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    • 76. 发明授权
    • Methods for identification of eicosapentaenoic acid analogs using anti-inflammatory receptors
    • 使用抗炎症受体鉴定二十碳五烯酸类似物的方法
    • US07803557B2
    • 2010-09-28
    • US12045427
    • 2008-03-10
    • Charles N. SerhanMakoto Arita
    • Charles N. SerhanMakoto Arita
    • G01N33/53G01N33/567
    • G01N33/5047G01N33/5023G01N33/5032G01N33/5041G01N33/505G01N33/566G01N2333/4703G01N2333/715G01N2333/726G01N2500/04
    • The present invention is directed to methods for the identification and uses of a receptors that interact with anti-inflammatory compounds derived from eicosapentaenoic acid (EPA). The receptors are of the G-protein coupled receptor (GPCR) family, and are useful to screen candidate substances for anti-inflammatory activity, especially substances that are analogs of EPA. Such analogs are termed “resolvins”; and are typically di- and tri-hydroxy EPA analogs. One analog herein denoted Resolvin E1 was identified in humans and prepared by total synthesis. In nanomolar range Resolvin E1 reduces dermal inflammation, peritonitis, dendritic cells (DCs) migration and IL-12 production. Also described herein is a receptor denoted Reso ER1 that interacts with Resolvin E1 to attenuate cytokine induced activation of inflammatory pathways mediated by transcription factor (NF)-kB. Treatment of DCs with small-interfering RNA specific for ResoE1 eliminated the ligand's ability to regulate IL-12. Assays of anti-inflammatory activity based on these discoveries are also described.
    • 本发明涉及鉴定和使用与二十碳五烯酸(EPA)衍生的抗炎化合物相互作用的受体的方法。 受体是G蛋白偶联受体(GPCR)家族,可用于筛选候选物质的抗炎活性,特别是类似于EPA的物质。 这样的类似物被称为“溶解素”; 并且通常是二羟基和三羟基EPA类似物。 在人类中鉴定了一种在本文中称为Resolvin E1的类似物,并通过全合成制备。 在纳摩尔范围内,Resolvin E1可减少皮肤炎症,腹膜炎,树突细胞(DCs)迁移和IL-12的产生。 本文还描述了称为Reso ER1的受体,其与Resolvin E1相互作用以减弱由转录因子(NF)-kB介导的炎症途径的细胞因子诱导的活化。 用特异于ResoE1的小干扰RNA处理DC消除了配体调节IL-12的能力。 还描述了基于这些发现的抗炎活性测定。
    • 77. 发明授权
    • Methods for identification and uses of anti-inflammatory receptors for eicosapentaenoic acid analogs
    • 用于二十碳五烯酸类似物的抗炎症受体的鉴定和使用方法
    • US07341840B2
    • 2008-03-11
    • US11218281
    • 2005-09-01
    • Charles N. SerhanMakoto Arita
    • Charles N. SerhanMakoto Arita
    • G01N33/53G01N33/567
    • G01N33/5047G01N33/5023G01N33/5032G01N33/5041G01N33/505G01N33/566G01N2333/4703G01N2333/715G01N2333/726G01N2500/04
    • The present invention is directed to methods for the identification and uses of receptors that interact with anti-inflammatory compounds derived from eicosapentaenoic acid (EPA). The receptors are of the G-protein coupled receptor (GPCR) family, and are useful to screen candidate substances for anti-inflammatory activity, especially substances that are analogs of EPA. Such analogs are termed “resolvins”; and are typically di- and tri-hydroxy EPA analogs. One analog herein denoted Resolvin E1 was identified in humans and prepared by total synthesis. In nanomolar range Resolvin E1 reduces dermal inflammation, peritonitis, dendritic cells (DCs) migration and IL-12 production. Also described herein is a receptor denoted Reso ER1 that interacts with Resolvin E1 to attenuate cytokine induced activation of inflammatory pathways mediated by transcription factor (NF)-kB. Treatment of DCs with small-interfering RNA specific for ResoE1 eliminated the ligand's ability to regulate IL-12. Assays of anti-inflammatory activity based on these discoveries are also described.
    • 本发明涉及鉴定和使用与二十碳五烯酸(EPA)衍生的抗炎化合物相互作用的受体的方法。 受体是G蛋白偶联受体(GPCR)家族,可用于筛选候选物质的抗炎活性,特别是类似于EPA的物质。 这样的类似物被称为“溶解素”; 并且通常是二羟基和三羟基EPA类似物。 在人类中鉴定了一种在本文中称为Resolvin E1的类似物,并通过全合成制备。 在纳摩尔范围内,Resolvin E1可减少皮肤炎症,腹膜炎,树突细胞(DCs)迁移和IL-12的产生。 本文还描述了称为Reso ER1的受体,其与Resolvin E1相互作用以减弱由转录因子(NF)-kB介导的炎症途径的细胞因子诱导的活化。 用特异于ResoE1的小干扰RNA处理DC消除了配体调节IL-12的能力。 还描述了基于这些发现的抗炎活性测定。