IndraLab

Statements


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"Glyburide and parthenolide both inhibited NLRP3 activation by LPS and ATP (data not shown)."

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"Previous studies have reported that MNS, parthenolide, BAY 11-7082, and INF39 can inhibit the ATPase activity of NLRP3 and show inhibitory activity for NLRP3 inflammasome in vitro."

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"IL-1beta secretion was not affected by treatment with the NLRP3 inhibitor glyburide XREF_BIBR or parthenolide, which has also been shown to inhibit NLRP3 XREF_BIBR."

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"OLT1177 , BOT-4-one , parthenolide , BAY 11-7082 , INF39 , and MCC950 could inhibit ATPase activity of NLRP3 ."
| DOI

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"For example, MCC950, CY-09, OLT1177/dapansutrile, MNS, and parthenolide inhibit NLRP3 by inhibiting its ATPase activity or modifying its ATPase domain38,48,54-57)."

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"Parthenolide inhibits NLRP1, NLRC4, and NLRP3 stimuli by alkylating a number of cysteine residues of caspase-1 thus blocking caspase-1 activation."

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"A few NLRP3 inflammasome inhibitors, including sulforaphane, isoliquiritigenin, beta-hydroxybutyrate (BHB), flufenamic acid, mefenamic acid, 3,4-methylenedioxy-beta-nitrostyrene (MNS), parthenolide, BAY 11-7082, INF39, and MCC950, have been developed, but there is no evidence showing that these compounds can specifically and directly inhibit NLRP3 itself."

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"Parthenolide, BAY 11-7082, INF39, and MNS have been reported to directly inhibit NLRP3 ATPase activity, but these inhibitors have unspecific roles."

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"OLT1177 , BOT-4-one , parthenolide , BAY 11-7082 , INF39 , and MCC950 could inhibit ATPase activity of NLRP3 ."

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"Parthenolide inhibits NLRP1 , NLRC4 , and NLRP3 stimuli by alkylating a number of cysteine residues of caspase-1 thus blocking caspase-1 activation ( Juliana et al. 2010 ) ."

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"The underlying mechanisms of action of these molecules are diverse : BHB and glyburide prevent the decline of intracellular K + required for NLRP3 activation and ASC oligomerization XREF_BIBR, XREF_BIBR, whereas parthenolide and Bay 11-7082 inhibit NLRP3 ATPase activity 18."

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"For example, MCC950, CY-09, OLT1177/dapansutrile, MNS, and parthenolide inhibit NLRP3 by inhibiting its ATPase activity or modifying its ATPase domain 38 , 48 , 54 - 57) ."

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"Bay 11–7082 and parthenolide directly inhibit NLRP3 and also inhibit caspase-1 activity, but are not suitable for clinical development due to the potential for widespread immunosuppression ( xref )."

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"However, previously identified NF-kappaB inhibitors Bay 11-7082 and parthenolide were also shown to inhibit the second step of NLRP3 inflammasome activation [XREF_BIBR]."

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"Parthenolide, a naturally occurring sesquiterpene lactone from Feverfew, and Bay 11-7082, a phenyl vinyl sulfone compound, disrupt the ATPase activity of NLRP3, concurrent with suppressed IκB kinase, NF-κB and caspase-1 activation [142,143,144]."

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"For example, MCC950, CY-09, OLT1177/dapansutrile, MNS, and parthenolide inhibit NLRP3 by inhibiting its ATPase activity or modifying its ATPase domain 38, 48, [54] [55] [56] [57] ."

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"In a similar manner, parthenolide, a sesquiterpene lactone alkylating agent, alkylated the NACHT domain and inhibited the ATPase of NLRP3 (Juliana et al., 2010)."

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"For example, MCC950, CY-09, OLT1177/dapansutrile, MNS, and parthenolide inhibit NLRP3 by inhibiting its ATPase activity or modifying its ATPase domain 38, 48, [54] [55] [56] [57] ."

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"Interestingly, in addition to its role in inhibiting caspase-1, parthenolide also directly inhibits NLRP3 by inhibiting its ATPase activity, which is required for activation of caspase-1."

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"Different NLRP3 inflammasome inhibitors, including sulforaphane, β-hydroxybutyrate, glyburide, flufenamic acid, mefenamic acid, parthenolide, BAY 11-7082, INF39, and MCC950 have been developed, but there is no evidence demonstrating that these compounds directly and specifically target NLRP3 itself (212)."

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"Parthenolide , a plant sesquiterpene lactone isolated from Tanacetum parthenium and Bay11-7082 , a synthetic vinyl sulfone discovered in 1968 , could prevent NLRP3 signaling and the release of IL-1beta from PMA-differentiated and ATP-stimulated THP - 1 cells [ 196 ] ."