Department of Agricultural Biotechnology, Seoul National University, Seoul 08826, Korea.
CRI Center for Chemical Proteomics, Department of Chemistry, Seoul National University, Seoul 08826, Korea.
ACS Infect Dis. 2020 Nov 13;6(11):3076-3082. doi: 10.1021/acsinfecdis.0c00587. Epub 2020 Oct 21.
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.
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。