| 引用本文: | 李名伟,张淼,许玮华,王冰.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[J].中国现代应用药学,2022,39(19):2557-2566. |
| LI Mingwei,ZHANG Miao,XU Weihua,Wang Bing.Research Progress in Function and Structure of Transient Receptor Potential Melastatin-Related 8 and Its Chemical Modulators[J].Chin J Mod Appl Pharm(中国现代应用药学),2022,39(19):2557-2566. |
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| 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 |
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李名伟1,2, 张淼3, 许玮华1,2,4, 王冰4
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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
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| 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Ca2+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。 |
| 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 |
| DOI：10.13748/j.cnki.issn1007-7693.2022.19.019 |
| 分类号:R915 |
| 基金项目:上海市科学技术委员会科技计划项目(21ZR1475200) |
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| Research Progress in Function and Structure of Transient Receptor Potential Melastatin-Related 8 and Its Chemical Modulators |
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LI Mingwei1,2, ZHANG Miao3, XU Weihua1,2,4, Wang Bing4
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1.Yangtze Delta Drug Advanced Research Institute, Yangtze Delta Pharmaceutical College, Nantong 226100, China;2.School of Pharmacy, Anhui University of Chinese Medicine, Hefei 230031, China;3.School of Pharmacy, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China;4.Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China
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| Abstract: |
| 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 Ca2+ 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. |
| Key words: transient receptor potential melastatin-related 8 channel chemical modulator Ca2+concentration therapeutic target |
