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Strategies for Targeting the NLRP3 Inflammasome in the Clinical and Preclinical Space
Journal of Medicinal Chemistry ( IF 7.3 ) Pub Date : 2020-12-22 , DOI: 10.1021/acs.jmedchem.0c01307
Adam G. Schwaid 1 , Kerrie B. Spencer 1
Affiliation  

Inhibiting the NLRP3 inflammasome mediates inflammation in an extensive number of preclinical models. As excitement in this field has grown, several companies have recently initiated testing of direct NLRP3 inhibitors in the clinic. At the same time, the NLRP3 inflammasome is part of a larger pro-inflammatory pathway, whose modulation is also being explored. Multiple targets in this pathway are already impinged upon by molecules that have been through clinical trials. These data, informed by the growing mechanistic understanding of the NLRP3 inflammasome in the preclinical space, provide a rich backdrop to assess the current state of the field. Here we explore attempts to inhibit the NLRP3 inflammasome in light of clinical and preclinical data around efficacy and safety.

中文翻译:

在临床和临床前空间中靶向NLRP3炎性小体的策略

在大量临床前模型中,抑制NLRP3炎性体可介导炎症。随着这一领域的热情日渐浓厚,几家公司最近开始在临床中测试直接NLRP3抑制剂。同时,NLRP3炎性小体是更大的促炎途径的一部分,该途径也正在研究中。已经通过临床试验的分子已经对该途径中的多个靶标产生了影响。这些数据来自对临床前空间中NLRP3炎性小体的日益增长的机械理解,为评估该领域的当前状况提供了丰富的背景。在这里,我们根据疗效和安全性方面的临床和临床前数据,探索抑制NLRP3炎性体的尝试。
更新日期:2021-01-14
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