Vortherms Timothy A, Roth Bryan L
Department of Biochemistry, Case Western Reserve University School of Medicine, Cleveland, OH 44106-4935, USA.
IDrugs. 2005 Jun;8(6):491-6.
An estimated 50% of currently marketed drugs target G protein-coupled receptors (GPCRs) for a wide variety of indications, including central nervous system (CNS) disorders. Although drug discovery efforts have focused on GPCRs, less than 10% of GPCRs are currently used as drug targets. Thus, GPCRs continue to represent a significant opportunity for future CNS drug development. Identifying the molecular targets of psychoactive compounds may result in the elucidation of novel targets for CNS drug discovery. This commentary will describe discovery-based approaches and provide several recent examples of novel ligand-receptor interactions discovered through systematic screening of the 'receptorome'.
据估计，目前市面上约50%的药物针对G蛋白偶联受体（GPCR），用于治疗包括中枢神经系统（CNS）疾病在内的多种适应症。尽管药物研发工作一直聚焦于GPCR，但目前只有不到10%的GPCR被用作药物靶点。因此，GPCR仍然是未来中枢神经系统药物开发的重要机会。确定精神活性化合物的分子靶点可能会阐明中枢神经系统药物发现的新靶点。本评论将描述基于发现的方法，并提供通过对“受体组”进行系统筛选发现的新型配体-受体相互作用的几个最新例子。
