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Tranilast inhibits NLRP3. 55 / 55
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"Among others, tranilast, an analog of a tryptophan metabolite, was proven to inhibit the activation of the NLRP3 inflammasome in vivo and efficiently suppressed IL-1β production and neutrophil influx after tissue exposure to MSU; it also reduced acute joint swelling in murine models [24]."
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"In this context, the activation of NLRP3 inflammasome via TLR4 or LPS may be involved in visceral pain and compromised gut barrier in these IBS models.Recently, tranilast, an anti-allergic drug, has b[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"TR has no effects on upstream signaling of NLRP3, but inhibits the assembly of NLRP3 inflammasome."
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"Whole genome sequencing is becoming more accessible and should be useful for providing patient-specific treatment especially if combined with individual organoids.Unlike many ocular surface inflammatory conditions, there are few published studies investigating the role of inflammasomes in ocular allergy, particularly SAC and PAC, despite data showing that Tranilast, used for the treatment of allergic conjunctivitis, directly inhibits NLRP3 [76]."
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"Tranilast binds directly to the NACHT domain of the NLRP3 inflammasome to inhibit NLRP3 oligomerisation [136] ."
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"TR inhibits NLRP3 activation invivo and has beneficial effects in mouse models of gouty arthritis and CAPS."
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"Since TR inhibits NLRP3 inflammasome activation invitro, we then determined to analyze the activity of TR invivo."
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"In vivo, BHB or a ketogenic diet attenuated caspase-1 activation and IL-1β secretion in mouse models of diseases mediated by NLRP3.Thus, the NLRP3 inflammasome may be a potential target for the treatment of COVID-19 [191,194], which is strongly supported by studies showing improved saturation, reduced hospitalization time and reduced mortality in patients with COVID-19 after treatment with NLRP3 inflammasome inhibitors such as Tranilast [200] or colchicine [198]."
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"Tranilast is a direct inhibitor of NLRP3 by binding to the NACHT domain and it suppresses the inflammasome assembly by blocking the oligomerization of NLRP3 (Huang et al., 2018)."
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"We then investigated how TR inhibited NLRP3 inflammasome activation."
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"Tranilast blocks NLRP3 inflammasome assembly independent of its ATPase activity."
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"Huang et al. reported that tranilast can inhibit NLRP3 specifically."
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"Additionally, tranilast inhibits NLRP3 inflammasome for the treatment of inflammatory-driven diseases in mouse models of CAPS, gouty arthritis and type 2 diabetes (T2D) [21] ."
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"More importantly, TR could prevent or treat NLRP3 dependent inflammatory diseases in mice models and was also active exvivo for samples from patients with gout."
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"TR specifically inhibits NLRP3 inflammasome activation inmacrophages."
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"NLRP3 Inhibitor Tranilast Attenuates Gestational Diabetes Mellitus in a Genetic Mouse Model."
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"Tranilast, an old anti-allergic clinical drug, inhibits the oligomerization of NLRP3 avoiding assembly and increasing body weight and survival [ 70 ]."
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"Additionally, tranilast remarkably reduced the elevated expression of NLRP3 and proinflammatory cytokines."
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"TR has been proposed to inhibit transient receptor potential cation channel subfamily V member 2 (TRPV2) (Zhang etal, 2012), and we then examined whether TR blocked NLRP3 inflammasome via inhibition of TRPV2."
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"There are several known NLRP3 inflammasome blockers, such as MCC950, CY-09, tranilast, oridonin, 3,4-methylenedioxyb-nitrostyrene, and OLT1177 [42,43,44,45,46,47,48]."
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"There are many well-known NLRP3 inflammasome inhibitors, such as MCC950, CY-09, tranilast, oridonin, 3,4-methylenedioxyb-nitrostyrene, and OLT1177 [42,44,45,46,47,48]."
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"TR blocks the assembly of NLRP3 inflammasome (Huang et al., 2018)."
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"TR inhibited NLRP3 inflammasome activation, but had no effects on AIM2 or NLRC4 inflammasome activation, suggesting that it acts on the upstream of ASC to suppress inflammasome activation."
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"Recently, it has been confirmed that tranilast can directly inhibit NLRP3 activity [112]."
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"Tranilast effectively prevented these GI changes by inhibiting the NLRP3 inflammasome."
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"When BMDMs were stimulated with TR for 30min after 3-h LPS treatment, TR had no effect on LPS induced NLRP3, pro-IL-1beta expression, TNF-alpha, or IL-6 production (Fig XREF_FIG C and D, and XREF_SUPPLEMENTARY), suggesting that TR induced NLRP3 inflammasome inhibition was not caused by the downregulation of NLRP3 or pro-IL-1beta expression at this condition."
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"The results showed that knockdown of TRPV2 in BMDMs had no effect on nigericin induced NLRP3 inflammasome activation (XREF_SUPPLEMENTARY), suggesting TRPV2 is not involved in TR induced NLRP3 inflammasome inhibition."
