| Project/Area Number |
20K15414
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| Research Category |
Grant-in-Aid for Early-Career Scientists
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| Allocation Type | Multi-year Fund |
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| Review Section |
Basic Section 37030:Chemical biology-related
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| Research Institution | University of the Ryukyus |
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Principal Investigator |
茅 迪 琉球大学, 理学部, 博士研究員 (60849058)
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| Project Period (FY) |
2020-04-01 – 2021-03-31
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| Project Status |
Discontinued (Fiscal Year 2020)
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| Budget Amount *help |
¥4,160,000 (Direct Cost: ¥3,200,000、Indirect Cost: ¥960,000)
Fiscal Year 2021: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2020: ¥2,600,000 (Direct Cost: ¥2,000,000、Indirect Cost: ¥600,000)
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| Keywords | Radical Chemistry / medicinal chemistry / chemical biology / Protein / Small molecule / Target engagement |
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| Outline of Research at the Start |
A new target protein labelling approach based on the radical chemistry will be developed to detect the engagement between bioactive molecules and their protein targets directly in living cells. Applying radical chemistry on target labelling in living cell may open a new gate for future study.
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| Outline of Annual Research Achievements |
To achieve the research goal, we firstly selected Carvedilol, a famous drug targeting on beta-receptor, as a model. Although Carvedilol was highly photo sensitive, its reaction with beta-receptor was not observed. Tamoxifen and Carprofen, the other two photo sensitive drugs, were next selected to validate the hypothesis. However, no photo reaction was observed between the drugs and their target proteins. The results suggested that the mechanism of photo-induced degradation of SQS might be unique. We next investigated the types of radicals that generated by YM53601. Highly reactive hydroxyl radical was indentified. The relationship between hydroxyl radical and SQS degradation are now under investigation.
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