Rational Design of a Two-Photon Fluorescent Probe for Human Cytochrome P450 3A and the Visualization of Mechanism-Based Inactivation,Angewandte Chemie International Edition

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Rational Design of a Two-Photon Fluorescent Probe for Human Cytochrome P450 3A and the Visualization of Mechanism-Based Inactivation
Angewandte Chemie International Edition ( IF 16.1 ) Pub Date : 2021-12-01 , DOI: 10.1002/anie.202113191
Jing Ning _{1,

2} , Zhenhao Tian ₃ , Jiayue Wang _{2,

4} , Bo Wang ₅ , Xiangge Tian ₂ , Zhenlong Yu ₂ , Xiaokui Huo ₂ , Lei Feng _{1,

6} , Jingnan Cui ₇ , Tony D James _{6,

8} , Xiaochi Ma _{1,

2}

Affiliation

A two-photon fluorescent probe for CYP3A was developed using a rational design strategy that optimized the key binding domain of the fluorophore. The probe semi-quantitatively detects and images CYP3A activity in various living systems, thereby providing a high-throughput screening system facilitating the evaluation of MBI-associated hepatotoxicity by CYP3A.

中文翻译：

人细胞色素 P450 3A 双光子荧光探针的合理设计和基于机制的失活的可视化

使用合理的设计策略开发了 CYP3A 的双光子荧光探针，优化了荧光团的关键结合域。该探针半定量检测和成像各种生命系统中的 CYP3A 活性，从而提供高通量筛选系统，促进评估 CYP3A 与 MBI 相关的肝毒性。

更新日期：2022-01-19

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