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Glyburide inhibits NLRP3. 118 / 118
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"Glyburide and MCC950 were used to inhibit the NLRP3 inflammasome."
34631111
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"An interesting point in the relationship between inflammasome and metabolism is that glyburide, a well-known drug of sulfonylurea class for type 2 diabetes inhibits NLRP3 stimulation, which is independent of its effect on ATP sensitive K ATP channel."
21637386
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"In this study, we show that the type 2 diabetes drug glyburide prevented activation of the Cryopyrin inflammasome."
19805629
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"Glyburide appears to inhibit the NLRP3 inflammasome and the subsequent IL-1β activation in macrophages."
32445957
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"Glyburide, an antidiabetic drug, can block NLRP3 inflammasome activation by inhibiting ATP sensitive K+ channels XREF_BIBR."
32505910
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"Lamkanfi et al. demonstrated that glyburide is able to inhibit assembly of the NLRP3 inflammasome in response to stimulation with lipopolysaccharide (LPS) and adenosine triphosphate (ATP) XREF_BIBR."
24147174
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"Glyburide was shown to inhibit the ATPase activity of NLRP3, but it is unclear whether other drugs from this class can act in a similar manner, and if this observation is related to the glyburide mediated inhibition of inflammasome formation."
27508077
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"It was reported that glyburide prevents Nlrp3 inflammasome activation in vitro; XREF_BIBR however, the effects of GLP-1 receptor activation on the Nlrp3 inflammasome has not been reported before."
27547413
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"Glibenclamide inhibited NLRP3 inflammasome via upstream inhibition of the inflammasome and downstream blockade of the P2X7 receptor, which then reduced NLRP3 inflammasome mediated caspase-1 activation and inhibited the maturation of IL-1beta [XREF_BIBR]."
29178967
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"Compound glyburide, which is known to inhibit NLRP3 function, blocked IL-1beta production because of M. tuberculosis and M. tuberculosis promoted necrosis (XREF_FIG)."
21740493
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"To eliminate that adverse effect, an intermediate of glibenclamide, 16673-34-0, has been designed to inhibit the NLRP3 inflammasome [135]."
35042840
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"Glyburide and YVAD significantly inhibited the activation of NLRP3 inflammasome and the production of IL-1beta stimulated by anti-dsDNA antibodies."
27250627
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"To investigate the role of the NLRP3 inflammasome in LPS induced IL-1beta production by the CFs, the cells were transfected with siRNA, which was specific for NLRP3, or CFs were pretreated with glyburide (an inhibitor of NLRP3 inflammasomes) prior to the LPS challenge XREF_BIBR."
25216263
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"In addition, a study has reported that glibenclamide inhibits the NLRP3 inflammasome and effectively reduces edema development [201]."
34059091
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"Similar results were obtained when glyburide instead of CASP1 inhibitor was used to block NLRP3 inflammasome XREF_BIBR, XREF_BIBR."
32332867
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"Glyburide, which specifically inhibits NLPR3 inflammasome activation [XREF_BIBR], was used to inhibit NLRP3, and capase-1 inhibitor YVAD was used to inhibit caspase-1."
27250627
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"Glibenclamide was also shown to inhibit activation of the NLRP3 inflammasome [XREF_BIBR]."
33456300
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"Glyburide, an antidiabetic drug, can block NLRP3 inflammasome activation by inhibiting ATP sensitive K+ channels [26]."
32505910
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"It has been observed that glyburide, a drug for the treatment of diabetes classified as a sulfonylurea, may block the activation of the NLRP3 inflammasome through the inhibition of ATP sensitive K+ channels."
33466589
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"It has been demonstrated that Glyburide can inhibit NLRP3 inflammasome, but not NLRC4 or AIM2 [XREF_BIBR]."
33803783
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"Glyburide appears to inhibit the NLRP3 inflammasome and the subsequent IL-1activation in macrophages."
