期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 25, 期 11, 页码 2261-2268出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2015.04.019
关键词
Nrf2; Keap1; Cul3; Protein-protein interaction; Adaptive stress response; Nrf2/Keap1 interaction; Nrf2 activator; Nrf2 repressor
资金
- University of Illinois at Chicago College of Pharmacy
- T32 training grant - Office of the Director, National Institute of Health National Center for Complementary and Integrative Health
- University of Illinois Cancer Center
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. (C) 2015 Elsevier Ltd. All rights reserved.
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