Chenical biology research using diketopiperazine-based anti-microtubule agent.
| Project/Area Number |
21790118
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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 | Tokyo University of Pharmacy and Life Science |
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Principal Investigator |
YAMAZAKI Yuri Tokyo University of Pharmacy and Life Science, 薬学部, 助手 (70459725)
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| Project Period (FY) |
2009 – 2010
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| Project Status |
Completed (Fiscal Year 2010)
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| Budget Amount *help |
¥4,160,000 (Direct Cost: ¥3,200,000、Indirect Cost: ¥960,000)
Fiscal Year 2010: ¥1,950,000 (Direct Cost: ¥1,500,000、Indirect Cost: ¥450,000)
Fiscal Year 2009: ¥2,210,000 (Direct Cost: ¥1,700,000、Indirect Cost: ¥510,000)
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| Keywords | 分子認識 / 医薬品化学 / 癌 / 生体分子 / 薬学 / チューブリン |
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| Research Abstract |
In order to understand the precise binding site of diketopiperadine-based anti-microtubule agent 'plinabulin' on tubulin, we designed and synthesized biotin-tagged plinabulin derivatives as chemical probes. Since these derivatives all showed a significant binding ability to tubulin and cytotoxicity, we performed tubulin photoaffinity labeling study. These results suggested that plinabulin derivatives may bind at the boundary region formed between the α-and β-tubulin subunits around the colchicine binding site, but not inside the site, to effectively disrupt the interaction between the two tubulin subunits, thereby producing microtubule depolymerization.
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Report
(3 results)
Research Products
(35 results)
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[Presentation] Plinabulin' a diketopiperazine-type vascular targeting anti-cancer agent based on microtubule depolymerization activity.2010
Author(s)
Yoshio Hayashi, Yuri Yamazaki, Makiko Sumikura, Tomoko Yoshida, Yuki Mori, Hiroyuki Yasui, Kyoko Kohno, Yoshiaki Kiso, Saskia Neuteboom, Barbara Potts, G.Kenneth Lloyd
Organizer
ACS Spring 2010 National Meeting & Exposition
Place of Presentation
San Francisco, USA
Related Report
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[Presentation] Plinabulin" a cyclic dipeptide-based vascular targeting anti-cancer agent based on microtubule depolymerization activity.2009
Author(s)
Yoshio Hayashi, Yuri Yamazaki, Makiko Sumikura, Tomoko Yoshida, Yuki Mori, Hiroyuki Yasui, Kyoko Kohno, Yoshiaki Kiso, Saskia Neuteboom, Barbara Potts, G.Kenneth Lloyd
Organizer
3rd Asia-Pacific International Peptide Symposium/13th Korean Peptide and Protein Symposium
Place of Presentation
Jeju Island, Korea
Related Report
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[Presentation] Cyclic dipeptide-based microtubule depolymerization agents as vascular targeting anti-cancer drugs2009
Author(s)
Yuri Yamazaki, Makiko Sumikura, Tomoko Yoshida, Yuki Mori, Hiroyuki Yasui, Kyoko Kohno, Yoshiaki Kiso, Gordafaried Deyanat-Yazdi, Saskia Neuteboom, Barbara Potts, G.Kenneth Lloyd, Yoshio Hayashi
Place of Presentation
Chains, Australia
Related Report
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