32445957
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"In addition, the anti-diabetic drug glyburide can inhibits NLRP3 and therefore may function partially via ani-inflammatory mechanisms."
23068074
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"Likewise, a sulfonylurea drug Glyburide which is widely used for the treatment of Diabetes type 2, was also shown to inhibit the NLRP3 inflammasome."
32574259
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"Collectively, these results demonstrate that glyburide acts upstream of Cryopyrin and downstream of the P2X 7 receptor to block Cryopyrin dependent inflammasome activation by PAMPs, DAMPs, and crystalline substances."
19805629
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"In fact, glyburide, which is used in the treatment of T2D, was found to inhibit NLRP3 inflammasome activity."
23276949
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"Glyburide appears to inhibit the NLRP3 inflammasome and the subsequent IL-1β activation in macrophages (178)."
32445957
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"Glyburide appears to inhibit the NLRP3 inflammasome and the subsequent IL 1betaactivation in macrophages."
32445957
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"Additionally, glibenclamide inhibited NLRP3 and caspase-1 expression [XREF_BIBR]."
28740332
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"Mechanistically, glibenclamide treatment blocked NLRP3 inflammasome activation evidenced by reduced expressions of NLRP3, activated caspase-1 and mature interleukin-1beta in glibenclamide co-treated mice compared with those in paraquat and maneb group mice."
34052309
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"Glombik et al [XREF_BIBR] observed that maternal diabetes causes the activation of NLRP3 inflammasome signaling by increasing the level of the NLRP3 protein subunit, and glyburide, as a NLRP3 inflammasome inhibitor, diminishes the level of NLRP3 protein and caspase-1 subunits, and has particular therapeutic value in anti- metabolic related inflammation."
33395071
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"In summary, XREF_FIG provides two important pieces of information : first, that the NLRP3 inflammasome is more active in obese mice, as indicated by a more robust IL-1beta response; and second, that glyburide effectively inhibits the NLRP3 inflammasome, as evidenced by a significant reduction in IL-1beta release."
25152324
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"Lamkanfi et al. demonstrated that glibenclamide could inhibit the assembly of the NALP3 inflammasomes in response to stimulation with lipopolysaccharide (LPS) and adenosine triphosphate (ATP) [XREF_BIBR]."
25077824
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"The decrease in nerve density was blocked by glyburide or anakinra, clearly implicating the NLRP3 pathway in denervation."
28984997
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"Our results indicated that glibenclamide suppressed NLRP3, caspase-1, and IL-1beta in mice spinal cord in morphine tolerance."
29178967
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"This, in addition to the findings by the same group showing glyburide inhibits the inflammasome upstream of the NLRP3 subunit (likely through inhibition of K ATP channel mediated efflux of K +), provides strong evidence that glyburide is indeed specifically inhibiting NLRP3 inflammasome activation [XREF_BIBR]."
25152324
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"In this study, we show that glyburide prevented activation of the Cryopyrin inflammasome by a variety of stimuli."
19805629
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"This decrease was blocked by glyburide, demonstrating the central role of NLRP3 and suggesting that NLRP3 inhibitors may further help prevent BOO-induced neurodeterioration by suppressing negative changes in neuroplasticity."
32602164
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"Glyburide, a potassium channel inhibitor, could block the outflow of potassium ions and inhibit the assembly of the NLRP3 inflammasome (Zahid et al., 2019)."
34869071
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"Though indirect, the potency of glyburide for NLRP3 led to enthusiastic research on sulfonylurea derivatives and to the discovery of MCC950- a selective and direct inhibitor of NLRP3 that did not impact AIM2, NLRC4, or NLRP1 inflammasome signaling [191]."
33036374
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"Glyburide inhibits NLRP3 inflammasome activity caused by islet amyloid polypeptide (IAPP), ATP, and nigericin."
33534121
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"Neither glyburide nor compound G1 reduced the ATPase activity of recombinant Cryopyrin (XREF_FIG; and Fig."
