NAD(P)H:quinone oxidoreductase 1 (NQO1) is a two-electron reductase responsible for detoxification of quinones and also bioactivation of certain quinones. It is abnormally overexpressed in many tumors and intimately linked with multiple carcinogenic processes. NQO1 is considered to be a cancer-specific target for therapy but currently available NQO1 inhibitors have not yet led to chemotherapeutic success. Utilization of NOQ1’s ability to bioactivate chemotherapeutic quinones, however, has emerged as a promising selective anticancer therapy. On the basis of the different levels of NQO1 between cancer and normal cells, the catalytic property of NQO1 has recently been exploited to develop effective probes for cancer detection. This article summarizes the most significant advances concerning the discovery and development of NQO1 inhibitors, NQO1-directed chemotherapeutic quinones, and NQO1-activated optical probes, along with the prospects and potential obstacles in this research area.

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NAD（P）H：奎宁氧化还原酶1（NQO1）作为癌症的治疗和诊断目标

NAD（P）H：醌氧化还原酶1（NQO1）是一种双电子还原酶，负责醌的解毒以及某些醌的生物活化。它在许多肿瘤中异常过表达，并与多种致癌过程密切相关。NQO1被认为是治疗癌症的特异性靶标，但是目前可用的NQO1抑制剂尚未导致化学疗法的成功。然而，利用NOQ1生物活化化学治疗醌的能力已成为一种有前途的选择性抗癌疗法。基于癌症和正常细胞之间不同水平的NQO1，最近已利用NQO1的催化特性来开发用于癌症检测的有效探针。本文总结了有关NQO1抑制剂的发现和开发的最重要进展，