关于5-HT 2A受体关键氨基酸位点的研究进展

Research progress on key amino acid sites of 5-HT 2A receptor

5-HT 2A受体作为许多精神活性药物如致幻剂、抗抑郁药、抗焦虑药和非典型抗精神病药等的作用靶点,一直是神经精神药理学领域研究热点。5-HT 2A受体的某些关键氨基酸位点对于维持受体的特定构象、偶联不同G蛋白以及行使相应特定功能等起重要作用。进一步的研究显示,突变这些特定的氨基酸位点,能够引起相应配体的亲和力、效能等变化。同时,5-HT 2A受体作为一种典型的G蛋白偶联受体,其结构域中不同的氨基酸位点能与不同配体产生相互作用,引起受体相应的动态结构变化,从而影响受体的功能。因此,研究5-HT 2A受体结构和功能与关键氨基酸位点的关系,对于相关精神疾病的治疗以及设计高效低毒的新型药物具有重要意义。

As the target of many psychoactive drugs such as hallucinogens,antidepressants,anxiolytics and atypical antipsychotics,5-HT 2A receptor has been a research hotspot in the field of neuropsychopharmacology.Some key amino acid sites of 5-HT 2A receptor play an important role in maintaining the specific conformation of receptor,coupling different G proteins,and exercising corresponding specific functions.Further studies have shown that mutations of these specific amino acid sites can cause changes in the affinity and potency of the corresponding ligands.Moreover,5-HT 2A receptor is a typical G-protein-coupled receptor,and different amino acid sites in its structural domain can interact with different ligands,causing corresponding dynamic structural changes of the receptor,thus affecting the receptor function.Therefore,studying the relationship between the structure and function of 5-HT 2A receptor and key amino acid sites is of great significance for the treatment of related psychiatric diseases and the design of new drugs with high efficiency and low toxicity.