上海交通大学学报（医学版）

上海交通大学学报（医学版） ›› 2018, Vol. 38 ›› Issue (12): 1484-.doi: 10.3969/j.issn.1674-8115.2018.12.016

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瞬时受体电位 M2型离子通道配体及功能研究进展

刘汉玮，于栋祯，殷善开   

  1. 上海交通大学附属第六人民医院耳鼻咽喉头颈外科，上海 200233
  • 出版日期:2018-12-28 发布日期:2019-01-27
  • 通讯作者: 于栋祯，电子信箱：drdzyu@126.com。
  • 作者简介:刘汉玮 (1992—)，男，博士生；电子信箱： entliuhw@163.com。
  • 基金资助:
    国家自然科学基金（81470690，8150030217）

Advances in function and ligands of transient receptor potential melastain 2 channels

LIU Han-wei, YU Dong-zhen, YIN Shan-kai   

  1. Department of Otorhinolaryngology Head & Neck Surgery, Shanghai Six People’s Hospital, Shanghai Jiao Tong University, Shanghai 200233, China
  • Online:2018-12-28 Published:2019-01-27
  • Supported by:
    National Natural Science Foundation of China, 81470690, 8150030217

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摘要： 瞬时受体电位 M2型（transient receptor potential melastain 2，TRPM2）离子通道作为配体门控的非选择性阳离子通道，在大脑中分布广泛，主要介导 Na+和 Ca2+等阳离子内流，使细胞去极化、胞内 Ca2+浓度升高，进而参与细胞相关的病理生理过程。高 Ca2+浓度或氧化应激等因素直接或间接作用下胞内生成的大量腺苷二磷酸核糖（ adenosine diphosphate ribose，ADPR）与 TRPM2通道的 NUDT9-H结构域结合，从而激活 TRPM2通道。虽然 TRPM2介导许多病理过程，但是现有的 TRPM2通道的拮抗剂尚缺乏特异性，因此通过寻找和研究其特异性拮抗剂有望使 TRPM2通道成为诸多相关疾病的潜在治疗靶点。

关键词: 瞬时受体电位 M2型, 腺苷二磷酸核糖, 氧化应激, 温度调节, 炎症反应

Abstract:

As nonselective cation channels, transient receptor potential melastain 2 (TRPM2) channels are widely distributed in the brain, mainly mediate the inflow of Na+ and Ca2+, leading to cell depolarization and the increasement of intracellular concentration of Ca2+, which are involved in many physiological and pathophysiological processes. Due to increased calcium concentration or oxidative stress, channel gating is inducedeither direct or indirect formation of adenosine diphosphate ribose (ADPR) that binds to a NUDT9 homology domain (NUDT9-H) in the channel. There is no specific TRPM2 antagonist so far. Considering some pathological processes are mediatedTRPM2 channels, the study and discovery of specific TRPM2 blockers might contribute to the effective treatment of many related diseases.

Key words: transient receptor potential melastain 2 (TRPM2), adenosine diphosphate ribose (ADPR), oxidative stress, temperature regulation, inflammatory reaction

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