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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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Richardson BG,Jain AD,Speltz TE,Moore TW

doi

10.1016/j.bmcl.2015.04.019

subject

Has Abstract

pub_date

2015-06-01 00:00:00

pages

2261-8

issue

11

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(15)00330-3

journal_volume

25

pub_type

杂志文章,评审

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