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Methods for Screening TLR4(Toll-like receptor 4) Signaling Inhibitors and Uses Thereof

机译:筛选TLR4(Toll样受体4)信号传导抑制剂的方法及其用途

摘要

The invention is a step for containing the TLR4 (Toll-like receptor 4) signaling inhibitor screening to how the service is: (a) TLR4 (Toll-like receptor 4) or TLR4 extracellular domain on the test material in contact to step; And (b) in the case of a covalent bond to a cysteine ​​residue in the extracellular domain of comprising a step of analyzing whether or not the covalently attached to a cysteine ​​residue in the extracellular domain of the test substance TLR4, the test substances are TLR4 by inhibiting TLR4 oligomerization it is determined by TLR4 signaling inhibitors. The TLR4 signaling inhibitors, more preferably the present invention is a thiol-reactive compound (e.g., SFN) is shared with the cysteine ​​residues present in the TLR4 or TLR4 extracellular domain binding control form a duct (adducts), and a ligand of TLR4-induced to suppress all non-dependent oligomerization - and the oligomerization of TLR4 ligand. Thus, (e.g., SFN) TLR4 signaling inhibitor or an efficacy enhancer of the present invention, compositions comprising as an active ingredient was significantly attenuated the inflammatory response is effective in the treatment of inflammatory diseases the reduction of improved and swelling of the skin, even effective. ;
机译:本发明是一个包含TLR4(Toll样受体4)信号抑制剂筛选的步骤,以了解其作用是如何的:并且(b)在与细胞外结构域中的半胱氨酸残基共价结合的情况下,包括分析受试物质TLR4在细胞外结构域中是否与半胱氨酸残基共价连接的步骤,被测物质是通过抑制TLR4的低聚而形成的TLR4,这是由TLR4信号抑制剂确定的。 TLR4信号抑制剂,更优选本发明是硫醇反应性化合物(例如SFN)与存在于TLR4或TLR4细胞外域结合控制通道中的半胱氨酸残基共享的通道(加合物),以及TLR4诱导抑制所有非依赖性寡聚-以及TLR4配体的寡聚。因此,本发明的(例如SFN)TLR4信号传导抑制剂或功效增强剂,包含作为活性成分的组合物被显着减弱了炎症反应,对于治疗炎症疾病是有效的,甚至可以减少皮肤的改善和肿胀,甚至有效。 ;

著录项

  • 公开/公告号KR101263757B1

    专利类型

  • 公开/公告日2013-05-14

    原文格式PDF

  • 申请/专利权人

    申请/专利号KR20100038895

  • 发明设计人 김소영;이주영;

    申请日2010-04-27

  • 分类号G01N33/68;G01N33/15;C07K14/705;

  • 国家 KR

  • 入库时间 2022-08-21 16:25:13

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