Non-electrophilic modulators of the canonical Keap1/Nrf2 pathway

作者：Richardson B G; Jain A D; Speltz T E; Moore T W^*

来源：Bioorganic & Medicinal Chemistry Letters, 2015, 25(11): 2261-2268.

DOI：10.1016/j.bmcl.2015.04.019

• Nrf2
• Keap1
• Cul3
• Protein-protein interaction
• Adaptive stress response
• Nrf2/Keap1 interaction
• Nrf2 activator
• Nrf2 repressor

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.

• 出版日期2015-6-1