LED209 is a potent small molecule inhibitor of bacterial receptor QseC, is a potent prodrug that is highly selective for QseC.
信号通路
Anti-infection
靶点
Antibacterial
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IC50
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体外研究
LED209 has desirable pharmacokinetics and does not present toxicity in vitro and in rodents. This is a unique antivirulence approach, with a proven broad-spectrum activity against multiple Gram-negative pathogens that cause mammalian infections.The LED209 QseC inhibitor has a unique mode of action by acting as a prodrug scaffold to deliver a warhead that allosterically modifies QseC, impeding virulence in several Gram-negative pathogens. LED209 is QseC sensor kinase inhibitor , as a potential lead compound to combat infections with Legionella or Mycobacterium spp. LED209 inhibits the binding of signals to QseC, preventing its autophosphorylation and consequently inhibiting QseC-mediated activation of virulence gene expression. LED209 inhibits EHEC virulence traits in vitro. LED209 markedly inhibits the virulence of several pathogens in animals. Inhibition of signaling offers a strategy for the development of broad-spectrum antimicrobial drugs.
体内研究
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临床实验
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特征
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相关实验数据(此数据来自于公开文献,联迈生物并不保证其有效性):
酶活性检测实验
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细胞实验
细胞系
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浓度
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处理时间
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方法
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动物实验
动物模型
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配制
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剂量
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给药方式
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参考文献: 1. CurtismM, et al. MBio. 2014 Nov 11, 5(6), e02165. 2. Harrison CF, et al. Microbiology. 2015 Jul, 161(7), 1392-406. 3. Rasko DA, et al. Science. 2008 Aug 22, 321(5892), 1078-80. 包装清单: