State Key Laboratory of Natural Medicines and Jiang Su Key Laboratory of Drug Design and Optimization , China Pharmaceutical University , Nanjing 210009 , China.
Department of Medicinal Chemistry, School of Pharmacy , China Pharmaceutical University , Nanjing 210009 , China.
J Med Chem. 2019 Apr 25;62(8):3840-3856. doi: 10.1021/acs.jmedchem.8b01121. Epub 2018 Nov 28.
Nuclear factor erythroid 2-related factor 2 (Nrf2) is a pleiotropic transcription factor, especially for its complex and dual effects in cancer. With the continuous growing research, new regulatory modes and new functions of Nrf2 and tumor-promoting effects of Nrf2 in malignant transformed tumors have become increasingly clear. Accumulating evidence has established that Nrf2 contributes to the whole process of pathogenesis, progression, metastasis, and prognosis of cancer, and Nrf2 could be a promising target in cancer therapy. However, the development of Nrf2 inhibitor is still limited. In this perspective, we will briefly describe the biological function and modulating network of Nrf2, stress its oncogenic role, and point out possible ways to inhibit Nrf2, as well as summarize the reported Nrf2 inhibitors.
核因子红细胞 2 相关因子 2（Nrf2）是一种多效转录因子，特别是在癌症中具有复杂的双重作用。随着研究的不断深入，Nrf2 的新调节模式和新功能以及 Nrf2 在恶性转化肿瘤中的促肿瘤作用变得越来越清楚。越来越多的证据表明，Nrf2 参与了癌症发病机制、进展、转移和预后的全过程，Nrf2 可能是癌症治疗的一个有前途的靶点。然而，Nrf2 抑制剂的发展仍然受到限制。在这篇观点文章中，我们将简要描述 Nrf2 的生物学功能和调节网络，强调其致癌作用，并指出可能的抑制 Nrf2 的方法，同时总结报道的 Nrf2 抑制剂。
