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Ligand-direct Radical Chemistry for Target Labelling in Living Cell

Ligand-direct Radical Chemistry for Target Labelling in Living Cell
用于活细胞中靶标标记的配体直接自由基化学
批准号:
20K15414
负责人:
茅 迪
金额:
$2.66万
依托单位:
依托单位国家:
日本
项目类别:
Grant-in-Aid for Early-Career Scientists
财政年份:
2020
资助国家:
日本
项目状态:
已结题
起止时间:
2020-04-01 至 2021-03-31

项目摘要

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中文摘要
翻译
为了达到研究目的,我们首先选择了著名的β受体靶向药物卡维地洛作为模型药物。卡维地洛具有高度的光敏性,但未观察到与β受体的反应。接下来选择另外两种光敏药物他莫昔芬和卡洛芬来验证假设。然而,没有观察到药物与其靶蛋白之间的光反应。结果表明,SQS的光降解机理可能是独特的。接下来,我们研究了由YM53601产生的自由基的类型。高活性羟基自由基的鉴定。羟基自由基与SQS降解的关系正在研究中。
英文摘要
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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