19805629
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"In this work, we found that glibenclamide could inhibit Nalp3 inflammasomes and Caspase-1 induced by LPS+ high glucose stimulation in cultured peritoneal macrophages, suggesting that the effects of glibenclamide on prevention of serum IL-1beta and TNF-alpha might be related to inhibiting Nalp3 inflammasomes and Caspase-1."
25077824
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"Importantly, both indicators of neuroinflammation were blocked by glyburide, indicating their dependence on NLRP3."
32602164
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"Consistently, glibenclamide also blocked the oligomerization of ASC (XREF_FIG) and the association of NLRP3 and ASC (XREF_FIG and XREF_SUPPLEMENTARY) in mouse BMDMs in response to 25-HC treatment."
27779191
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"Furthermore, SARS-CoV-2-induced lytic cell death is reversed by the diabetes medicine glyburide, which abolishes the activation of the NLRP3 inflammasome."
34360684
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"( 4 ) Glyburide that inhibits NALP3 , which is a component of the inflammasome and coded by the NLRP3 gene [ 58 ] ."
31018556
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"Collectively, these results indicate that glyburide inhibits engagement of the Cryopyrin inflammasome by diverse stimuli and that inhibition occurs downstream of the P2X 7 receptor (XREF_FIG)."
19805629
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"Glyburide (International Nonproprietary Name : glibenclamide), an antidiabetic sulfonylurea drug, inhibits NLRP3 inflammasome activation by several stimuli, without affecting the NLRC4 or NLRP1 inflammasomes [XREF_BIBR]."
25152324
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"However, the doses of glyburide used in vivo to inhibit NLRP3 are very high, which results in hypoglycaemia, so it is limited to treating T2D only [247] ."
35365780
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"For instance, glybenclamide (aka glyburide), which blocks potassium efflux and therefore NLRP3 inflammasome activation, was shown to significantly reduce colitis in Il10 -/- mice as well as the expres[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
29433944
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"Moreover, our study provided a clinically safe and effective hypoglycemic drug, glibenclamide, which inhibited HSP70 release by blocking K ATP channel and suppressed NLRP3 inflammasome activation, which consequently attenuated morphine tolerance."
29178967
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"Glyburide (glibenclamide), a sulfonylurea drug used for the treatment of type-2 diabetes, is known to inhibit ATP sensitive K + channels and can thus prevent NLRP3 inflammasome activation."
26279628
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"As shown in Fig. 7e–g, the secretion of IL-1β and IL-18 was also inhibited in glyburide-treated T2D mice, indicating that the activation of NLRP3 inflammasome was inhibited by glyburide in vivo, although glyburide didn’t directly inhibit NLRP3 protein ."
30291237
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"The mechanism how glibenclamide inhibits NALP3 inflammasomes and suppresses IL-1beta secretion is an intriguing question."
25077824
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"Glyburide inhibits NLRP3 inflammasome activity."
33603747
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"Glyburide (Gly) could inhibit NLRP3 inflammasome, as well as could be treated with Type 2 diabetes as a common medication."
34037304
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"This study revealed that glyburide inhibits NLRP3 inflammasome activation by various stimuli, thereby preventing secretion of IL-1beta [XREF_BIBR]."
20861596
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"Glyburide and fluoxetine impeded activation of NLRP3 inflammasome in pancreas by suppressing upstream molecule TXNIP."
29084550
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"For example, Glyburide can inhibit NLRP3 inflammasome mediated caspase-1 activation and both IL-1beta and IL-18 release 15."
22430788
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"To explore whether N. caninum also induced NLRP3 inflammasome activation via K + efflux, glyburide, which inhibits the NLRP3 inflammasome by inhibiting K + efflux, was added to BMDMs."
30105037
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"To further validate the role of NLRP3 inflammasome during HS induced cellular responses, cells were co-cultured with the NLRP3 antagonist glyburide or the caspase-1 specific inhibitor YVAD."
