High throughput screening to identify small molecules inducing receptor internalization as potential aniticancer agents
| Project/Area Number |
26560441
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| Research Category |
Grant-in-Aid for Challenging Exploratory Research
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| Allocation Type | Multi-year Fund |
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| Research Field |
Chemical biology
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| Research Institution | The University of Tokyo |
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Principal Investigator |
Asanuma Daisuke 東京大学, 医学(系)研究科(研究院), 助教 (10611204)
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| Project Period (FY) |
2014-04-01 – 2016-03-31
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| Project Status |
Completed (Fiscal Year 2015)
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| Budget Amount *help |
¥3,770,000 (Direct Cost: ¥2,900,000、Indirect Cost: ¥870,000)
Fiscal Year 2015: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2014: ¥2,210,000 (Direct Cost: ¥1,700,000、Indirect Cost: ¥510,000)
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| Keywords | ハイスループットスクリーニングシステム / 受容体 / ダウンレギュレーション / 創薬科学 / がん / ハイスループットスクリーニング / HER2 / ヒト上皮成長因子受容体2 |
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| Outline of Final Research Achievements |
Enhanced expression of receptor tyrosine kinases in cancers, e.g., human epidermal growth factor receptor 2 (HER2) in ovarian and breast cancers, is associated with aggressiveness. Blockade of receptor signaling via induction of receptor internalization and degradation is a promising approach for cancer therapy. By employing a recently developed acidic-pH-activatable probe (Asanuma, D. et al., Angew. Chem. Int. Ed. Engl. 53, 6085-6089 (2014)), a cell-based high-throughput screening system was developed to identify molecules that induce HER2 internalization. From a ~155,000 small-molecule library, three hit compounds that induce internalization and degradation of HER2 were successfully identified.
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Report
(3 results)
Research Products
(8 results)
