
CLC number:
On-line Access: 2026-01-27
Received: 2025-04-22
Revision Accepted: 2025-11-03
Crosschecked: 2026-01-27
Cited: 0
Clicked: 586
Citations: Bibtex RefMan EndNote GB/T7714
Yi LIU, Fuqin DUAN, Runpeng LIN, Subinuer SHABUERJIANG, Fan YANG, Aerziguli AIERKEN. @article{title=" %0 Journal Article TY - JOUR
TRPV1:从结构到功能--多维度治疗靶点的研究进展1新疆医科大学基础医学院生理学教研室, 中国乌鲁木齐市, 830017 2新疆地方病分子生物学重点实验室, 中国乌鲁木齐市, 830017 3新疆医科大学校级科研平台神经生理基础与临床转化重点实验室, 中国乌鲁木齐市, 830017 4浙江大学医学院生物物理系, 浙江大学附属第一医院肾脏病中心, 中国杭州市, 310058 5良渚实验室, 中国杭州市, 311121 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。 关键词组: Darkslateblue:Affiliate; Royal Blue:Author; Turquoise:Article
Reference[1]AbdallaSS, HarbAA, AlmasriIM, et al., 2022. The interaction of TRPV1 and lipids: insights into lipid metabolism. Front Physiol, 13:1066023. ![]() [2]AhernGP, BrooksIM, MiyaresRL, et al., 2005. Extracellular cations sensitize and gate capsaicin receptor TRPV1 modulating pain signaling. J Neurosci, 25(21):5109-5116. ![]() [3]AndreevYA, KozlovSA, KoshelevSG, et al., 2008. Analgesic compound from sea anemone Heteractis crispa is the first polypeptide inhibitor of vanilloid receptor 1 (TRPV1). J Biol Chem, 283(35):23914-23921. ![]() [4]AndreevYA, KozlovSA, KorolkovaYV, et al., 2013. Polypeptide modulators of TRPV1 produce analgesia without hyperthermia. Mar Drugs, 11(12):5100-5115. ![]() [5]AneirosE, CaoLS, PapakostaM, et al., 2011. The biophysical and molecular basis of TRPV1 proton gating. EMBO J, 30(6):994-1002. ![]() [6]AraiT, OhkuriT, YasumatsuK, et al., 2010. The role of transient receptor potential vanilloid-1 on neural responses to acids by the chorda tympani, glossopharyngeal and superior laryngeal nerves in mice. Neuroscience, 165(4):1476-1489. ![]() [7]ArnoldWR, MancinoA, MossIII FR, et al., 2024. Structural basis of TRPV1 modulation by endogenous bioactive lipids. Nat Struct Mol Biol, 31:1377-1385. ![]() [8]AzlanA, SultanaS, HueiCS, et al., 2022. Antioxidant, anti-obesity, nutritional and other beneficial effects of different chili pepper: a review. Molecules, 27(3):898. ![]() [9]BaeC, AnselmiC, KaliaJ, et al., 2016. Structural insights into the mechanism of activation of the TRPV1 channel by a membrane-bound tarantula toxin. eLife, 5:e11273. ![]() [10]BlumbergPM, PearceLV, LeeJ, 2011. TRPV1 activation is not an all-or-none event: TRPV1 partial agonism/antagonism and its regulatory modulation. Curr Top Med Chem, 11(17):2151-2158. ![]() [11]BohlenCJ, PrielA, ZhouS, et al., 2010. A bivalent tarantula toxin activates the capsaicin receptor, TRPV1, by targeting the outer pore domain. Cell, 141(5):834-845. ![]() [12]BrauchiS, OrtaG, SalazarM, et al., 2006. A hot-sensing cold receptor: C-terminal domain determines thermosensation in transient receptor potential channels. J Neurosci, 26(18):4835-4840. ![]() [13]CaoEH, Cordero-MoralesJF, LiuBY, et al., 2013a. TRPV1 channels are intrinsically heat sensitive and negatively regulated by phosphoinositide lipids. Neuron, 77(4):667-679. ![]() [14]CaoEH, LiaoMF, ChengYF, et al., 2013b. TRPV1 structures in distinct conformations reveal activation mechanisms. Nature, 504:113-118. ![]() [15]CaoT, HoCT, WangWS, et al., 2025. Capsaicin mitigates Reverbα-involved lipid metabolism disorder in HepG2 cells and obese mice through a Trpv1-dependent mechanism. J Agric Food Chem, 73(9):5300-5310. ![]() [16]CaoX, MaLL, YangF, et al., 2014. Divalent cations potentiate TRPV1 channel by lowering the heat activation threshold. J Gen Physiol, 143(1):75-90. ![]() [17]CaterinaMJ, SchumacherMA, TominagaM, et al., 1997. The capsaicin receptor: a heat-activated ion channel in the pain pathway. Nature, 389:816-824. ![]() [18]CaterinaMJ, LefflerA, MalmbergAB, et al., 2000. Impaired nociception and pain sensation in mice lacking the capsaicin receptor. Science, 288(5464):306-313. ![]() [19]ChenB, HuZT, ChenXL, et al., 2024. Molecular mechanisms of two novel and selective TRPV1 channel activators. Int J Biol Macromol, 275(Pt 1):133658. ![]() [20]ChengJJ, ZengML, PengBW, et al., 2024. Transient receptor potential vanilloid-1 (TRPV1) channels act as suppressors of the growth of glioma. Brain Res Bull, 211:110950. ![]() [21]ChibaT, MasukoS, KawanoH, 1986. Correlation of mitochondrial swelling after