Stroke Drug Development Targeting Microglia

Activation of microglia is the first step in the inflammatory response in the brain. It can be activated rapidly within minutes of the onset of an ischemic stroke. Activated microglia can produce a variety of mediators, including iNOS, nitric oxide, inflammatory factors, anti-inflammatory cytokines, and growth and trophic factors. Moderate activation facilitates recovery of brain function, whereas excessive activation hinders brain repair. Microglia activation inhibitors have demonstrated promising results in stroke treatment. Therefore, Ace Therapeutics offers comprehensive services to accelerate the development of your stroke drug targeting microglia.

Target Identification & Validation

Studies have shown that microglia activation and polarization can regulate immune processes, neurotransmitters, neuropeptides, metabolite activation, and many other pathways during stroke. Currently targeting microglia activation, the TLR4 pathway and other pathways have shown potential therapeutic effects in stroke. Therefore, Ace Therapeutics provides target identification and validation services for targeting microglia to discover more targets for stroke treatment.

• We have established microglia and experimental animal models of stroke injury to screen and validate candidate targets.
• We offer gene ontology enrichment analysis and KEGG enrichment analysis to screen for candidate targets.
• We establish in vitro and in vivo stroke models by drug administration and genetic manipulation to explore the effects of candidate targets on stroke.
• We determine the activity and mechanism of action of candidate targets by fluorescein reporter system, RNA pull-down, RIP-PCR, gel migration, or electrophoretic migration assays.

High Throughput Screening of Microglia Modulators

Because of the different phenotypes and multiple modes of action of microglia in stroke, the types of microglia targets used to treat stroke are equally complex. Given the complexity of the targets, Ace Therapeutics offers a comprehensive and flexible service to screen drug candidates against the targets.

• We have established different screening platforms, including high-throughput screening platforms and virtual screening platforms targeted screening against targets and known potential drugs.
• To address the different roles of microglia in stroke, we set up in vitro and in vivo models of microglia activation and polarization in different ways to validate the effects of modulators on microglia in pathological states.

Preclinical Evaluation of Drug Candidates for the Treatment of Stroke

We have validated the effects of modulators on microglia. Immediately afterward, we offer various pharmacological activity assessment services to study the therapeutic effects of microglia modulators on stroke, while exploring their specific mechanisms of action and drug metabolism.

• We offer different in vitro and in vivo stroke models to validate the therapeutic effect of microglia modulators on stroke and further explore the mechanism of action of astrocytes.
• We investigate the effects of microglia modulators on microglia-related signaling pathways through molecular co-expression correlations, molecular interactions, molecular localization, activity, and conformational assays.

If you would like to learn more about our services, please feel free to contact us.

1. Zhao, S. C., et al., Regulation of microglial activation in stroke. Acta Pharmacol Sin, 2017. 38(4): p. 445-458.
2. Yenari, M. A., et al., Microglial activation in stroke: Therapeutic targets. Neurotherapeutics, 2010. 7(4): p. 378-391.