Non-electrophilic modulators of the canonical Keap1/Nrf2 pathway

[Display omitted] 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-electroph...

Full description

Saved in:
Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2015-06, Vol.25 (11), p.2261-2268
Main Authors: Richardson, B.G., Jain, A.D., Speltz, T.E., Moore, T.W.
Format: Article
Language:English
Subjects:
Adaptive stress response
Cul3
Humans
Intracellular Signaling Peptides and Proteins - genetics
Intracellular Signaling Peptides and Proteins - metabolism
Keap1
Kelch-Like ECH-Associated Protein 1
Models, Molecular
NF-E2-Related Factor 2 - agonists
NF-E2-Related Factor 2 - genetics
NF-E2-Related Factor 2 - metabolism
Nrf2
Nrf2 activator
Nrf2 repressor
Nrf2/Keap1 interaction
Protein Binding
Protein Conformation
Protein–protein interaction
Signal Transduction - drug effects
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:[Display omitted] 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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2015.04.019