...
  • 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Proceedings of the National Academy of Sciences of the United States of America >Mimics of the binding sites of opioid receptors obtained by molecular imprinting of enkephalin and morphine.
【24h】

Mimics of the binding sites of opioid receptors obtained by molecular imprinting of enkephalin and morphine.

机译：通过脑啡肽和吗啡的分子印迹获得的阿片样物质受体结合位点的模拟物。

获取原文
获取原文并翻译 | 示例
           
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

Molecular imprinting of morphine and the endogenous neuropeptide [Leu5]enkephalin (Leu-enkephalin) in methacrylic acid-ethylene glycol dimethacrylate copolymers is described. Such molecular imprints possess the capacity to mimic the binding activity of opioid receptors. The recognition properties of the resultant imprints were analyzed by radioactive ligand binding analysis. We demonstrate that imprinted polymers also show high binding affinity and selectivity in aqueous buffers. This is a major breakthrough for molecular imprinting technology, since the binding reaction occurs under conditions relevant to biological systems. The antimorphine imprints showed high binding affinity for morphine, with Kd values as low as 10(-7) M, and levels of selectivity similar to those of antibodies. Preparation of imprints against Leu-enkephalin was greatly facilitated by the use of the anilide derivative rather than the free peptide as the print molecule, due to improved solubility in the polymerization mixture. Free Leu-enkephalin was efficiently recognized by this polymer (Kd values as low as 10(-7) M were observed). Four tetra- and pentapeptides, with unrelated amino acid sequences, were not bound. The imprints showed only weak affinity for two D-amino acid-containing analogues of Leu-enkephalin. Enantioselective recognition of the L-enantiomer of phenylalanylglycine anilide, a truncated analogue of the N-terminal end of enkephalin, was observed.
机译：描述了甲基丙烯酸-乙二醇二甲基丙烯酸酯共聚物中吗啡和内源性神经肽[Leu5]脑啡肽（Leu-脑啡肽）的分子印迹。这样的分子印迹具有模拟阿片受体的结合活性的能力。通过放射性配体结合分析来分析所得印迹的识别特性。我们证明，印迹聚合物还显示出在水性缓冲液中的高结合亲和力和选择性。这是分子印迹技术的重大突破，因为结合反应发生在与生物系统相关的条件下。抗吗啡印迹显示出对吗啡的高结合亲和力，Kd值低至10（-7）M，选择性水平与抗体相似。由于改进了在聚合混合物中的溶解度，使用苯胺衍生物而不是游离肽作为印刷分子极大地促进了对亮-脑啡肽的印迹的制备。该聚合物可有效识别游离的亮脑啡肽（观察到的Kd值低至10（-7）M）。未结合氨基酸序列不相关的四个四肽和五肽。印迹显示仅对两种亮氨酸脑啡肽的含D-氨基酸的类似物具有弱亲和力。观察到对苯丙氨酰甘氨酸苯胺的L对映体的对映选择性识别，这是脑啡肽N末端的截短类似物。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

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