ArticleBioorganic & medicinal chemistry2022
Targeting NLRP3 signaling by a novel-designed sulfonylurea compound for inhibition of microglial inflammation.
Article in Bioorganic & medicinal chemistry, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers, 1 of them a synthesis that pooled it.
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Who cites it
12 citing papers in PubMed, 1 synthesis or guideline pooled it, 24 citations in OpenAlex.
- Pre-clinical Studies Identifying Molecular Pathways of Neuroinflammation in Parkinson's Disease: A Systematic Review.Frontiers in aging neuroscience · 2022Pooled it
- Investigating antidiabetic drug targets as potential therapeutic modulators for schizophrenia.Psychopharmacology · 2026Article
- Development of highly potent EP2 antagonists as novel anti-inflammatory neuroprotectants.Bioorganic & medicinal chemistry · 2026Article
- Lead optimization of AMS-17 identifies AMS-4 as a modulator of inflammasome-driven cocaine-associated neuroinflammation.Biochemical and biophysical research communications · 2026Article
- A Novel NLRP3 Inhibitor AMS-17 Rescues Deficits in Long-Term Potentiation Following Mild Traumatic Brain Injury in Adult C57Bl/6 Mice.Hippocampus · 2026Article
- Association between antidiabetic drug targets and psychiatric disorders.Schizophrenia (Heidelberg, Germany) · 2025Article
- Targeting NLRP3 signaling with a novel sulfonylurea compound for the treatment of vascular cognitive impairment and dementia.Fluids and barriers of the CNS · 2025Article
- Increased inflammasome protein expression identified in microglia from postmortem brains with schizophrenia.Journal of neuropathology and experimental neurology · 2024Article
- Review on the role of nucleotide-binding oligomerization domain-like receptor protein 3 (NLRP3) inflammasome pathway in diabetes: mechanistic insights and therapeutic implications.Inflammopharmacology · 2024Review
- Review
- Abnormal expression of miR-3653-3p, caspase 1, IL-1β in peripheral blood of schizophrenia.BMC psychiatry · 2023Article
- Ablation of Siglec-E augments brain inflammation and ischemic injury.Journal of neuroinflammation · 2022Article
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Authors and funding
7 authors at 5 institutions in 1 country.
Funding
Abstract
The nucleotide-binding oligomerization domain (NOD)-like receptor protein 3 (NLRP3) inflammasome plays an important role in microglia-mediated inflammation. Dysregulation of NLRP3 signaling results in microglial activation and triggers inflammatory responses contributing to the development of neurological disorders including ischemic stroke, schizophrenia, Alzheimer's disease (AD), Parkinson's disease (PD), and amyotrophic lateral sclerosis (ALS). Inhibition of the NLRP3-linked inflammatory pathways reduces microglia-induced inflammation and is considered as a promising therapeutic approach for neuro-inflammatory diseases. In the present study, we report the development of AMS-17, a rationally-designed tertiary sulfonylurea compound for inhibition of inflammation in microglia. AMS-17 inhibited expression of the NLRP3, and its downstream components and cytokines such as caspase-1, tumor necrosis factor-α (TNF-α), IL-1β and inducible nitric oxide synthase (iNOS). It also suppressed lipopolysaccharide (LPS)-induced N9 microglial cell phagocytosis in vitro and activation of the microglia in mouse brain in vivo. Together, these results provide promising evidences for the inhibitory effects of AMS-17 in inflammation. This proof-of-concept study provides a new chemical scaffold, designed with the aid of pharmacophore modeling, with NLRP3 inhibitory activity which can be further developed for the treatment of inflammation-associated neurological disorders.
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