.e., i-motif ligands.
Among our synthetic libraries together with the compounds suggested by the in silico docking studies, we started ca. forty compounds as candidates for i-motif ligands. With the evaluations by FRET melting analysis, CD spectra analysis, and EMAS experiments, we found the compound which selectively stabilize i-motifs derived from telomere, c-kit, c-myc and bcl-2, respectively. Stabilizing ability of the ligand is high, and delta Tm valu was obtained at 20 °C.
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Report
(3 results)
Research Products
(86 results)
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[Journal Article] Time-resolved crystal structures of the reaction intermediate of nitrile hydrase reveal a role for the cystein-sulfenic acid ligand as a catalyst nucleophile2015
Author(s)
Yasuaki Yamanaka, Yuki Kato, Koichi Hashimoto, Keisuke Iida, Kazuo Nagasawa, Hiroshi Nakayama, Naoshi Dohmae, Keiichi Noguchi, Takumi Noguchi, Masafumi Yohda, and Masafumi Odaka
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Journal Title
Angew. Chem., Int. Ed.
Volume: 54
Issue: 37
Pages: 10763-10767
DOI
Related Report
Peer Reviewed
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[Journal Article] Rif1 binds to G-quadruplexes and suppresses replication over long distances.2015
Author(s)
Yutaka Kanoh, Seiji Matsumoto, Rino Fukatsu, Naoko Kakusho, Nobuaki Kono, Claire Renard-Guillet, Koji Masuda, Keisuke Iida, Kazuo Nagasawa, Katsuhiko Shirahige, and *Hisao Masai
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Journal Title
Nature Struct. Mol. Biol.
Volume: 22
Issue: 11
Pages: 889-897
DOI
Related Report
Peer Reviewed / Open Access / Int'l Joint Research / Acknowledgement Compliant
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[Presentation] 貝毒サキシトキシン類の化学2015
Author(s)
長澤和夫
Organizer
第32回有機合成化学セミナー
Place of Presentation
ニューウェルシティ湯河原（静岡県・熱海市）
Year and Date
2015-09-15
Related Report
Invited
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[Presentation] パラウアミンの合成研究2015
Author(s)
岩田真、今岡拓哉、松尾浩喜、長澤和夫
Organizer
第69回有機合成化学協会関東支部シンポジウム
Place of Presentation
横浜国立大学（神奈川県・横浜市）
Year and Date
2015-05-16
Related Report
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