IndraLab

Statements



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"Together, these results suggest that : (i) the NLRP3 inflammasome and local IL-1beta (+) F4/80 (+) Ly6C (+) macrophages as novel players in the pathogenesis of VCP associated myopathy; and (ii) identified the sulfonylurea MCC950 inhibitor of the NLRP3 inflammasome with promising therapeutic potential for the future treatment of patients with VCP associated myopathy."

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"While Lamkanfi et al clearly showed this drug directly inhibits NLRP3, it is also a widely used sulfonylurea drug for the treatment of type 2 diabetes where it acts at ATP-sensitive K (KATP) channels and Kir6.2."

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"Agarwal et al. (2020) reported that thiazolo-alkenyl sulfonylurea derivative 7 inhibited the activation of NLRP3 by inhibiting ASC oligomerisation (Agarwal, Pethani, et al., 2020)."

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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."

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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."

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"Glyburide, the most widely used sulfonylurea drug for type 2 diabetes in the US, inhibits the Nalp3 inflammasome."

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"The mechanism by which sulfonylurea compounds inhibit NLRP3 activation is currently not understood."

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"However, unlike for CY-09, the molecular target and mechanism by which MCC950 and CRID3 and related sulfonylurea molecules inhibit the NLRP3 inflammasome remains enigmatic."

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"As evidence showed that another sulfonylurea drug glipizide also inhibited Sur1 containing K ATP channels but failed to inhibit NLRP3 inflammasome activation."

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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."

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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."

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"reported that thiazolo-alkenyl sulfonylurea derivative 7 inhibited the activation of NLRP3 by inhibiting ASC oligomerisation ."

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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."

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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]."

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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]."

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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."

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"Compounds with a sulfonylurea fragment can specifically inhibit the activation of the NLRP3 inflammasome in the activation phase without affecting the priming stage dependent on NF-κB signaling [83]."
| PMC

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"Moreover, the present study identified the sulfonylurea MCC950 inhibitor of the NLRP3 inflammasome as a promising therapeutic drug for the treatment of VCP associated myopathy."

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"Glibenclamide (GBC), a sulfonylurea drug used for diabetes, has been shown to inhibit the NLRP3 inflammasome pathway, suppress microglia and astrocyte activation, and support favorable neurologic outcomes following rodent CA (93)."

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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]."

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"The results confirm that the NLRP3 inflammasome and local IL-1beta (+) F4/80 (+) Ly6C (+) macrophages as novel players in the pathogenesis of VCP associated myopathy and identified the sulfonylurea MCC950 inhibitor of the NLRP3 inflammasome with promising therapeutic potential for the treatment of VCP associated myopathy."

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"Furthermore, inhibition of NLRP3 inflammasome by glybenclamide, a sulfonylurea inhibitor of NLRP3 inflammasome, was found to be able to suppress microglial proinflammatory activation and nuclear factor-kappaB activation induced by paraquat and maneb."