IndraLab

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Parthenolide inhibits NLRP3. 38 / 38
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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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"Parthenolide also impedes the ATPase activity of NLRP3 and the protease activity of caspase 1."
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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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"Separate to its effects on NFκB activation parthenolide has now also been shown to inhibit caspase-1 and NLRP3."
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"Parthenolide also directly inhibits NLRP3 by inhibiting its ATPase activity that is required for activation [ 55 ]."
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"Juliana and coworkers [70] reported that parthenolide at a concentration of 10 μM can selectively inhibit the ATPase activity of NLRP3 through binding to cysteine in the p20 subunit of caspase-1."
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"Parthenolide was a direct inhibitor of caspase-1 and NLRP3, representing a therapeutic approach against inflammatory diseases [164] ."
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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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"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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"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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"OLT1177 , BOT-4-one , parthenolide , BAY 11-7082 , INF39 , and MCC950 could inhibit ATPase activity of NLRP3 ."
| DOI
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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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"MNS, parthenolide and BOT-4-one impair NLRP3 ATPase activity, thereby suppressing NLRP3 inflammasome activation."
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"Parthenolide inhibits the ATPase activity of NLRP3, which in turn decreases NLRP3 activity."
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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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"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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"Moreover, Parthenolide suppresses caspase-1 by causing alkylation of caspase-1 and limits NLRP3 by directly inhibiting its ATPase activity."
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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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"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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"Parthenolide (PTL), a naturally occurring nuclear factor kappa B (NF-κB) inhibitor, is also known to inhibit NLRP3 inflammasome."
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"Glyburide and parthenolide both inhibited NLRP3 activation by LPS and ATP (data not shown)."
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"Besides, INF39, Parthenolide and BAY 11-7082 are also able to inhibit the ATPase activity of NLRP3, however, the detailed molecular mechanism is not yet fully understood (Juliana et al., 2010; Shi et al., 2021c)."
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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 xref , xref , xref - xref ."
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"The results showed that epalrestat, sulforaphane, parthenolide and OLT1177 could inhibit the activation of NLRP3 inflammasome at the concentration of 40 μmol/L, and epalrestat is more effective than OLT1177 at this concentration (Additional file 2)."
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"Parthenolide and Bay11-7082 also inhibited NLRP3 ATPase activity in vitro [112], but are unlikely to act as specific NLRP3 inhibitors due to their diverse biological activities."
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"Besides using antibodies against inflammasome components a recent study showed that Bay-11-7082 and Parthenolide, both NF-κB pathway inhibitors were able to inhibit NLRP3 receptor ATPase activity, whi[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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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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"One study has demonstrated that parthenolide inhibits multiple inflammasome pathways including NLRP3, NLRP1, and NLRC4 and directly inhibits caspase-1, but does not inhibit the AIM2 pathway (Juliana et al., 2010; Coll et al., 2011)."
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"For example, taraxasterol and parthenolide suppress the activation of NLRP3 inflammasome by blocking the activation of NF-κB (126, 127), and celastrol resolves the inflammatory response to RA through inhibition of the ROS/NF-κB/NLRP3 axis (128)."
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"Parthenolide also directly inhibits NLRP3 by inhibiting its ATPase activity that is required for activation [ 55 ]."
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"Even, chemical inhibition of NLRP3 by parthenolide diminishes the occurrence of diabetes."
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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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"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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"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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"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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"Therefore, possible treatment for these diseases have been suggested by identifying therapeutic candidates such as miR-223, parthenolide, MCC950, and tranilast that block activation of NLRP3 inflammas[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"The vinyl sulfone Bay 11-7082, the sesquiterpene lactone parthenolide, and the benzoxathiole derivative BOT-4-one all block the ATPase activity of NLRP3 [116,117]."
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"Even, chemical inhibition of NLRP3 by parthenolide diminishes the occurrence of diabetes."
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