Protein Knockdown Approach : Hybrid Small Molecules which Induce Proteasome Degradation of Target Proteins
| Project/Area Number |
21651092
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| Research Category |
Grant-in-Aid for Challenging Exploratory Research
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| Allocation Type | Single-year Grants |
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| Research Field |
Living organism molecular science
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| Research Institution | The University of Tokyo |
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Principal Investigator |
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| Co-Investigator(Renkei-kenkyūsha) |
ISHIKAWA Minoru 東京大学, 分子細胞生物学研究所, 助教 (70526839)
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| Project Period (FY) |
2009 – 2011
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| Project Status |
Completed (Fiscal Year 2011)
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| Budget Amount *help |
¥3,170,000 (Direct Cost: ¥2,900,000、Indirect Cost: ¥270,000)
Fiscal Year 2011: ¥1,170,000 (Direct Cost: ¥900,000、Indirect Cost: ¥270,000)
Fiscal Year 2010: ¥1,300,000 (Direct Cost: ¥1,300,000)
Fiscal Year 2009: ¥700,000 (Direct Cost: ¥700,000)
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| Keywords | 生物活性分子の設計・合成 / タンパク質の自己分解 / ベスタチン / ユビキチン / タンパク質分解誘導 / cIAP1 / プロテアソーム / サリドマイド / 結合タンパク / ハイブリッド分子 / CRABP / レチノイン酸 / タンパク質分解 / プロテインノックダウン / CRABPD |
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| Research Abstract |
Protein knockdown can be achieved by the use of a small molecule that possesses affinity for both the target protein and ubiquitin ligase. As the ubiquitin ligase, we selected cIAP1 which specifically binds methylbestatin. Several hybrid molecules consisting of methylbestatin and a ligand for various proteins were designed and synthesized. These hybrid molecules induced selective decomposition of the target proteins.
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Report
(4 results)
Research Products
(27 results)
