Luo Jialie, Hu Hongzhen
The Center for the Study of Itch, Washington University Pain Center, The Department of Anesthesiology, Washington University School of Medicine in St. Louis, St. Louis, MO, USA.
Curr Top Membr. 2014;74:325-64. doi: 10.1016/B978-0-12-800181-3.00012-9.
TRPV3 is a temperature-sensitive transient receptor potential (TRP) ion channel. The TRPV3 protein functions as a Ca(2+)-permeable nonselective cation channel with six transmembrane domains forming a tetrameric complex. TRPV3 is known to be activated by warm temperatures, synthetic small-molecule chemicals, and natural compounds from plants. Its function is regulated by a variety of physiological factors including extracellular divalent cations and acidic pH, intracellular adenosine triphosphate, membrane voltage, and arachidonic acid. TRPV3 shows a broad expression pattern in both neuronal and non-neuronal tissues including epidermal keratinocytes, epithelial cells in the gut, endothelial cells in blood vessels, and neurons in dorsal root ganglia and CNS. TRPV3 null mice exhibit abnormal hair morphogenesis and compromised skin barrier function. Recent advances suggest that TRPV3 may play critical roles in inflammatory skin disorders, itch, and pain sensation. Thus, identification of selective TRPV3 activators and inhibitors could potentially lead to beneficial pharmacological interventions in several diseases. The intent of this review is to summarize our current knowledge of the tissue expression, structure, function, and mechanisms of activation of TRPV3.
瞬时受体电位香草酸亚型3（TRPV3）是一种对温度敏感的瞬时受体电位（TRP）离子通道。TRPV3蛋白作为一种钙离子通透的非选择性阳离子通道发挥作用，它具有六个跨膜结构域，形成一个四聚体复合物。已知TRPV3可被温暖的温度、合成小分子化学物质以及植物中的天然化合物激活。其功能受多种生理因素调节，包括细胞外二价阳离子和酸性pH值、细胞内三磷酸腺苷、膜电压以及花生四烯酸。TRPV3在神经元和非神经元组织中均有广泛的表达模式，包括表皮角质形成细胞、肠道上皮细胞、血管内皮细胞以及背根神经节和中枢神经系统中的神经元。TRPV3基因敲除小鼠表现出毛发形态发生异常和皮肤屏障功能受损。最近的研究进展表明，TRPV3可能在炎症性皮肤病、瘙痒和疼痛感觉中起关键作用。因此，鉴定选择性TRPV3激活剂和抑制剂可能会为多种疾病带来有益的药物干预。本综述的目的是总结我们目前对TRPV3的组织表达、结构、功能和激活机制的认识。