30611121
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"NOD like receptor protein-3 (NLRP-3) is pro inflammatory in the kidney; glibenclamide inhibits production of NLRP-3."
24291534
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"Glyburide inhibits the Cryopyrin inflammasome downstream of the P2X 7 receptor."
19805629
eidos
"Although glyburide potently inhibits NLRP3 activation in vitro , it requires high doses in vivo and the mechanism of action is unknown ."
31036962
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"The use of glibenclamide and interference plasmids to inhibit NLRP3 inflammasome activation revealed that the number of CSFV virus gene copies and the virus titer after 24 and 48 h increased following CSFV infection in PBMCs, indicating that NLRP3 had a negative effect on CSFV replication."
30013955
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"Antioxidants and glyburide block upstream signaling of the NLRP3 inflammasome in vitro."
25596299
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"Glyburide, a drug commonly used in type 2 diabetes, can also prevent NLRP3 dependent IL-1beta production [XREF_BIBR]."
28192528
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"Additionally, glyburide can inhibit the NLRP3 inflammasome in cells infected with RNA viruses [131]."
34183243
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"Glyburide and parthenolide both inhibited NLRP3 activation by LPS and ATP (data not shown)."
22216309
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"Results suggested glyburide might inhibit NLRP3 inflammasome to attenuate inflammation related lung tumorigenesis caused by intratracheal instillation of B (a) p/LPS in non diabetes mice."
34037304
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"Likewise, another biaryl compound, glyburide, with an intrachain and a sulfone group, also inhibits NLRP3 in spite of its main therapeutic indications toward type 2 diabetes [14]."
35566202
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"Nano molar concentration of MCC950, glyburide, sulofenur, glimepiride, gliquidone, or glisoxepide inhibits NLRP3 activation and stimulates insulin secretion in mouse pancreatic cells, indicating the dual effects (Hill et al., 2017)."
34539410
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"Interestingly, glibenclamide (also known as glyburide), a diabetes drug proposed as a novel treatment for acute brain injury due to its ability to inhibit the Sur1-Trpm4 channel involved in brain edema [XREF_BIBR], was also shown to inhibit the NLRP3 inflammasome [XREF_BIBR]."
25091898
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"Glibenclamide decreased infiltration of chronic inflammatory cells, fibrosis, tubular damage and expression of HO-1, TNF-alpha and NLRP-3 in the kidney."
24291534
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"Glyburide, a K + channel blocker, also inhibited NLRP3 inflammasome in vitro, which appears to confirm the role of K + efflux."
29892295
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"Glyburide inhibits the Cryopyrin and Nalp3 inflammasome."
19805629
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"Glibenclamide Might Inhibit the Activation of NLRP3 Inflammasome."
28740332
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"To determine whether NLRP3 inflammasome is involved in islet cell death induced by hypoxia, NLRP3 inflammasome was inhibited by glyburide under hypoxia and cell death analyzed."
29941940
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"The sulfonylurea drug glyburide, usually used clinically to treat type II diabetes, is a non selective antagonist of NALP3 and could prevent activation of the NALP3 inflammasome and crystal induced IL-1beta secretion."
30186184
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"Glibenclamide inhibited NLRP3 inflammasome activation and subsequently protected against organ inflammation and tissue damage either in a cerulean induced obese mouse model of SAP, or in an adenine-diet rat model of chronic kidney disease, or in a cyclophosphamide induced rat model of bladder inflammation, or in a lipopolysaccharide induced myocardial injury in streptozocin induced diabetic rats [XREF_BIBR, XREF_BIBR, XREF_BIBR, XREF_BIBR]."
28740332
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"NOD2 stimulation by systemic administration of muramyl dipeptide appears to be beneficial in mouse models of colitis.123 Glyburide (glibenclamide), a sulfonylurea drug for the treatment of type 2 diabetes, is known to inhibit ATP-sensitive K+ channels and thus can prevent NLRP3 inflammasome activation.124 Glyburide has been shown to prevent ventilator-induced lung injury in mice and delay endotoxin-induced lethality in mice, but it has not been applied for animal models of colitis.124, 125PRR signaling has significant roles in intestinal homeostasis, which is mainly composed of the maintenance of commensals."
