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通过调节群体感应调节子 SmcR 对 的表型发现抗病毒剂。

Phenotypic Discovery of an Antivirulence Agent against via Modulation of Quorum-Sensing Regulator SmcR.

机构信息

Department of Agricultural Biotechnology, Seoul National University, Seoul 08826, Korea.

CRI Center for Chemical Proteomics, Department of Chemistry, Seoul National University, Seoul 08826, Korea.

出版信息

ACS Infect Dis. 2020 Nov 13;6(11):3076-3082. doi: 10.1021/acsinfecdis.0c00587. Epub 2020 Oct 21.

Abstract

An antivirulence agent against named quoromycin (QM) was discovered by a phenotype-based elastase inhibitor screening. Using the fluorescence difference in two-dimensional gel electrophoresis (FITGE) approach, SmcR, a quorum-sensing master regulator and homologue of LuxR, was identified as the target protein of QM. We confirmed that the direct binding of QM to SmcR inhibits the quorum-sensing signaling pathway by controlling the DNA-binding affinity of SmcR and thus effectively alleviates the virulence of and . QM can be regarded as a novel antivirulence agent for the treatment of infection.

摘要

一种名为 quoromycin (QM) 的抗毒剂是通过基于表型的弹性蛋白酶抑制剂筛选发现的。使用二维凝胶电泳荧光差异(FITGE)方法,SmcR,一种群体感应主调节剂和 LuxR 的同源物,被鉴定为 QM 的靶蛋白。我们证实,QM 与 SmcR 的直接结合通过控制 SmcR 的 DNA 结合亲和力来抑制群体感应信号通路,从而有效减轻 和 的毒力。QM 可以被视为治疗 感染的新型抗毒剂。

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