Nuclear Factor Erythroid 2-Related Factor 2 (Nrf2) Inhibition: An Emerging Strategy in Cancer Therapy.

J Med Chem

State Key Laboratory of Natural Medicines and Jiang Su Key Laboratory of Drug Design and Optimization , China Pharmaceutical University, Nanjing 210009 , China.

Published: April 2019


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Article Abstract

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.

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http://dx.doi.org/10.1021/acs.jmedchem.8b01121DOI Listing

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