Richardson B G, Jain A D, Speltz T E, Moore T W
Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, 833 S. Wood St., Chicago, IL 60612, United States.
Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, 833 S. Wood St., Chicago, IL 60612, United States; University of Illinois Cancer Center, University of Illinois at Chicago, 833 S. Wood St., Chicago, IL 60612, United States.
Bioorg Med Chem Lett. 2015 Jun 1;25(11):2261-8. doi: 10.1016/j.bmcl.2015.04.019. Epub 2015 Apr 16.
Nrf2 is the major transcription factor that regulates many of the cytoprotective enzymes involved in the adaptive stress response. Modulation of Nrf2 could be therapeutically useful in a number of disease states. Activation can occur through either an electrophilic or non-electrophilic mechanism. To date, most of the research has focused on electrophilic Nrf2 activators, but there is increasing interest in non-electrophilic modulators of Nrf2. This Digest examines the current selection of small molecules that modulate Nrf2 through non-electrophilic mechanisms, and it highlights new opportunities for this important therapeutic target.
Nrf2是调节许多参与适应性应激反应的细胞保护酶的主要转录因子。Nrf2的调节在多种疾病状态下可能具有治疗作用。其激活可通过亲电或非亲电机制发生。迄今为止，大多数研究都集中在亲电Nrf2激活剂上，但人们对Nrf2的非亲电调节剂的兴趣与日俱增。本综述探讨了目前通过非亲电机制调节Nrf2的小分子的选择，并突出了这一重要治疗靶点的新机遇。
