Table 2.
Inhibitors of the NLRP3 inflammasome
| Mechanism | Agents | Targets | Diseases | References |
|---|---|---|---|---|
| Direct targeting of NLRP3 | Bay 11–7082 | NLRP3 NACHT domain (ATPase region) | Systemic lupus erythematosus | (Juliana et al. 2010) |
| β‐carotene | NLRP3 PYD domain | Gout | (Yang et al. 2020a) | |
| CY-09 | NLRP3 NACHT domain (Walker A motif) | Gout, T2D, CAPS | (Jiang et al. 2017) | |
| MNS | NLRP3 LRR and NACHT domains | Inflammation-associated diseases | (He et al. 2014) | |
| MCC950 | NLRP3 NACHT domain (Walker B motif) | Multiple sclerosis, CAPS | (Coll et al. 2015) | |
| OLT1177 | NLRP3 NACHT domain (ATPase region) | Degenerative arthritis, CAPS | (Marchetti et al. 2018a) | |
| Oridonin | NLRP3 NACHT domain (cysteine 279) | T2D, peritonitis, gout | (He et al. 2018) | |
| Parthenolide | NLRP3 NACHT domain (cysteine modification) | Cystic fibrosis | (D'Anneo et al. 2013) | |
| Tranilast | NLRP3 NACHT domain | Gout, CAPS, T2D | (Huang et al. 2018) | |
| Direct targeting of ASC | Caffeic acid phenethyl ester | ASC | Gout | (Lee et al. 2016) |
| Direct targeting of caspase-1 | VX-740, VX-765 | Caspase-1 | Rheumatoid arthritis, epilepsy, psoriasis, AD, myocardial infarction | (Linton 2005) |
| Targeting IL-1β | Anakinra | IL-1α and IL-1β | Gout, rheumatoid arthritis coronary artery disease, acute Kawasaki disease | (So et al. 2007) |
| Canakinumab | IL-1β | CAPS, gout | (Church and McDermott 2010) | |
| Gevokizumab | IL-1β | T1D, T2D, Rheumatoid arthritis | (Cavelti-Weder et al. 2012) | |
| Rilonacept | IL-1 | CAPS, gout, systemic sclerosis | (Kone-Paut and Galeotti 2015) | |
| Targeting IL-18 | GSK1070806 | IL-18 | Autoimmune diseases, non-Hodgkin’s lymphoma, IBD | (Mistry et al. 2014) |
| Indirect inhibition | Auranofin | IKK kinase, thioredoxin reductase | Rheumatoid arthritis, acne | (Isakov et al. 2014) |
| β-hydroxybutyrate | K + efflux, ASC aggregation | MWS, FCAS, urate crystal–induced peritonitis | (Youm et al. 2015) | |
| Celastrol | K + efflux | Autoimmune diseases, tumor | (Lee et al. 2019a) | |
| EGCG | Mitochondrial DNA | Gout | (Lee et al. 2019b) | |
| FC11A-2 | Caspase-1, IL-1β, IL-18 | Colitis | (Liu et al. 2013b) | |
| Glyburide, 16,673–34-0, JC171 | ATP-sensitive K + channels, ASC, P2X7 signaling | T2D, acute myocardial infarction |
(Lamkanfi et al. 2009b) (Marchetti et al. 2014) (Guo et al. 2017) |
|
| JC124 | ASC aggregation | Traumatic brain injury, neuroinflammatory, Acute myocardial infarction, AD | (Yin et al. 2018) | |
| Licochalcone A | Mitochondrial ROS, UCP1 expression | P. acnes-mediated acne, obesity | (Lee et al. 2018) | |
| Sulforaphane | AMP-activated protein kinase/autophagy axis | NAFLD, gout | (Yang et al. 2016) |