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Design, Synthesis and Evaluation of an NLRP3 Inhibitor Diazirine Photoaffinity Probe
Tetrahedron Letters ( IF 1.5 ) Pub Date : 2020-03-16 , DOI: 10.1016/j.tetlet.2020.151849
James R. Hill , Rebecca C. Coll , Kate Schroder , Avril A.B. Robertson

The NLRP3 inhibitor MCC950/CRID3 ameliorates a remarkable number of inflammatory disorders in animal models. Herein we describe a trifluoromethyl phenyl diazirine (TPD) photoaffinity probe, called TPD-950-Br, to probe the molecular interactions of MCC950. We show that TPD-950-Br covalently captures proximal species upon photo-activation and inhibits IL-1β production in an NLRP3 inhibitor assay.



中文翻译:

NLRP3抑制剂重氮嗪光亲和探针的设计,合成和评估

NLRP3抑制剂MCC950 / CRID3可改善动物模型中的大量炎症性疾病。在本文中,我们描述了一种称为TPD-950-Br的三氟甲基苯基重氮(TPD)光亲和探针,以探测MCC950的分子相互作用。我们显示,TPD-950-Br在NLRP3抑制剂检测中共激活并在光活化后捕获近端物质,并抑制IL-1β的产生。

更新日期:2020-03-19
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