Department of Molecular Neurobiology, Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences (IBCh RAS), 16/10 Miklukho-Maklay Str., 117997 Moscow, Russia.
Institute of Molecular Medicine, Sechenov First Moscow State Medical University, Trbetskaya Str. 8, Bld. 2, 119991 Moscow, Russia.
Int J Mol Sci. 2023 May 11;24(10):8601. doi: 10.3390/ijms24108601.
Transient receptor potential vanilloid subtype 3 (TRPV3) is an ion channel with a sensory function that is most abundantly expressed in keratinocytes and peripheral neurons. TRPV3 plays a role in Ca homeostasis due to non-selective ionic conductivity and participates in signaling pathways associated with itch, dermatitis, hair growth, and skin regeneration. TRPV3 is a marker of pathological dysfunctions, and its expression is increased in conditions of injury and inflammation. There are also pathogenic mutant forms of the channel associated with genetic diseases. TRPV3 is considered as a potential therapeutic target of pain and itch, but there is a rather limited range of natural and synthetic ligands for this channel, most of which do not have high affinity and selectivity. In this review, we discuss the progress in the understanding of the evolution, structure, and pharmacology of TRPV3 in the context of the channel's function in normal and pathological states.
瞬时受体电位香草酸亚型 3（TRPV3）是一种具有感觉功能的离子通道，在角质形成细胞和外周神经元中表达最为丰富。TRPV3 由于非选择性离子导电性而在钙稳态中发挥作用，并参与与瘙痒、皮炎、毛发生长和皮肤再生相关的信号通路。TRPV3 是病理性功能障碍的标志物，其表达在损伤和炎症情况下增加。该通道也存在与遗传疾病相关的致病性突变形式。TRPV3 被认为是疼痛和瘙痒的潜在治疗靶点，但该通道的天然和合成配体的范围相当有限，其中大多数配体没有高亲和力和选择性。在这篇综述中，我们讨论了在正常和病理状态下通道功能的背景下，对 TRPV3 的进化、结构和药理学的理解进展。
