Department of Medicine, University of Colorado Denver, Aurora, CO.
J Cardiovasc Pharmacol. 2019 Oct;74(4):285-296. doi: 10.1097/FJC.0000000000000718.
NLRP3 is a cytosolic receptor member of the nucleotide-binding oligomerization domain NOD-like receptor family that surveys the intracellular environment for the presence of infection, pathogens, and metabolic alarms. Although the surveillance activity of NLRP3 is required to protect the host from several pathogens, uncontrolled activity can be detrimental to the host. Pharmacological and genetic strategies limiting NLRP3 inflammasome activation have been shown to be beneficial in a wide range of experimental models, from common pathologies such as arthritis, cardiovascular disease, and metabolic syndromes to rare genetic disorders such as cryopyrin-associated periodic syndrome. Thus, compounds that prevent NLRP3 inflammasome activation are of common interest with relevant therapeutic potential. The focus of this review is recent developments in NLRP3 inflammasome inhibitors.
NLRP3 是细胞溶质受体成员核苷酸结合寡聚结构域 NOD 样受体家族，用于检测细胞内环境中是否存在感染、病原体和代谢警报。尽管 NLRP3 的监测活动对于宿主抵御多种病原体是必需的，但不受控制的活动可能对宿主有害。已经表明，限制 NLRP3 炎性小体激活的药理学和遗传学策略在广泛的实验模型中是有益的，从常见的病理学如关节炎、心血管疾病和代谢综合征到罕见的遗传疾病如 Cryopyrin 相关周期性综合征。因此，预防 NLRP3 炎性小体激活的化合物具有共同的治疗潜力。本综述的重点是 NLRP3 炎性小体抑制剂的最新进展。
