TRPV1: from structure to function-a multidimensional target for therapeutic advances.

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Abstract

Transient receptor potential vanilloid subtype 1 (TRPV1), a polymodally activated, calcium-permeable non-selective cation channel, is broadly present in all parts of the body, with notable expression in the nociceptive neurons. Both physiological and pathological functions rely heavily on this ion channel, mediating responses to a variety of stimuli and contributing to the maintenance of bodily homeostasis. Its unique ability to respond to temperature changes, chemical ligands, and voltage fluctuations positions TRPV1 as a key target in understanding and modulating normal bodily functions, in addition to diagnosing and treating diseases. This review synthesizes current knowledge on the structure, gating mechanisms, and physiological and pathological roles of TRPV1, highlighting its potential as a therapeutic target across multiple disease states. By providing a comprehensive overview of the multifaceted functions of TRPV1, this review aims to inform and inspire future research, finally contributing to the advancement of new therapeutic techniques focusing on TRPV1 to enhance human health.
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Abstract

Transient receptor potential vanilloid subtype 1 (TRPV1), a polymodally activated, calcium-permeable non-selective cation channel, is broadly present in all parts of the body, with notable expression in the nociceptive neurons. Both physiological and pathological functions rely heavily on this ion channel, mediating responses to a variety of stimuli and contributing to the maintenance of bodily homeostasis. Its unique ability to respond to temperature changes, chemical ligands, and voltage fluctuations positions TRPV1 as a key target in understanding and modulating normal bodily functions, in addition to diagnosing and treating diseases. This review synthesizes current knowledge on the structure, gating mechanisms, and physiological and pathological roles of TRPV1, highlighting its potential as a therapeutic target across multiple disease states. By providing a comprehensive overview of the multifaceted functions of TRPV1, this review aims to inform and inspire future research, finally contributing to the advancement of new therapeutic techniques focusing on TRPV1 to enhance human health. 摘要 瞬时受体电位香草素亚型1(transient receptor potential vanilloid subtype 1, TRPV1)是一种多模态激活的钙离子通透性非选择性阳离子通道蛋白, 广泛分布于全身各部位, 在伤害感觉神经元中表达显著。该离子通道在生理与病理状态下均发挥关键作用, 不仅介导多种刺激的应答反应, 还参与维持机体稳态。TRPV1凭借其对温度变化、化学配体及电压波动的独特响应能力, 成为理解与调控正常生理功能的关键靶点, 同时也为疾病诊断与治疗提供重要依据。本文系统综述了TRPV1的结构、门控机制及其生理和病理作用, 强调了其在多种疾病中的潜在治疗价值。本综述全面概述TRPV1的多重功能, 旨在为未来研究提供思路, 并推动以TRPV1为靶点的新疗法研发, 从而助力提升人类健康水平。 Similar content being viewed by others

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Exp Lung Res, 39(7):283–294. https://doi.org/10.3109/01902148.2013.813610 Zhu C, Wang MY, Guo J, et al., 2022. Angelica dahurica extracts attenuate CFA-induced inflammatory pain via TRPV1 in mice. Evid Based Complement Alternat Med, 2022:4684830. https://doi.org/10.1155/2022/4684830 Zhu H, Wang Y, He YB, et al., 2022. Inflammation-mediated macrophage polarization induces TRPV1/TRPA1 heteromers in endometriosis. Am J Transl Res, 14(5):3066–3078. Acknowledgments This work was supported by the Natural Science Foundation of Xinjiang Uyghur Autonomous Region (No. 2022D01C721), the Tianchi Young Talent Program of Xinjiang Uyghur Autonomous Region, and the General Program of the National Natural Science Foundation of China (NSFC) (No. 32571328). Author information Authors and Affiliations Contributions Yi LIU, Fuqin DUAN, Runpeng LIN, and Subinuer SHABUERJIANG performed the writing – original draft. Fan YANG and Aerziguli AIERKEN contributed to the writing – review & editing and conceptualization. All authors have read and agreed to the final manuscript. Corresponding authors Ethics declarations Fan YANG is a Young Scientist Committee Member for Journal of Zhejiang University-SCIENCE B and was not involved in the editorial review or the decision to publish this article. Yi LIU, Fuqin DUAN, Runpeng LIN, Subinuer SHABUERJIANG, Fan YANG, and Aerziguli AIERKEN declare that they have no conflicts of interest. This review does not contain any studies with human or animal subjects performed by any of the authors. Additional information Declaration on the use of generative AI tools During the preparation of this manuscript, the authors used ERNIE Bot to verify specialized terminology and ensure correct usage of technical vocabulary. After utilizing this tool, the authors thoroughly reviewed and revised all content as necessary and take full responsibility for the accuracy and integrity of the final publication. Rights and permissions About this article Cite this article Liu, Y., Duan, F., Lin, R. et al. TRPV1: from structure to function—a multidimensional target for therapeutic advances. J. Zhejiang Univ. Sci. B 27, 1–22 (2026). https://doi.org/10.1631/jzus.B2500209 Received: Accepted: Published: Version of record: Issue date: DOI: https://doi.org/10.1631/jzus.B2500209

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