| Project/Area Number |
23310148
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| Research Category |
Grant-in-Aid for Scientific Research (B)
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| Allocation Type | Single-year Grants |
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| Section | 一般 |
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| Research Field |
Living organism molecular science
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| Research Institution | University of Tsukuba |
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Principal Investigator |
KIGOSHI Hideo 筑波大学, 数理物質系, 教授 (90169839)
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| Co-Investigator(Kenkyū-buntansha) |
HAYAKAWA Ichiro 筑波大学, 数理物質系, 助教 (20375413)
KITA Masaki 筑波大学, 数理物質系, 准教授 (30335012)
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| Co-Investigator(Renkei-kenkyūsha) |
UESUGI Motonari 京都大学, 物質-細胞統合システム拠点, 教授 (10402926)
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| Project Period (FY) |
2011-11-18 – 2014-03-31
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| Project Status |
Completed (Fiscal Year 2013)
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| Budget Amount *help |
¥10,400,000 (Direct Cost: ¥8,000,000、Indirect Cost: ¥2,400,000)
Fiscal Year 2013: ¥5,200,000 (Direct Cost: ¥4,000,000、Indirect Cost: ¥1,200,000)
Fiscal Year 2012: ¥5,200,000 (Direct Cost: ¥4,000,000、Indirect Cost: ¥1,200,000)
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| Keywords | アプリロニンＡ / アクチン / チューブリン / 海洋天然物 / 三元複合体 / アポトーシス / ビセライドＡ / 全合成 / アプリロニンA / ハテルマライト / ビセライト / 脱重合 / ハテルマライド / ビセライド / アクチン関連タンパク質 / オーリライド / プロヒビチン / アリル酸化 |
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| Research Abstract |
The molecular mechanism of antitumor activity of aplyronine A, a marine macrolide, has been investigated. Using chemical probes aplyronine A was found to bind to actin and tubulin to form a ternary complex.
As a result, aplyronine A inhibits tubulin polymerization, induces irregular, multipolar spindle structures, inhibits cell-cycle progression in M-phase, and induces apoptosis.
Total synthesis of biselide A, a cytotoxic marine macrolide, was achieved by using Wittig reaction and sereoselective enzymatic hydrolysis of allylic alcohol as key steps.
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