瞬时受体电位8型的功能结构及其化学调节剂的研究进展  

Research Progress in Function and Structure of Transient Receptor Potential Melastatin-Related 8 and Its Chemical Modulators

作　　者：李名伟 张淼 许玮华 王冰 LI Mingwei;ZHANG Miao;XU Weihua;Wang Bing(Yangtze Delta Drug Advanced Research Institute,Yangtze Delta Pharmaceutical College,Nantong 226100,China;School of Pharmacy,Anhui University of Chinese Medicine,Hefei 230031,China;School of Pharmacy,Shanghai University of Traditional Chinese Medicine,Shanghai 201203,China;Shanghai Institute of Materia Medica,Chinese Academy of Sciences,Shanghai 201203,China)

机构地区：[1]长三角药物高等研究院,长三角药学高等工程院,江苏南通226100 [2]安徽中医药大学药学院,合肥230031 [3]上海中医药大学中药学院,上海201203 [4]中国科学院上海药物研究所,上海201203

出　　处：《中国现代应用药学》2022年第19期2557-2566,共10页Chinese Journal of Modern Applied Pharmacy

基　　金：上海市科学技术委员会科技计划项目(21ZR1475200)。

摘　　要：瞬时受体电位8型(transient receptor potential melastatin-related 8,TRPM8)是一种非选择性钙离子通道,其功能异常或缺失会导致多种疾病。TRPM8参与生物体的体温调节、肿瘤、炎症、疼痛和哮喘等生理及病理活动,特别是在肿瘤治疗过程中,TRPM8常被用作治疗的潜在靶点。大部分化学调节剂是通过影响细胞内Ca^(2+)浓度平衡来激活TRPM8通道。本文对TRPM8通道的结构、功能及其对不同疾病的调节作用等进行归纳及分析,为TRPM8作为临床治疗及新药开发靶点提供借鉴。Transient receptor potential melastatin-related 8(TRPM8)is a non-selective calcium channel whose abnormal function or deficiency leads to a variety of diseases.TRPM8 is involved in the physiological and pathological activities of organisms such as thermoregulation,tumors,inflammation,pain and asthma.Especially TRPM8 is often used as a potential target for therapy during tumor treatment.Most chemomodulators activate TRPM8 channels by affecting the intracellular Ca^(2+) concentration balance.This paper summarizes and analyzes the structure and function of TRPM8 channels and their modulatory effects on different diseases to provide a reference for TRPM8 as a target for clinical treatment and new drug development.

关 键 词：瞬时受体电位8型通道 化学调节剂 Ca2+浓度 治疗靶点 

分 类 号：R915[医药卫生—微生物与生化药学]