综合方法理解 GPCR 上的抗精神病药物作用。
Integrated approaches to understanding antipsychotic drug action at GPCRs.
机构信息
Department of Cell Biology, Duke University Medical Center, Durham, NC 27710, United States.
Department of Psychiatry and Behavioral Sciences, Duke University Medical Center, Durham, NC 27710, United States.
出版信息
Curr Opin Cell Biol. 2014 Apr;27:56-62. doi: 10.1016/j.ceb.2013.11.002. Epub 2013 Dec 14.
Abstract
The G-protein coupled receptor (GPCR) family of genes represents one of the largest druggable families of genes in the human genome. This is evident by the fact that approximately 30% of currently marketed drugs target GPCRs. However, many of these drugs are limited in their clinical potential as they are associated with debilitating side effects-a consequence of our incomplete understanding of their pharmacology and the signaling pathways regulated by GPCRs. Because of the limited range of tools available to resolve these issues, integrated approaches are required to fully understand the pharmacological action of drugs and the biochemical repertoire regulated by GPCRs. In this review we will focus on the action of antipsychotic drugs on certain monoamine GPCRs in the central nervous system (CNS) and the approaches being developed to elucidate their distinct pharmacology.
摘要
G 蛋白偶联受体 (GPCR) 家族的基因是人类基因组中最大的可成药基因家族之一。这一事实显而易见，因为目前市场上约 30%的药物都针对 GPCR。然而，由于我们对其药理学和 GPCR 调节的信号通路的理解不完全，许多这些药物在临床应用上都受到限制，因为它们会产生使人虚弱的副作用。由于解决这些问题的可用工具范围有限，因此需要综合方法来全面了解药物的药理学作用和 GPCR 调节的生化库。在这篇综述中，我们将重点介绍抗精神病药物在中枢神经系统 (CNS) 中某些单胺 GPCR 上的作用，以及正在开发的阐明其独特药理学的方法。
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