Nuclear Factor Erythroid 2-Related Factor 2 (Nrf2) Inhibition: An Emerging Strategy in Cancer Therapy
Nuclear Factor Erythroid 2-Related Factor 2 (Nrf2) Inhibition: An Emerging Strategy in Cancer Therapy
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核因子红细胞 2 相关因子 2 (Nrf2) 抑制：癌症治疗的新兴策略
DOI：
10.1021/acs.jmedchem.8b01121
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发表时间：
2019
影响因子：
7.3
通讯作者：
You Qi-Dong
中科院分区：
文献类型：
--
作者：
Jiang Zheng-Yu;Lu Meng-Chen;You Qi-Dong
核因子红细胞2相关因子2（Nrf2）是一种多效性转录因子，尤其是其在癌症中的复杂和双重作用。随着研究的不断深入，Nrf2新的调控模式、新的功能以及Nrf2在恶性转化肿瘤中的促肿瘤作用日益清晰。越来越多的证据表明，Nrf2参与了肿瘤的发生、发展、转移和预后的全过程，Nrf2有望成为肿瘤治疗的一个新靶点。然而，Nrf2抑制剂的开发仍然受到限制。本文将简要介绍Nrf2的生物学功能和调控网络，强调其致癌作用，指出抑制Nrf2的可能途径，并对已报道的Nrf2抑制剂进行综述。
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.