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Induction of heme oxygenase I (HMOX1) by HPP-4382: a novel modulator of Bach1 activity.


ABSTRACT: Oxidative stress is generated by reactive oxygen species (ROS) produced in response to metabolic activity and environmental factors. Increased oxidative stress is associated with the pathophysiology of a broad spectrum of inflammatory diseases. Cellular response to excess ROS involves the induction of antioxidant response element (ARE) genes under control of the transcriptional activator Nrf2 and the transcriptional repressor Bach1. The development of synthetic small molecules that activate the protective anti-oxidant response network is of major therapeutic interest. Traditional small molecules targeting ARE-regulated gene activation (e.g., bardoxolone, dimethyl fumarate) function by alkylating numerous proteins including Keap1, the controlling protein of Nrf2. An alternative is to target

SUBMITTER: Attucks OC 

PROVIDER: S-EPMC4096395 | biostudies-literature | 2014

REPOSITORIES: biostudies-literature