具有潜在逆境作用的瞬时受体电位通道的特性和治疗潜力:关注 TRPC5、TRPM2 和 TRPA1。

Properties and therapeutic potential of transient receptor potential channels with putative roles in adversity: focus on TRPC5, TRPM2 and TRPA1.

机构信息

Institute of Membrane & Systems Biology, Faculty of Biological Sciences, University of Leeds, Leeds, LS2 9JT, UK.

出版信息

Curr Drug Targets. 2011 May;12(5):724-36. doi: 10.2174/138945011795378568.

Abstract

Mammals contain 28 genes encoding Transient Receptor Potential (TRP) proteins. The proteins assemble into cationic channels, often with calcium permeability. Important roles in physiology and disease have emerged and so there is interest in whether the channels might be suitable therapeutic drug targets. Here we review selected members of three subfamilies of mammalian TRP channel (TRPC5, TRPM2 and TRPA1) that show relevance to sensing of adversity by cells and biological systems. Summarized are the cellular and tissue distributions, general properties, endogenous modulators, protein partners, cellular and tissue functions, therapeutic potential, and pharmacology. TRPC5 is stimulated by receptor agonists and other factors that include lipids and metal ions; it heteromultimerises with other TRPC proteins and is involved in cell movement and anxiety control. TRPM2 is activated by hydrogen peroxide; it is implicated in stress-related inflammatory, vascular and neurodegenerative conditions. TRPA1 is stimulated by a wide range of irritants including mustard oil and nicotine but also, controversially, noxious cold and mechanical pressure; it is implicated in pain and inflammatory responses, including in the airways. The channels have in common that they show polymodal stimulation, have activities that are enhanced by redox factors, are permeable to calcium, and are facilitated by elevations of intracellular calcium. Developing inhibitors of the channels could lead to new agents for a variety of conditions: for example, suppressing unwanted tissue remodeling, inflammation, pain and anxiety, and addressing problems relating to asthma and stroke.

摘要

哺乳动物包含 28 种编码瞬时受体电位 (TRP) 蛋白的基因。这些蛋白组装成阳离子通道,通常具有钙通透性。它们在生理学和疾病中的重要作用已经显现出来,因此人们对这些通道是否可能成为合适的治疗药物靶点产生了兴趣。在这里,我们回顾了哺乳动物 TRP 通道(TRPC5、TRPM2 和 TRPA1)三个亚家族的选定成员,这些成员与细胞和生物系统对逆境的感知有关。总结了它们的细胞和组织分布、一般特性、内源性调节剂、蛋白伴侣、细胞和组织功能、治疗潜力和药理学。TRPC5 受受体激动剂和其他因素的刺激,包括脂质和金属离子;它与其他 TRPC 蛋白异聚化,并参与细胞运动和焦虑控制。TRPM2 被过氧化氢激活;它与应激相关的炎症、血管和神经退行性疾病有关。TRPA1 受多种刺激物的刺激,包括芥子油和尼古丁,但也有争议地受到有害的冷和机械压力的刺激;它与疼痛和炎症反应有关,包括在气道中。这些通道的共同特点是它们表现出多模态刺激,其活性受到氧化还原因子的增强,对钙具有通透性,并通过细胞内钙的升高得到促进。开发这些通道的抑制剂可能会导致针对多种疾病的新药物:例如,抑制不需要的组织重塑、炎症、疼痛和焦虑,并解决与哮喘和中风相关的问题。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d17f/3267159/d41917f02085/CDT-12-724_F1.jpg

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