NAD(P)H:quinone oxidoreductase-1 (NQO1) is attractive as a potential cancer biomarker because it is abnormally expressed in many solid tumors and is closely related to a variety of carcinogenic processes. Determining and evaluating the content/activity of NQO1 in tumors is of great significance for early cancer diagnosis and therapeutic effect evaluation. Enzyme-activated imaging probes with tailored properties, high selectivity and sensitivity, and high temporal and spatial resolution have become powerful tools for detecting and monitoring NQO1 activity. In this review, we aim to offer a rigorous but succinct overview of activatable imaging probes by reporting the significant progress made in accurately detecting and imaging NQO1 activity. The design strategies, mechanisms and applications of relevant probes are rationally analyzed and discussed. We also emphasized the potential challenges and prospects of NQO1-activated imaging probes to further advance the development of diagnosis and therapeutic methods for NQO1-related cancers.

NAD（P）H：醌氧化还原酶-1（NQO1）作为潜在的癌症生物标记物具有吸引力，因为它在许多实体瘤中异常表达，并且与多种致癌过程密切相关。确定和评估NQO1在肿瘤中的含量/活性对于早期癌症诊断和治疗效果评估具有重要意义。具有定制属性，高选择性和灵敏度以及高时间和空间分辨率的酶激活成像探针已成为检测和监视NQO1活性的强大工具。在这篇综述中，我们旨在通过报告在准确检测和成像NQO1活性方面取得的重大进展，来提供可激活的成像探针的严格但简洁的概述。对相关探针的设计策略，机理和应用进行了合理分析和讨论。