State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macao, China.
State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macao, China.
Drug Discov Today. 2021 Jun;26(6):1394-1408. doi: 10.1016/j.drudis.2021.02.018. Epub 2021 Feb 23.
Innate immunity serves as a first line of defence against danger signals, invading pathogens and microbes. The inflammasomes, as pattern recognition receptors, sense these danger signals to initiate pro-inflammatory cascades. The nucleotide-binding domain leucine-rich repeat and pyrin domain containing receptor 3 (NLRP3) inflammasome is the most well characterised inflammasome, and its aberrant activation is implicated in many inflammatory diseases. In the past decade, targeting the NLRP3 inflammasome has become an emerging strategy for inflammatory diseases. To avoid off-target immunosuppressive effects, specific NLRP3 inhibitors have been developed and show promising therapeutic effects. This review discusses the therapeutic effects and clinical perspectives of specific NLRP3 inhibitors, as well as recent progress in the development of these inhibitors for the treatment of inflammatory diseases.
先天免疫作为抵御危险信号、入侵病原体和微生物的第一道防线。模式识别受体炎性小体感知这些危险信号，启动促炎级联反应。核苷酸结合域富含亮氨酸重复和吡喃结构域受体 3（NLRP3）炎性小体是最具特征性的炎性小体，其异常激活与许多炎症性疾病有关。在过去的十年中，针对 NLRP3 炎性小体已成为炎症性疾病的一种新兴治疗策略。为了避免脱靶的免疫抑制作用，已经开发出了特异性 NLRP3 抑制剂，并显示出有前景的治疗效果。本文讨论了特异性 NLRP3 抑制剂的治疗效果和临床前景，以及这些抑制剂在治疗炎症性疾病方面的最新进展。
