GPR52——治疗神经系统疾病的新靶点

GPR52——A New Target for Central Nervous System Diseases

GPR52是G蛋白偶联受体家族的一员,它的内源性配体至今仍未发现。但其在大脑纹状体中高度表达,能够抑制多巴胺D_(2)受体并通过促进神经细胞中cAMP的积累激活多巴胺D_(1)受体和NMDA受体,成为治疗精神分裂症的潜在靶点。同时GPR52受体反向激动剂被证明不仅可以降低mHTT的水平而且能够治疗小鼠模型中的亨廷顿病相关症状。

GPR52 is a member of the G protein-coupled receptor family, and its endogenous ligand has not been found so far. However, it is highly expressed in the striatum species of the brain, and can inhibit the dopamine D_(2) receptor and activate the dopamine D_(1) receptor and NMDA receptor by promoting the cAMP level of nerve cells, thus becoming a potential target for the treatment of schizophrenia. Meanwhile, GPR52 receptor inverse agonists have been shown to not only reduce mHTT levels but also treat symptoms associated with Huntington’s disease in a mouse model.