药物发现
G蛋白偶联受体
计算生物学
虚拟筛选
药物开发
药品
生物
信号转导
生物信息学
遗传学
药理学
作者
Hanting Yang,Yongfu Wang,Wei Liu,Taiping He,Jia‐Yu Liao,Zhong‐Zhi Qian,Jing‐Hao Zhao,Zhaotong Cong,Dan Sun,Zhixiang Liu,Can Wang,Lingping Zhu,Shilin Chen
标识
DOI:10.1016/j.apsb.2024.06.023
摘要
G protein-coupled receptors (GPCRs) are pivotal in mediating diverse physiological and pathological processes, rendering them promising targets for drug discovery. GPCRs account for about 40% of FDA-approved drugs, representing the most successful drug targets. However, only approximately 15% of the 800 human GPCRs are targeted by market drugs, leaving numerous opportunities for drug discovery among the remaining receptors. Cell expression systems play crucial roles in the GPCR drug discovery field, including novel target identification, structural and functional characterization, potential ligand screening, signal pathway elucidation, and drug safety evaluation. Here, we discuss the principles, applications, and limitations of widely used cell expression systems in GPCR-targeted drug discovery, GPCR function investigation, signal pathway characterization, and pharmacological property studies. We also propose three strategies for constructing genome-wide pan-GPCR cell libraries, which will provide a powerful platform for GPCR ligand screening, and facilitate the study of GPCR mechanisms and drug safety evaluation, ultimately accelerating the process of GPCR-targeted drug discovery.
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