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NLRP3 inflammasome and its inhibitors: a review
Open accessAbstract
Inflammasomes are newly recognized, vital players in innate immunity. The best characterized is the NLRP3 inflammasome, so-called because the NLRP3 protein in the complex belongs to the family of nucleotide-binding and oligomerization domain-like receptors (NLRs) and is also known as "pyrin domain-containing protein 3". The NLRP3 inflammasome is associated with onset and progression of various diseases, including metabolic disorders, multiple sclerosis, inflammatory bowel disease, cryopyrin-associated periodic fever syndrome, as well as other auto-immune and auto-inflammatory diseases. Several NLRP3 inflammasome inhibitors have been described, some of which show promise in the clinic. The present review will describe the structure and mechanisms of activation of the NLRP3 inflammasome, its association with various auto-immune and auto-inflammatory diseases, and the state of research into NLRP3 inflammasome inhibitors.
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“Additionally, it has been demonstrated that NF‐κB–mediated signaling is also involved in the NLRP3 inflammasome activation by regulating the transcription of inflammasome‐related components, including inactive NLRP3, pro‐IL‐1β, and pro‐IL‐18.46”
From Trimethylamine‐N‐Oxide Induces Vascular Inflammation by Activating the NLRP3 Inflammasome Through the SIRT3‐SOD2‐mtROS Signaling Pathway (2017) · cites this paper as [46]
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NLRP3 inflammasome activity is required for wound healing after burns
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“into active caspase-1, which then cleaves pro-IL-1β and proIL-18 to their active forms [14, 15].”
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“Recently, the activation of the pyrin domain-containing protein 3 (NLRP3) inflammasome has been found to be associated with various neurological disorders, such as Alzheimer’s disease [14], cerebrovascular disease [15, 16] and epilepsy [17].”
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“Interactions among these three proteins tightly regulate inflammasome functions through inducing the production and secretion of IL-1 β and IL-18, whose maturity is triggered by caspase-1 from their “pro” forms (110).”
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NLRP3 inflammasome: a new therapeutic target for high-risk reproductive disorders?
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Gut Microbiota in NSAID Enteropathy: New Insights From Inside
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“NLRP3 recruits and activates the pro-inflammatory protein Caspase-1, and activated Caspase-1 stimulates macrophage secretion of IL-1b to induce liver damage (Shao et al., 2015).”
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“nucleatum could destabilize host-cell mitochondria, which results in mROS production, which in turn is regulated by NLRX1 [54, 39, 51, 12, 27].”
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Role of Microgliosis and NLRP3 Inflammasome in Parkinson’s Disease Pathogenesis and Therapy
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“It plays a vital role in the process of myocardial fibrosis [45].”
Mitochondria-associated membranes: A hub for neurodegenerative diseases
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Celastrol ameliorates inflammation through inhibition of NLRP3 inflammasome activation
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“Thus, characterization of the NLRP3 inflammasome inhibitor may provide novel insights into the control of inflammatory processes [28].”
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Metadata
- Authors
- Shao, B.-Z., Xu, Z.-Q., Han, B.-Z., Su, D.-F., & Liu, C.
- Affiliations
- Second Military Medical University (CN)
- Corresponding author
- Liu, Chong
- Venue
- Frontiers in Pharmacology
- Publisher
- Frontiers Media SA
- Published
- 2015-11-05
- Volume
- 6
- Pages
- 262-262
- ISSN
- 1663-9812 (ISSN-L)
- PMC
- PMC4633676
- OpenAlex
- W2137444266
- Cited by
- 836
- References
- 115
- Citations by year
- 2026: 42 · 2025: 62 · 2024: 102 · 2023: 107 · 2022: 114 · 2021: 105 · 2020: 91 · 2019: 68 · 2018: 61 · 2017: 57 · 2016: 24 · 2015: 2
- FWCI
- 4.60
- Type
- journal article
- Language
- en
- Open access
- gold
- doi.org
- Licence
- cc-by
- Locations
- Frontiers in Pharmacology (publishedVersion, cc-by)
- Europe PMC (PubMed Central) (publishedVersion, cc-by)
- PubMed Central (publishedVersion, cc-by)
- PubMed (publishedVersion)
- DOAJ (DOAJ: Directory of Open Access Journals) (submittedVersion, cc-by-sa)
- Frontiers in Pharmacology (cc-by)
- Funders
- Natural Science Foundation of Shanghai (13ZR1448400)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Inflammasome and immune disorders
- Life Sciences › Immunology and Microbiology › Immunology › Immune Response and Inflammation
- Health Sciences › Medicine › Hematology › Autoimmune and Inflammatory Disorders Research
- Keywords
- NLRP3 inflammasome, inflammasome inhibitors, innate immunity, autoinflammatory disease, autoimmune disease, metabolic disorders, multiple sclerosis, inflammatory bowel disease
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