MCC950 直接针对 NLRP3 的 ATP 水解结构域，抑制炎症小体。
MCC950 directly targets the NLRP3 ATP-hydrolysis motif for inflammasome inhibition.
机构信息
Institute for Molecular Bioscience and IMB Centre for Inflammation and Disease Research, The University of Queensland, St Lucia, Queensland, Australia.
Institute for Glycomics, Griffith University, Gold Coast, Queensland, Australia.
出版信息
Nat Chem Biol. 2019 Jun;15(6):556-559. doi: 10.1038/s41589-019-0277-7. Epub 2019 May 13.
Inhibition of the NLRP3 inflammasome is a promising strategy for the development of new treatments for inflammatory diseases. MCC950 is a potent and specific small-molecule inhibitor of the NLRP3 pathway, but its molecular target is not defined. Here, we show that MCC950 directly interacts with the Walker B motif within the NLRP3 NACHT domain, thereby blocking ATP hydrolysis and inhibiting NLRP3 activation and inflammasome formation.
抑制 NLRP3 炎性小体是开发炎症性疾病新疗法的有前途的策略。MCC950 是 NLRP3 途径的有效且特异性的小分子抑制剂，但它的分子靶标尚未确定。在这里，我们表明 MCC950 直接与 NLRP3 NACHT 结构域内的 Walker B 基序相互作用，从而阻断 ATP 水解并抑制 NLRP3 激活和炎性小体形成。
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