| 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)
|
| 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 |
|---|
| 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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