23515136
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"NLRP3 inflammasome signaling pathway was augmented by LPS but suppressed by glyburide."
27614764
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"Finally, specific FDA approved reagents that inhibit molecules involved in asbestos induced inflammation are available : anakinra, an IL-1beta receptor antagonist; infliximab, a chimeric human-mouse anti-TNF-alpha; etanercept, a soluble TNF receptor fusion protein; glyburide, that inhibits the NALP3 inflammasome [XREF_BIBR]."
26308799
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"Glyburide inhibited the NLRP3 inflammasome, lowered secreted IL-1β and decreased fibrosis."
35625564
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"Finally, we treated monocytes and MDC with 100 muM glibenclamide, a sulfonylurea drug which inhibits NLRP3 activation but not NLRC4 activation [XREF_BIBR]."
28081233
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"This can be explained by the fact that Nlrp3 inflammasome inhibition by glibenclamide was only partial, as residual amounts of IL-1beta and cleaved caspase-1 were still detectable in myeloid cells (unpublished data)."
23980097
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"Similar to RIPK3 dependent IL-1beta activation in caspase-8 or IAP depleted macrophages, the caspase-1 and IL-1beta secretion (but not TNF secretion) observed in LPS treated Ripk1 -/- FLDMs was abrogated by glyburide inhibition of NLRP3 (XREF_FIG)."
25693118
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"Our results are in agreement with the study of Tschopp et al., who showed that NLRP3 inflammasome is expressed and inhibited by glyburide in murine islet cells 20."
29941940
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"Glibenclamide (GLB), a sulphonylurea drug used to treat type II diabetes, possesses anti-inflammatory properties and inhibits NLRP3 inflammasomes."
31761320
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"Furthermore, glyburide impedes PAMP, DAMP, and crystal mediated NLRP3 inflammasome activation in bone marrow derived macrophages [XREF_BIBR]."
32693241
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"In our study, we chose glibenclamide not only because of its protective role in neurological diseases by inhibiting K ATP channels, but also because that glibenclamide could abolish the activation of NLRP3 inflammasome in bone marrow derived macrophages (BMDMs) [XREF_BIBR], although the exact mechanism was not fully understood."
29178967
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"Glyburide (glibenclamide), a sulfonylurea drug for the treatment of type 2 diabetes, is known to inhibit ATP sensitive K+ channels and thus can prevent NLRP3 inflammasome activation."
23515136
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"For inhibitor experiments, glyburide (100 mumol/L) and Z-YVAD-FMK (2 mumol/L) were added 30 minutes before PM 10 exposure to inhibit the NLRP3 inflammasome 38 or caspase-1, respectively."
22227418
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"Primarily acting by blocking the ATP sensitive K + channels (K ATP) in beta-cells of the pancreas, Glyburide was shown to act upstream and prevent NLRP3 inflammasome activation."
32574259
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"Glyburide, a sulfonylurea, is reported to inhibit the activation of NLRP3 inflammation by blocking the ATP-sensitive K+ channels (KATP)[61]."
34754842
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"Glibenclamide abolished inflammasome activation in macrophages lacking K ATP channel subunits as well [XREF_BIBR]."
28740332
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"The structure activity relationship experiments (XREF_FIG) suggest that glyburide inhibits the Cryopyrin inflammasome independently of SUR1 containing K ATP channels."
19805629
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"Glyburide, the most widely used sulfonylurea drug for type 2 diabetes in the US, inhibits the Nalp3 inflammasome."
22065079
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"The sulfonylurea Glyburide inhibits ATP sensitive K + (K ATP) channels and has been shown to inhibit NLRP3 inflammasome activation, without affecting the NLRP1 or NLRC4 inflammasomes."
