• 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Chemistry: A European journal >Chemoproteomic Approach to Explore the Target Profile of GPCR ligands: Application to 5-HT1A and 5-HT6 Receptors
【24h】

Chemoproteomic Approach to Explore the Target Profile of GPCR ligands: Application to 5-HT1A and 5-HT6 Receptors

机译：化学旋转研究GPCR配体目标概况的方法：在5-HT1A和5-HT6受体中的应用

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

Determination of the targets of a compound remains an essential aspect in drug discovery. A complete understanding of all binding interactions is critical to recognize in advance both therapeutic effects and undesired consequences. However, the complete polypharmacology of many drugs currently in clinical development is still unknown, especially in the case of G protein-coupled receptor (GPCR) ligands. In this work we have developed a chemoproteomic platform based on the use of chemical probes to explore the target profile of a compound in biological systems. As proof of concept, this methodology has been applied to selected ligands of the therapeutically relevant serotonin 5HT(1A) and 5-HT6 receptors, and we have identified and validated some of their off-targets. This approach could be extended to other drugs of interest to study the targeted proteome in disease-relevant systems.
机译：化合物靶标的确定仍然是药物发现中必不可少的方面。全面了解所有结合相互作用对于提前识别治疗效果和不良后果至关重要。但是，目前仍在临床开发中的许多药物的完整多药理学仍是未知的，尤其是在G蛋白偶联受体（GPCR）配体的情况下。在这项工作中，我们基于化学探针的使用开发了一个化学旋转平台，以探索化合物在生物系统中的目标谱。作为概念的证明，此方法已应用于治疗相关的血清素5HT（1A）和5-HT6受体的选定配体，我们已经鉴定并验证了它们的一些脱靶靶标。这种方法可以扩展到其他感兴趣的药物，以研究疾病相关系统中的目标蛋白质组。

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