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一个高度选择性的二光子光探测器用于人类细胞染色体P450 1A

Zi-Ru Dai¹, Guang-Bo Ge^1,2, Lei Feng^1,2

¹Dalian Institute of Chemical Physics, Chinese Academy of Sciences , Dalian 116023, China.

Journal of the American Chemical Society

|October 22, 2015

概括

研究人员开发了一种新的光探针NCMN,用于检测P450 1A (CYP1A) 酶活性. 这种探测器可以在生物系统和细胞成像中对CYP1A进行敏感,选择性和实时监测.

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 1A (CYP1A) 是一个关键的人类I阶段药物代谢酶,参与激活致癌物质.
准确检测和监测CYP1A活性对于了解致癌性和药物代谢至关重要.

研究的目的:

开发一种新型,选择性和敏感的光探测器来检测P450 1A (CYP1A) 的活性.
在复杂的生物系统中实现CYP1A的实时监测和生物成像.

主要方法:

基于1,8纳胺的二光子光探针 (NCMN) 的设计和合成.
使用人类CYP异型组的结构选择性关系探索.
验证NCMN用于活细胞和组织中的酶活性监测和双光子成像.

主要成果:

NCMN对CYP1A具有很高的选择性和敏感性,对CYP1A催化O- 脱甲基化有比度光反应.
该探测器成功地实时监测了生物系统中的CYP1A活性.
在活细胞和深层组织中,NCMN可实现细胞内CYP1A的高分辨率双光子成像.

结论:

一种新型的两光子激发式光探测器NCMN已被开发用于敏感和选择性检测CYP1A.
在内源性CYP1A的生物成像和研究其在生物功能中的作用方面,NCMN具有显著的前景.
该探针可以快速选CYP1A调节剂.

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