| 梁珂维,王 康,蔡 芬,梅凯迪,王媛媛,姚 镜.靶向TRPA1通道的药物开发研究进展[J].,2019,19(5):996-1000 |
| 靶向TRPA1通道的药物开发研究进展 |
| Development and Research Progress of Drug Targeting TRPA1 Channel |
| 投稿时间：2018-05-23 修订日期：2018-06-18 |
| DOI：10.13241/j.cnki.pmb.2019.05.045 |
| 中文关键词: TRPA1通道 生理调节 药物开发 |
| 英文关键词: TRPA1 Chanel Physiological regulation Drug development |
| 基金项目:湖北省自然科学基金项目（2015CFA095, 2017CFA063） |
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| 中文摘要: |
| 摘要：瞬时受体势（Transient Receptor Potential，TRP）通道是一种非选择性阳离子通道，广泛分布于神经和非神经细胞中。TRPA1作为TRP通道的一个亚型，是一种温度敏感型的TRP通道，其温度激活阈值与物种有关。在小鼠体内，TRPA1可以被低温（<17 ℃）激活，然而在绿安乐蜥体内TRPA1的温度激活阈值却达到了35.8 ℃。TRPA1除了可以响应温度刺激之外，还可以被化学刺激、机械刺激等多种理化方式激活。TRPA1基因的功能获得性突变会导致家族性发作性疼痛综合征。由于TRPA1在温度感知、痛觉产生、哮喘、瘙痒等众多生理与病理过程中发挥着重要作用，因而TRPA1受到了广泛关注。文章总结TRPA1通道的生理特性，并对其参与的机体生理调节及靶向TRPA1通道的药物开发现状和前景进行综述，以期为临床上治疗相关疾病提供理论基础。 |
| 英文摘要: |
| ABSTRACT: The Transient receptor potential (TRP) channel is a non selective cation channel, and is widely distributed in neuronal and non neuronal cells. As a subtype of TRP channel, TRPA1 is a temperature sensitive TRP channel which temperature activation threshold is related to species. TRPA1 in mouse is activated by cold temperature (<17 ℃), however TRPA1 in the green lizard is sensi- tive to warm temperature(35.8 ℃). In addition to the response to the temperature, TRPA1 can also be activated by chemical stimuli, me- chanical stimulation and other physical and chemical means. A recent study shows that a gain-of-function mutation in TRPA1 can lead to familial paroxysmal pain syndrome. Due to TRPA1 has been proposed to function in many physiological and pathological processes such as temperature perception, pain producing, asthma and itching, TRPA1 has become one of the most intensively studied ion channels and attracted wide attention. In this review, we summarize the biophysical characteristics of TRPA1 channels, and discuss recent advances in our understanding of TRPA1 physiology, pharmacology, and molecular function in order to provide theoretical basis for clinical treat- ment of related diseases. |
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