Non-electrophilic modulators of the canonical Keap1/Nrf2 pathway
journal contribution
posted on 2016-09-10, 00:00 authored by BG Richardson, AD Jain, TE Speltz, TW MooreNrf2 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.
Funding
The authors thank the University of Illinois at Chicago College of Pharmacy and the University of Illinois Cancer Center for their support of this work. T.E.S. was supported by a T32 training grant funded by the Office of the Director, National Institute of Health National Center for Complementary and Integrative Health.
History
Publisher Statement
This is the author’s version of a work that was accepted for publication in Bioorganic and Medicinal Chemistry Letters. Changes resulting from the publishing process, such as peer review, editing, corrections, structural formatting, and other quality control mechanisms may not be reflected in this document. Changes may have been made to this work since it was submitted for publication. A definitive version was subsequently published in Bioorganic and Medicinal Chemistry Letters. 2015. 25(11): 2261-2268. DOI: 10.1016/j.bmcl.2015.04.019.Publisher
Elsevier Inc.issn
0960-894XIssue date
2015-06-01Usage metrics
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