Research progress on key amino acid sites of 5-HT2A receptor
- VernacularTitle:关于5-HT2A受体关键氨基酸位点的研究进展
- Author:
Lu-Lu XIE
1
;
Xiao-Qian LIU
;
Rui-Bin SU
;
Yu-Ting LI
;
Bo TAN
Author Information
- Keywords: 5-HT2A receptor; G protein-coupled receptor; ami-no acid sites; interactions; molecular docking; molecular mech-anism
- From: Chinese Pharmacological Bulletin 2024;40(11):2001-2004
- CountryChina
- Language:Chinese
- Abstract: As the target of many psychoactive drugs such as hal-lucinogens,antidepressants,anxiolytics and atypical antipsychot-ics,5-HT2A receptor has been a research hotspot in the field of neuropsychopharmacology.Some key amino acid sites of 5-HT2A receptor play an important role in maintaining the specific con-formation of receptor,coupling different G proteins,and exerci-sing 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-HT2A receptor is a typical G-protein-coupled recep-tor,and different amino acid sites in its structural domain can in-teract with different ligands,causing corresponding dynamic structural changes of the receptor,thus affecting the receptor function.Therefore,studying the relationship between the struc-ture and function of 5-HT2A receptor and key amino acid sites is of great significance for the treatment of related psychiatric dis-eases and the design of new drugs with high efficiency and low toxicity.
