Title : A translocator protein 18 kDa ligand, Ro5-4864, inhibits ATP-induced NLRP3 inflammasome activation.

Pub. Date : 2016 Jun 3

PMID : 27103438






7 Functional Relationships(s)
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1 A translocator protein 18 kDa ligand, Ro5-4864, inhibits ATP-induced NLRP3 inflammasome activation. 4'-chlorodiazepam NLR family pyrin domain containing 3 Homo sapiens
2 Here, we demonstrate for the first time that TSPO ligands, especially Ro5-4864, potently suppressed ATP-induced NLRP3 inflammasome activation in THP-1 and BMDM cells. 4'-chlorodiazepam NLR family pyrin domain containing 3 Homo sapiens
3 Ro5-4864 efficiently attenuated NLRP3 translocation to mitochondria, inflammasome assembly/oligomerization, activation of caspase-1, and subsequent secretion of the mature forms of interleukin-1beta and -18. 4'-chlorodiazepam NLR family pyrin domain containing 3 Homo sapiens
4 Ro5-4864 also reduced the production of mitochondrial superoxide and preserved the mitochondrial membrane potential in ATP-treated cells, suggesting that Ro5-4864 may act on mitochondria or more upstream targets in NLRP3 inflammasome signaling. 4'-chlorodiazepam NLR family pyrin domain containing 3 Homo sapiens
5 Ro5-4864 also reduced the production of mitochondrial superoxide and preserved the mitochondrial membrane potential in ATP-treated cells, suggesting that Ro5-4864 may act on mitochondria or more upstream targets in NLRP3 inflammasome signaling. 4'-chlorodiazepam NLR family pyrin domain containing 3 Homo sapiens
6 Collectively, our novel findings demonstrate that Ro5-4864 effectively inhibited ATP-induced NLRP3 inflammasome activation through the prevention of mitochondrial perturbation. 4'-chlorodiazepam NLR family pyrin domain containing 3 Homo sapiens
7 Our results indicate Ro5-4864 as a promising candidate for the treatment of NLRP3 inflammasome-related diseases. 4'-chlorodiazepam NLR family pyrin domain containing 3 Homo sapiens