4.7 Article

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

Journal

JOURNAL OF MEDICINAL CHEMISTRY
Volume 62, Issue 8, Pages 3840-3856

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.8b01121

Keywords

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Funding

  1. National Natural Science Foundation of China [81602948, 81773581, 81773639, 81803363]
  2. Natural Science Foundation of Jiangsu Province of China [BK20160746]
  3. China Postdoctoral Science Foundation [1600010006, 2018T110576]
  4. National Major Science and Technology Project of China (Innovation and Development of New Drugs) [2015ZX09101032, 2017ZX09302003]
  5. Priority Academic Program Development of Jiangsu Higher Education Institutions
  6. Program for Outstanding Scientific and Technological Innovation Team of Jiangsu Higher Education [YY20180315004]
  7. 111 Project [B16046]
  8. Double First-Class University Project [CPU2018GY02]

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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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