• 主题
高级搜索  >
历史搜索 清空历史
首页> 外国专利> New crystalline ligand-binding domain of the ecdysone receptor, useful for identifying specific ligands, potentially useful as insecticides and for controlling expression of target gene

New crystalline ligand-binding domain of the ecdysone receptor, useful for identifying specific ligands, potentially useful as insecticides and for controlling expression of target gene

机译：蜕皮激素受体的新结晶配体结合结构域，可用于鉴定特定的配体，潜在用作杀虫剂并控制靶基因的表达

页面导航
  • 摘要
  • 著录项
  • 相似文献

摘要

A ligand-binding domain (LBD) of the ecdysone receptor (EcR), in crystalline form, is new. Independent claims are also included for the following: (1) discovering ligands (I) of EcR, comprising: (a) computer-assisted representation of LBD; and (b) virtual screening of data banks, containing structural data of compounds, to identify structures that interact specifically with LBD; (2) discovering ligands (I) of EcR, comprising: (a) computer-assisted representation of LBD; and (b) computer-assisted modeling of compounds able to interact specifically with LBD; (3) discovering plant-protection agents (II), or effectors (III), comprising: (a) applying method (1) or (2); (b) synthesizing identified compounds; and (c) testing them for biological activity; (4) (II) and (III) identified by method (3); (5) generating protein models of EcR LBD, or of LBD from related nuclear receptors, comprising generating a three-dimensional (3D) image of a first LBD, then of an LBD that has a mutated amino acid sequence; and (6) generating protein models of an EcR ligand binding pocket, or pocket from related receptor, by computer-assisted representation of first the 3D structure for LBD and then of a pocket having the amino acids of a selected organism or other nuclear receptor. ACTIVITY : Insecticide. The agonistic EcR ligand N-(3-methoxy-2-methylbenzoyl)-N'-(2-methoxynicotinoyl)-N'-tert-butyl-hydrazine, identified by modeling to the 3D structure of LBD, was tested against larvae of Spodoptera frugiperda on maize leaf disks. After 7 days exposure to a concentration of 4 parts per million (ppm) of the ligand, all larvae had been killed and mortality was 25 % at ligand concentration 0.8 ppm. MECHANISM OF ACTION : Insecticides identified using LBD modulate development of invertebrates regulated by the ecdysone/juvenile hormone system.
机译：晶体形式的蜕皮激素受体（EcR）的配体结合域（LBD）是新的。还包括以下方面的独立权利要求：（1）发现EcR的配体（I），其包括：（a）LBD的计算机辅助表示; （b）虚拟筛选数据库，其中包含化合物的结构数据，以鉴定与LBD特异性相互作用的结构; （2）发现EcR的配体（I），其包括：（a）LBD的计算机辅助表示; （b）能够与LBD特异性相互作用的化合物的计算机辅助建模; （3）发现植物保护剂（II）或效应子（III），其包括：（a）施用方法（1）或（2）; （b）合成已鉴定的化合物; （c）测试它们的生物活性; （4）通过方法（3）确定的（II）和（III）; （5）从相关核受体产生EcR LBD或LBD的蛋白质模型，包括产生第一个LBD，然后是具有突变的氨基酸序列的LBD的三维（3D）图像; （6）首先通过计算机辅助表示LBD的3D结构，然后通过具有所选生物或其他核受体氨基酸的口袋的计算机辅助表示，生成EcR配体结合口袋或相关受体口袋的蛋白质模型。活动：杀虫剂。通过模拟LBD的3D结构鉴定了激动性EcR配体N-（3-甲氧基-2-甲基苯甲酰基）-N'-（2-甲氧基烟酰基）-N'-叔丁基肼针对斜纹夜蛾幼虫的能力在玉米叶盘上的frugiperda。暴露于浓度为百万分之4（ppm）的配体7天后，所有幼虫均被杀死，配体浓度为0.8 ppm时死亡率为25％。作用机理：使用LBD鉴定的杀虫剂可调节蜕皮激素/少年激素系统调节的无脊椎动物的发育。

著录项

相似文献

  • 专利
  • 外文文献
  • 中文文献
获取专利

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号