2020 Fiscal Year Annual Research Report
Ligand-direct Radical Chemistry for Target Labelling in Living Cell
Project/Area Number |
20K15414
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Research Institution | University of the Ryukyus |
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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Keywords | Radical Chemistry / medicinal chemistry / chemical biology |
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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