Stroke Drug Development Targeting Nrf2

Studies have shown that Nrf2 has many activities, including antioxidant, anti-inflammatory, modulation of heme, regulation of iron metabolism, and detoxification of xenobiotics. Some inducers of Nrf2 such as tert-butylhydroquinone, dimethyl fumarate, or activators such as sulforaphane have also been found to be effective in restoring the neuroprotective effects of ischemic stroke injury. Therefore, targeting Nrf2 for stroke drug development is a potential avenue for stroke treatment. In view of this, Ace Therapeutics offers excellent services to develop stroke drugs targeting Nrf2.

Screening of Nrf2 Modulator

The current studies suggest that the direction of targeting Nrf2 for stroke is mainly Nrf2 inducers and activators. Therefore, the main focus of Ace Therapeutics in developing stroke drugs for Nrf2 is on inducers and activators of Nrf2. Based on our ultra-large small molecule library and different drug screening platforms, we perform extensive screening of Nrf2 inducers and activators to improve the success rate of obtaining potential modulators.

• We provide high throughput screening against Nrf2 to rapidly obtain more potential modulators based on our ultra-large small molecule library, including compound libraries, natural product libraries, and fragment libraries.
• For potential modulators, we provide different in vitro stroke models with abnormal Nrf2 expression to initially validate the effect of potential modulators on stroke and also to screen drug candidates.
• We analyze the way drug candidates interact with Nrf2 at the subcellular level by high content imaging.

Preclinical Evaluation of Drug Candidates for the Treatment of Stroke

After confirming the activity of inducers and activators of Nrf2, along with preliminary validation to obtain drug candidates, for the drug candidates obtained from the screening, Ace Therapeutics conducts a more in-depth study to elucidate their specific mechanisms of action and efficacy in stroke treatment.

• We establish in vitro or in vivo models of Nrf2 expression abnormalities by means of drug modulation or genetic manipulation to validate the effect of drug candidates on Nrf2 and the mechanism of action of drug candidates.
• We provide different in vitro and in vivo stroke models to evaluate the effect of drug candidates on stroke.
• We screen Nrf2-associated genes or proteins during a stroke by gene microarray and protein microarray technologies to further elucidate the mechanism of action of Nrf2 modulators.
• For genes or proteins closely associated with Nrf2 during stroke pathology, we provide different qualitative, quantitative, and localization services to further explore the mechanisms by which candidate drugs exert their pharmacological effects.

At the same time, we can tailor our research services exclusively to your research needs. If you would like to learn more about our services, please feel free to contact us.

1. Farina, M., et al., The nrf2 pathway in ischemic stroke: A review. Molecules, 2021. 26(16).