Activatable imaging probes for cancer-linked NAD(P)H:quinone oxidoreductase-1 (NQO1): Advances and future prospects

Abstract 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.