IndraLab

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Parthenolide inhibits CASP1. 32 / 32
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"Juliana et al. [64] reported that parthenolide inhibited the activity of inflammasomes in primary macrophage cell cultures by directly inhibiting caspase-1, which led to the downregulation of IL-1β and IL-18 level."
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"As shown in Fig. 2 A , caspase-1 activity was significantly ( P < 0.01) inhibited by the caspase-1 inhibitor Ac-YVAD-CMH (positive control; 100 μM), and parthenolide, but not by DMF and MMF (all at 10[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"Caspase-1 is the only common component in all inflammatory pathways, and the study has explored whether parthenolide might directly inhibit in vitro caspase-1 activation in THP-1 lysates."
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"Since parthenolide inhibits both NF-kappaB and caspase-1 activation, we determined whether this result is due predominantly to inflammasome inhibition by treating THP-1 cells with Bay 11-7082, which selectively inhibits the NLRP3 inflammasome independently of its effect on NF-kappaB activity."
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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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"Juliana et al. xref have shown that parthenolide directly inhibits caspase-1 by alkylation of certain cysteine residues."
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"Our results disagree with this assertion as we did not find that parthenolide inhibited caspase-1 in response to AIM2 stimulation."
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"However, the previous study xref did not test AIM2 activation so perhaps parthenolide only inhibits caspase-1 in response to NLRP3 or NLRC4 activation."
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"Notably, the combination of chloroquine and 6-AN triggered activation of the NF-kB and inflammasome pathways in a TSC2 dependent manner, and parthenolide 16, which inhibits both NF-kB and caspase-1, rescued proliferation under these conditions."
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"Parthenolide inhibited caspase-1 activation in response to NLRP3, NLRP1 and NLRC4 stimulation."
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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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"XREF_BIBR It was thought to be an NFkappaB inhibitor through selective inhibition of kappaB kinase beta (IKKbeta) kinase activity; however, in addition to its effects on NFkappaB activation, parthenolide has now been shown to inhibit activation of caspase-1 in response to NLRP3, NLRP1, and NLRC4 stimulation."
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"The effect of parthenolide on the spectrum of inflammasomes implies that it acts on a common component and, accordingly, it has been shown that parthenolide is a direct inhibitor of caspase-1, causing alkylation of caspase-1 on a number of cysteine residues."
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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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"Parthenolide and Bay 11-7082 directly inhibit activation of the protease caspase-1 to inhibit the various inflammasomes in macrophages [167]."
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"To test the hypothesis that activation of NF-kB is necessary for the inhibition of cell proliferation by chloroquine and 6-AN, we treated the cells with parthenolide, which inhibits both p65/RelA and caspase-1 via alkylation xref ."
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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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"VX-765 and pralnacasan/VX-740 are peptidomimetic compounds and are analogs of parthenolide and act by inhibiting caspase-1, acting as."
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"Parthenolide also inhibits caspase-1 and, thus, inhibits signaling by all canonical inflammasomes."
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"In addition, the herbal anti-inflammatory compound parthenolide and other IKKβ inhibitors are also able to inhibit caspase-1 ( Juliana et al., 2010 )."
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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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"Mass spectrometry results show that parthenolide irreversibly inhibits caspase-1 by alkylating C285 of the p20 subunit, blocking activity and cleavage of downstream events."
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"XREF_BIBR have shown that parthenolide directly inhibits caspase-1 by alkylation of certain cysteine residues."
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"Parthenolide also impedes the ATPase activity of NLRP3 and the protease activity of caspase 1."
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"Our results disagree with this assertion as we did not find that parthenolide inhibited caspase-1 in response to AIM2 stimulation."
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"Mass spectrometry results show that parthenolide irreversibly inhibits caspase-1 by alkylating C285 of the p20 subunit, blocking activity and cleavage of downstream events."
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"Parthenolide is another vinylsulfone that blocks caspase-1 , and therefore prevents caspase-1 activity in response to the activation of NLRP3 , NLRC4 , and AIM2 inflammasomes [ 113 ] ."
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"Parthenolide inhibits caspase-1 activation , however , has poor solubility and bioavailability ."
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"Parthenolide has also been shown to directly inhibit caspase-1 by alkylation of the enzyme 's p20 subunit [XREF_BIBR]."
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"Parthenolide has previously been shown to inhibit NLRC4 dependent caspase-1 activation 15, although it did not do so in these experiments (XREF_FIG)."
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"To test the hypothesis that activation of NF-kB is necessary for the inhibition of cell proliferation by chloroquine and 6-AN, we treated the cells with parthenolide, which inhibits both p65 and RelA and caspase-1 via alkylation 16."
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"Parthenolide also inhibits caspase-1 and, thus, inhibits signaling by all canonical inflammasomes."
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