ArticleJournal of medicinal chemistry2025
Mechanistic Characterization of a Small Molecule as a Direct NLRP3 Inhibitor via Binding to the NACHT Domain.
Article in Journal of medicinal chemistry, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.
What it found
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The trial behind it
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Who cites it
2 citing papers in PubMed.
- Discovery of a brain penetrant NLRP3 inflammasome inhibitor that reduces neuropathic pain in mice.European journal of medicinal chemistry · 2026Article
- Targeting the Crosstalk Between Metabolism and Chronic Inflammation: In Silico Multitargeting Drug Design Approach for Cardiometabolic Syndrome.Biomedicines · 2026Article
Corrections and comments
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Authors and funding
7 authors.
Funding
Abstract
The NLRP3 inflammasome has recently emerged as a viable drug target, and small-molecule inhibitors of this protein complex are being actively tested in preclinical disease models. However, the mechanisms of action for the majority of these compounds remain unclear. Our recent medicinal chemistry campaign led to the discovery of several potent lead NLRP3 inhibitors from a distinct chemical scaffold. Herein, further characterization using biophysical, biochemical, chemical biology, and molecular biology approaches of one of the lead inhibitors revealed direct binding to the NACHT domain of the NLRP3 protein. The studies also suggested potentially multiple binding sites within the NACHT domain that can be targeted by different small-molecule inhibitors. Furthermore, an activity-based probe with high labeling efficacy was developed and can serve as a valuable tool to contribute to ongoing efforts in understanding NLRP3 biology and in developing NLRP3-targeted therapies for various diseases.
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