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"Tranilast also acts to inhibit NLRP3 inflammasome specifically without disrupting the activation of the other known inflammasomes such as NLRC2 and AIM2."
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"Tranilast directly binds to the NACHT domain of NLRP3, inhibiting the interaction of NLRP3 and subsequent ASC oligomers [10,13] ."
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"The results of these studies are presented in the form of review articles in which the efficacy of NLRP3 inflammasome inhibitors like Tranilast, has been suggested (Table 1)."
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"Similar to tranilast, dapansutrile inhibits the NLRP3 inflammasome and thus inhibits activation of IL-1β."
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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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"A single-arm prospective cohort (phase II) study designed to observe the efficacy and safety of tranilast (a small molecule inhibitor of the NLRP3 inflammasome) in CAPS patients."
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"Thus, these results indicate that TR can suppress the pre-activated NLRP3 inflammasome in cells from patients and suggest that TR or its analogues might be used to control NLRP3 driven diseases in clinics."
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"Like the three specific inhibitors mentioned above, Tranilast does not interfere with the upstream signaling pathways of NLRP3 inflammasome, including NLRP3 and pro-IL-1beta expression, K + efflux, mitochondrial damage, ROS production, and chloride efflux, and can not prevent the newly identified NLRP3 inflammasome component NEK7 from interacting with NLRP3 109."
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"Moreover, triple combination drug treatment comprising of amlexanox (TBK1/IKKα inhibitor), SS-31 (mitochondria-targeted antioxidant) and tranilast (an inhibitor of NLRP3) reduces redox stress-mediated mitophagic flux, lysosome enlargement and cell death [34]."
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"Unlike the CY-09 identified by the same group, Tranilast inhibits NLRP3 inflammasome activation via an ATPase independent manner, by blocking direct NLRP3-NLRP3 interaction 109."
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"NLRP3 inflammasome inhibitors such as tranilast, tetracycline, resveratrol, nicardipine, erythropoietin and colchicine are under clinical trials for management of COVID-19 [16]."
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"These results suggest that TR acts upstream of caspase-1 and ASC oligomerization to inhibit NLRP3 inflammasome activation."
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"Tranilast suppressed NLRP3 activation in low density lipoprotein receptor and apolipoprotein E deficient macrophages [46]."
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"Tranilast, an old anti-allergic clinical drug, inhibits the oligomerization of NLRP3 avoiding assembly and increasing body weight and survival [ 79 ]."
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"To further confirm that TR prevents or treats metabolic disorders through inhibition of NLRP3 inflammasome activation, we tested whether TR treatment inhibited the NLRP3 inflammasome activation and metainflammation in diabetic mouse models."
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"Thus, these results suggest that TR acts downstream of potassium efflux, mitochondrial damage, and chloride efflux to inhibit NLRP3 activation."
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"Next, we assessed whether TR inhibited the assembly of NLRP3 inflammasome."
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"Tranilast, a tryptophan metabolite analogue, inhibits NLRP3 ATPase activity through cysteine modification and blocks the activation of NLRP3 inflammasome (117)."
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"Interestingly, TR could not block cLPS induced gasdermin D (Gsdmd) activation and pyroptosis, suggesting that TR targets the downstream of caspase-11 to inhibit non canonical NLRP3 activation (XREF_SUPPLEMENTARY)."
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"Moreover, several inhibitors, including parthenolide, Bay 11-7082, INF39, 3,4-methylenedioxy-beta-nitrostyrene, and CY-09, have been reported to inhibit NLRP3 inflammasome activation by suppressing the ATPase activity of NLRP3 (Juliana etal, 2010; He etal, 2014; Cocco etal, 2017; Jiang etal, 2017), so it is possible that TR might inhibit the ATPase activity of NLRP3 to block its oligomerization."
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"As a safe small-compound drug employed frequently in clinic, tranilast (TR) is newly reported to block the activation of NLRP3 inflammasome in macrophage."
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"As a safe small-compound drug employed frequently in clinic, tranilast (TR) is newly reported to block the activation of NLRP3 inflammasome in macrophage."
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"Moreover, tranilast inhibited the activation of the NLRP3 inflammasome in vivo, demonstrating a protective effect on NLRP3 mediated acute inflammation and tissue damage, which could be employed in clinical practice (Huang et al., 2018)."
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"TR inhibits NLRP3 inflammasome activation in macrophages, but has no effects on AIM2 or NLRC4 inflammasome activation."
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"Thus, these results indicate that TR treatment can inhibit NLRP3 inflammasome activation and metainflammation in diabetic mice."
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"The potential NLRP3 inflammasome inhibitors, such as MCC950, CY-09, OLT1177, Tranilast, and Oridonin, were validated in vitro, and in a mouse model including Parkinson's disease, acute arthritis, or HFD-induced diabetes [242526272829]."
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"Tranilast suppresses inflammation by inhibiting NLRP3 inflammasomes but not AIM2 or NLRC4 inflammasomes."
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"Taken together, these results demonstrate that TR can specifically inhibit NLRP3 inflammasome activation and the subsequent IL-1beta production."
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