Details

Autor(en) / Beteiligte

• Lin, Hongzhi
• Qiao, Yuting
• Yang, Hongyu
• Nan, Qin
• Qu, Wei
• Feng, Feng
• Liu, Wenyuan
• Chen, Yao
• Sun, Haopeng

Titel

Small molecular Nrf2 inhibitors as chemosensitizers for cancer therapy

Ist Teil von

• Future medicinal chemistry, 2020-02, Vol.12 (3), p.243-267

Ort / Verlag

England: Newlands Press Ltd

Erscheinungsjahr

2020

Beschreibungen/Notizen

• The basic leucine zipper transcription factor Nrf2 is the primary regulator of cellular oxidative stress. Activation of Nrf2 is regarded as a potential preventive and therapeutic strategy. However, aberrant hyperactivation of Nrf2 is found in a variety of cancers and promotes cancer progression and metastasis. Moreover, constitutive activation of Nrf2 confers cancer cells resistance to chemo- and radio-therapy. Thus, inhibiting Nrf2 could be a new therapeutic strategy for cancer. With the aim of accelerating the discovery and development of novel Nrf2 inhibitors, we summarize the biological and pathological functions of Nrf2 in cancer. Furthermore, the recent studies of small molecular Nrf2 inhibitors and potential Nrf2 inhibitory mechanisms are also summarized in this review.