2010 Fiscal Year Final Research Report
Anti-cancer drug design targeting a novel tertiary structure of ras oncogene product
| Project/Area Number |
20590280
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Single-year Grants |
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| Section | 一般 |
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| Research Field |
General medical chemistry
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| Research Institution | Kobe University |
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Principal Investigator |
SHIMA Fumi Kobe University, 大学院・医学研究科, 講師 (60335445)
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| Co-Investigator(Renkei-kenkyūsha) |
KUMASAKA Takashi 高輝度光科学研究センター, 利用研究促進部門, 副主席研究員 (30291066)
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| Project Period (FY) |
2008 – 2010
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| Keywords | インシリコ / 創薬 / rasがん遺伝子 / シグナル伝達 / がん / 低分子量G蛋白質 |
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| Research Abstract |
GTP-bound form of ras oncogene product Ras exhibits dynamic equilibrium between two interconverting conformations, "inactive" state 1 and "active" state 2. Based on a novel tertiary structure of Ras-GTP, we have performed in silico and in vitro screening for low molecular weight compounds which inhibit Ras function. Consequently, we have succeeded in identification of several hit compounds which specifically bind and inhibit Ras function in vitro and in vivo.
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Research Products
(14 results)
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[Journal Article] Critical Roles of Interactions Among Switch I-preceding Residues and Between Switch II and Its Neighboring・-helix on Conformational Dynamics of the GTP-bound Ras Family Small GTPases.2011
Author(s)
Matsumoto, K., Shima, F., Muraoka, S., Araki, M., Hu, L., Ijiri, Y., Hirai, R., Yoshioka, T., Kumasaka, T., Yamamoto, M., Tamura, A., Kataoka, T.
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Journal Title
J.Biol.Chem. 286(in press.)
Peer Reviewed
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[Journal Article] Structural basis for conformational dynamics of GTP-bound Ras protein.2010
Author(s)
Shima, F., Ijiri, Y., Muraoka, S., Liao, J., Ye, M., Araki, M., Matsumoto, K., Yamamoto, N., Sugimoto, T., Yoshikawa, Y., Kumasaka, T., Yamamoto, M., Tamura, A., Kataoka, T.
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Journal Title
J.Biol.Chem. 285(29)
Pages: 22696-22705
Peer Reviewed
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[Journal Article] Biochemical characterization of missense mutations in the Arf/Arl-family small GTPase Arl6 causing Bardet-Biedl syndrome.2009
Author(s)
Kobayashi, T., Hori, Y., Ueda, N., Kajiho, H., Muraoka, S., Shima, F., Kataoka, T., Kontani, K., Katada, T.
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Journal Title
Biochem Biophys Res Commun. 381(3)
Pages: 439-442
Peer Reviewed
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[Presentation] New strategy to develop Ras specific inhibitors(ポスター発表)2008
Author(s)
Moto Hiramatsu, Fumi Shima, Yoko Yoshikawa, Shin Muraoka, Satomi Kaizawa, Min Ye, Takeshi Sugimoto, Jingling Liao, Kousuke Matsumoto, Tohru Kataoka,
Organizer
第3回グローバルCOE研究討論会兼グローバルCOE第2回ワークショップ
Place of Presentation
神戸
Year and Date
20080700
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