26024799
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"Dimethyl fumarate-mediated Nrf2/ARE pathway activation and glibenclamide-mediated NLRP3 inflammasome cascade inhibition alleviate type II diabetes-associated fatty liver in rats by mitigating oxidative stress and inflammation."
36999408
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"Glyburide and fluoxetine inhibited NLRP3 inflammasome activation in hippocampi via downregulating TXNIP."
29084550
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"Glyburide, a type 2 diabetes drug, has been shown to specifically inhibit the NLRP3 inflammasome in response to microbial and crystalline stimuli XREF_BIBR."
25254654
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"The effects of the caspase‐1 inhibitor ZYVAD‐fmk or NLRP3 antagonist glyburide, and treatment with S1P or the S1P receptor regulator FTY720, with or without exposure to cigarette smoke extract were investigated.In alveolar macrophages, cigarette smoke induced increased intracellular expression of IL‐1β (~15%, p<0.05 on pooled data from 3 donors), with particulate staining for cleaved IL‐1β increased both inside and outside the cell (5 fold, p<0.001 on pooled data)."
28299871
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"This is the first study demonstrating that experimental SAP in obese rodents can be mitigated using glyburide, which has been shown to inhibit the NLRP3 inflammasome."
25152324
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"Glyburide (glibenclamide), a sulfonylurea drug for the treatment of type 2 diabetes, is known to inhibit ATP sensitive K+ channels and thus can prevent NLRP3 inflammasome activation."
23515136
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"Glyburide had no effect on NLRP3, caspase-1 and IL-1beta expression as compared with the control group, while the NLRP3, caspase-1 and IL-1beta were decreased by (20.49 +/-7.6)% (t = 2.862, P < 0.01), (32.94 +/-3.44)% (t = 4.154, P < 0.001) and (24.67 +/-5.29)% (t = 2.335, P < 0.05) in the PDGF+ glyburide group, respectively, as compared with the PDGF group."
28592027
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"When infection experiments were performed in the presence of glyburide, a compound that inhibits NLRP3 inflammasome, or A151, a specific AIM2 inhibitor, the secretion of IL-1beta was significantly inhibited with respect to uninfected controls."
32038610
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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."
22216309
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"Glyburide appears to inhibit the NLRP3 inflammasome and the subsequent IL-1activation in macrophages (178) ."
32445957
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"Glibenclamide is known to block the NLRP3 (NACHT, LRR, and PYD domains containing protein 3) inflammasome, which has been implicated in the pathophysiology of EAE [XREF_BIBR]."
26581714
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"The type 2 diabetes drug glyburide also prevents activation of the NLRP3 inflammasome [XREF_BIBR]."
28473983
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"Glyburide also inhibits NLRP3 inflammasome by inhibiting ATP-sensitive potassium channel and thus disturbs ASC aggregation59)."
33678767
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"This possibility is supported by a preliminary study, in which we found that a long-term treatment of glyburide to inhibit NLRP3 did not extend the survival of M. tuberculosis infected mice (data not shown)."
21740493
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"Previous study demonstrated that glibenclamide was able to suppress NALP3 activation independently of K ATP [XREF_BIBR]."
25077824
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"Another inhibitor of NLRP3, the sulfonylurea diabetes drug glyburide, reduced IL-6 secretion by SARS-CoV-2-infected human monocytes65."
34373622
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"Another inhibitor of NLRP3, the sulfonylurea diabetes drug glyburide, reduced IL-6 secretion by SARS-CoV-2-infected human monocytes ."
34373622
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"Anti-diabetic drug glibenclamide (GLB) possesses anti-inflammatory properties and inhibits NACHT, LRR, and PYD domains-containing protein 3 (NLRP3) inflammasome activation."
34664134
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"Glyburide (glibenclamide), a sulfonylurea drug used for the treatment of type-2 diabetes, is known to inhibit ATP sensitive K + channels and can thus prevent NLRP3 inflammasome activation."
26279628