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Non-electrophilic modulators of the canonical Keap1/Nrf2 pathway.


ABSTRACT: 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.

SUBMITTER: Richardson BG 

PROVIDER: S-EPMC4643947 | biostudies-literature | 2015 Jun

REPOSITORIES: biostudies-literature

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Non-electrophilic modulators of the canonical Keap1/Nrf2 pathway.

Richardson B G BG   Jain A D AD   Speltz T E TE   Moore T W TW  

Bioorganic & medicinal chemistry letters 20150416 11


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  ...[more]

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