在活细胞中进行快速生物对等蛋白标记的绝缘屏蔽稳定胺
Peng An1, Tracey M Lewandowski1, Tuğçe G Erbay2
1Department of Chemistry , State University of New York at Buffalo , Buffalo , New York 14260-3000 , United States.
Journal of the American Chemical Society
|March 23, 2018
概括
研究人员开发了一种生物启发的策略,使用分子形状来控制活性胺 (NI) 二极体的选择性. 这种方法增强了生物系统的反应性而不会影响选择性.
科学领域:
- 有机生物化学
- 化学生物学
- 分子成像
背景情况:
- 生物对角反应对于生物分子选择性标记至关重要.
- 在这些反应中实现高反应性与选择性仍然是一个重大挑战.
- 过渡性,高反应性物种,如化物,具有潜力,但需要控制的选择性.
研究的目的:
- 开发一种生物启发的策略来控制反应性胺二极体的选择性.
- 通过调整它们的反应性和稳定性来增强烯胺在生物对应标签中的效用.
- 在活细胞成像中展示一种新胺的应用.
主要方法:
- 在N-aryl环的正确位置上有可调节的结构.
- 使用1,3-双极循环添加与核友添加对光生成胺的选择性进行了研究.
- 使用密度函数理论 (DFT) 计算来理解分子形状在选择性中的作用.
- 在水性介质中评估了胺的稳定性 (半衰期).
- 在活哺乳动物细胞中证明了葡萄糖受体的生物对角标记.
主要成果:
- 发现调整结构吊的形状会产生一种绝缘屏蔽的化物.
- 屏蔽胺选择性地支持1,3-双极循环添加而不是核友添加.
- 在水溶液中获得102秒的异常长半衰期.
- 成功进行快速 (约. 在活哺乳动物细胞中对葡萄糖受体进行生物对应标记.
结论:
- 分子形状是一个强大的工具来控制短暂的反应性二极体,如化物.
- 开发的绝缘屏蔽胺为生物对角应用提供了增强的稳定性和选择性.
- 这一策略使得活细胞中的生物分子能够得到高效和快速的标记,进步了化学生物学工具.
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