构建近红外光探测器的分子设计策略,用于选择性地检测人类细胞染色体P450 2J2
Jing Ning1,2, Tao Liu2, Peipei Dong1
1College of Integrative Medicine, The National & Local Joint Engineering Research Center for Drug Development of Neurodegenerative Disease, College of Pharmacy , Dalian Medical University , Dalian 116044 , China.
Journal of the American Chemical Society
|December 12, 2018
概括
研究人员开发了一种新的光探针BnXPI,用于实时监测P450 2J2 (CYP2J2) 酶活性. 这种工具可以提高对CYP2J2的理解.
科学领域:
- 生物化学
- 分子生物学
- 化学生物学
背景情况:
- 细胞染色体P450 2J2 (CYP2J2) 对于代谢异生菌和内生化合物至关重要,影响各种生理和病理过程.
- 由于缺乏实时监测工具,对CYP2J2在瘤发生和癌症诊断中的作用尚不清楚.
研究的目的:
- 开发一种用于实时监测生物系统中的CYP2J2活性的分子工具.
- 研究CYP2J2在瘤发生中的生物功能.
主要方法:
- 使用近红外光器创建了一个CYP2J2选择性光探针 (HXPI).
- 在HXPI衍生物中加入了一种自燃链接剂,以增强CYP2J2狭窄基质通道的反应性和特异性.
- 在查后,BnXPI是一种O-基化HXPI衍生物被确定为最佳探针.
主要成果:
- 在体外和体内检测CYP2J2时,BnXPI具有很高的特异性,敏感性和适用性.
- 通过CYP2J2进行O- 脱甲基化后,BnXPI会发生自燃反应,释放HXPI,从而实现实时光监测.
- BnXPI成功监测了生物系统中的CYP2J2活性,包括细胞,瘤组织和瘤动物.
结论:
- 为开发高度具体且广泛适用的CYP2J2监测工具制定了一项实用策略.
- BnXPI为探索CYP2J2在瘤形成和癌症诊断中的生物功能提供了一个有前途的工具.
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