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靶向Toll样受体4的小分子调节剂

张晓铮 ,  张天舒 ,  崔凤超 ,  李云琦 ,  彭英华 ,  王晓辉

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引用本文: 张晓铮, 张天舒, 崔凤超, 李云琦, 彭英华, 王晓辉. 靶向Toll样受体4的小分子调节剂[J]. 应用化学, 2016, 33(8): 876-886. doi: 10.11944/j.issn.1000-0518.2016.08.160206 shu
Citation:  ZHANG Xiaozheng, ZHANG Tianshu, CUI Fengchao, LI Yunqi, PENG Yinghua, WANG Xiaohui. Toll-like Receptor 4 Small Molecule Modulators[J]. Chinese Journal of Applied Chemistry, 2016, 33(8): 876-886. doi: 10.11944/j.issn.1000-0518.2016.08.160206 shu

靶向Toll样受体4的小分子调节剂

  • 1.

    a 中国科学院长春应用化学研究所, 化学生物学实验室 长春 130022;

  • 2.

    b 中国科学院大学 北京 100039;

  • 3.

    c 中国科学院上海药物研究所, 新药研究国家重点实验室 上海 201203;

  • 4.

    d 中国科学院长春应用化学研究所, 合成橡胶重点实验室 长春 130022;

  • 5.

    e 中国农业科学院特产研究所, 吉林省特种动物分子生物学重点实验室 长春 130112

    • 通讯作者: 王晓辉,研究员; Tel:0431-85262249; Fax:0431-85262240; E-mail:xiaohui.wang@ciac.ac.cn; 研究方向:药物化学生物学
  • 基金项目:

    国家自然科学基金（21543013) 

    中国科学院上海药物研究所新药国家重点实验室开放基金（SIMM1601KF-17) 

    吉林省自然科学基金（20160101211JC) 

    吉林省留学人员科技创新创业项目择优资助和中国科学院率先行动百人计划、NSFC-广东联合基金（第二期）超级计算科学应用研究专项资助、国家超级计算广州中心支持项目 

摘要: Toll样受体（Toll-like receptors，TLRs）是进化保守的天然免疫模式识别受体，能够识别外源的病原菌相关分子模式（Pathogen-associated molecular patterns，PAMPs）、内源的损害相关分子模式（Damage-associated molecular patterns，DAMPs）和异源物相关分子模式（Xenobiotic-associated molecular patterns），诱导炎症免疫反应。其中，TLR4（Toll-like receptor 4）是目前研究最为广泛的Toll样受体之一，TLR4是脂多糖（lipopoiysaccharide，LPS）的主要受体，LPS激活的TLR4信号通路在炎症信号的传递中发挥着重要作用，而此信号转导需要通过LPS与TLR4及其附属蛋白髓样分化因子2（myeloid differentiation factor 2，MD-2）的相互作用来实现。因此，TLR4/MD-2成为炎症反应和免疫调控最重要的研究热点。本文综述靶向TLR4/MD-2的小分子激动剂和抑制剂的研究进展，以进一步理解TLR4小分子调节剂与其相互作用的复杂性，帮助靶向TLR4/MD-2的免疫调节剂药物发现。

English

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  • 收稿日期:  2016-05-18
  • 网络出版日期:  2016-06-06
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