Abstract:

Enzyme plays an extremely important role in maintaining homeostasis and the normal life activities in biological systems.The abnormality of some particular enzymes activity is closely relevant to the occurrence and development of related diseases.Therefore, it is of great significance to detect and visualize specific enzyme in vivo with an in-situ and real-time method.The chemical fluorescent probes are endowed with the obvious advantages such as good selectivity, high sensitivity, high imaging resolution and so forth.In recent years, researchers have designed and synthesized a series of fluorescent probes for enzyme detection and visualized imaging in living systems.Based on the trigger mode of fluorescence response, the enzymatic fluorescent probes can be generally divided into two categories:(1) probes based on the recognition between enzyme and specific groups of its inhibitor existing in the probes, called inhibitor-based enzymatic fluorescent probes and(2) probes based on the effective catalytic ability of specific enzyme, also known as the reaction-activated enzymatic fluorescent probes.Herein, in this review, the design strategies of reaction-activated fluorescent probe for enzymes and the research progress of reaction-activated fluorescent probes for four important disease-related enzymes(monoamine oxidase, β-galactosidase, nitroreductase, γ-gumatyl transpeptidase) were mainly reviewed, and the future research of fluorescent probes for enzymes was prospected.

Key words: fluorescence, probes, enzyme, imaging, cell biology

摘要：

酶在维持生物体内稳态与生命活动的正常运行方面发挥着举足轻重的作用。某些特定酶含量及活性的异常与人类重大疾病的发生与发展密切相关。因此，生物体内特定酶的实时原位检测及可视化成像具有重要的意义。化学荧光探针具有选择性好、灵敏度高及高时空分辨率可视化成像等优点，近年来研究者设计合成了大量的可用于生物体系内酶识别与可视化成像的荧光探针。目前识别酶的荧光探针主要有两类：（1）基于酶对荧光探针分子中酶抑制剂基团的识别引起探针荧光信号的变化；（2）基于酶对荧光探针特异性催化反应来实现识别前后荧光信号的激活，称为反应激活型酶荧光探针。对反应激活型酶荧光探针的设计策略及4种重大疾病相关的生物标志酶（单胺氧化酶、β-半乳糖苷酶、硝基还原酶、γ-谷氨酰转肽酶）的识别可视化荧光探针研究进展进行了综述，对未来酶识别荧光探针的研究方向进行了展望。

关键词: 荧光, 探针, 酶, 成像, 细胞生物学