capsaicin treatment and substance P and somatostatin immunoreactivity in small neurons of dorsal root ganglion in the rat. Neurosci Lett, 64(3):311-316. ![]() [22]ChouMZ, MtuiT, GaoYD, et al, 2004. Resiniferatoxin binds to the capsaicin receptor (TRPV1) near the extracellular side of the S4 transmembrane domain. Biochemistry, 43(9):2501-2511. ![]() [23]ClaphamDE, MillerC, 2011. A thermodynamic framework for understanding temperature sensing by transient receptor potential (TRP) channels. Proc Natl Acad Sci USA, 108(49):19492-19497. ![]() [24]de la RocheJ, WaltherI, LeonowW, et al., 2016. Lactate is a potent inhibitor of the capsaicin receptor TRPV1. Sci Rep, 6:36740. ![]() [25]DendaS, DendaM, InoueK, et al., 2010. Glycolic acid induces keratinocyte proliferation in a skin equivalent model via TRPV1 activation. J Dermatol Sci, 57(2):108-113. ![]() [26]DengF, ZhaoBC, YangX, et al., 2021. The gut microbiota metabolite capsiate promotes Gpx4 expression by activating TRPV1 to inhibit intestinal ischemia reperfusion-induced ferroptosis. Gut Microbes, 13(1):1902719. ![]() [27]DerryS, MooreRA, 2012. Topical capsaicin (low concentration) for chronic neuropathic pain in adults. Cochrane Database Syst Rev, 2012(9):CD010111. ![]() [28]DerryS, RiceASC, ColeP, et al., 2017. Topical capsaicin (high concentration) for chronic neuropathic pain in adults. Cochrane Database Syst Rev, 1(1):CD007393. ![]() [29]ElokelyK, VelisettyP, DelemotteL, et al., 2016. Understanding TRPV1 activation by ligands: insights from the binding modes of capsaicin and resiniferatoxin. Proc Natl Acad Sci USA, 113(2):E137-E145. ![]() [30]FakihD, Guerrero-MorenoA, BaudouinC, et al., 2021. Capsazepine decreases corneal pain syndrome in severe dry eye disease. J Neuroinflammation, 18:111. ![]() [31]FanJP, KeH, LeiJ, et al., 2024. Structural basis of TRPV1 inhibition by SAF312 and cholesterol. Nat Commun, 15:6689. ![]() [32]FreynhagenR, BaronR, HuygenF, et al., 2025. Narrative review of the efficacy and safety of the high-concentration (179 mg) capsaicin patch in peripheral neuropathic pain with recommendations for clinical practice and future research. PAIN Rep, 10(2):e1235. ![]() [33]GaoNN, YangF, ChenSY, et al., 2020. The role of TRPV1 ion channels in the suppression of gastric cancer development. J Exp Clin Cancer Res, 39:206. ![]() [34]GaoY, CaoEH, JuliusD, et al., 2016. TRPV1 structures in nanodiscs reveal mechanisms of ligand and lipid action. Nature, 534:347-351. ![]() [35]GaoZS, YanXZ, Wang-SattlerR, et al., 2025. Metabolomics reveals reasons for the efficacy of acupuncture in migraine patients: the role of anaerobic glycolysis and mitochondrial citrate in migraine relief. Phenomics, online. ![]() [36]GaramiA, ShimanskyYP, RumbusZ, et al., 2020. Hyperthermia induced by transient receptor potential vanilloid-1 (TRPV1) antagonists in human clinical trials: insights from mathematical modeling and meta-analysis. Pharmacol Ther, 208:107474. ![]() [37]GouinO, L'HerondelleK, LebonvalletN, et al., 2017. TRPV1 and TRPA1 in cutaneous neurogenic and chronic inflammation: pro-inflammatory response induced by their activation and their sensitization. Protein Cell, 8(9):644-661. ![]() [38]GrandlJ, KimSE, UzzellV, et al., 2010. Temperature-induced opening of TRPV1 ion channel is stabilized by the pore domain. Nat Neurosci, 13:708-714. ![]() [39]GunthorpeMJ, RamiHK, JermanJC, et al., 2004. Identification and characterisation of SB-366791, a potent and selective vanilloid receptor (VR1/TRPV1) antagonist. Neuropharmacology, 46:133-149. ![]() [40]HaltiaT, FreireE, 1995. Forces and factors that contribute to the structural stability of membrane proteins. Biochim Biophys Acta Rev Biomembr, 1241(2):295-322. ![]() [41]HofmannNA, BarthS, Waldeck-WeiermairM, et al., 2014. TRPV1 mediates cellular uptake of anandamide and thus promotes endothelial cell proliferation and network-formation. Biol Open, 3(12):1164-1172. ![]() [42]HolzerP, 1988. Local effector functions of capsaicin-sensitive sensory nerve endings: involvement of tachykinins, calcitonin gene-related peptide and other neuropeptides. Neuroscience, 24(3):739-768. ![]() [43]HolzerP, 1991. Capsaicin: cellular targets, mechanisms of action, and selectivity for thin sensory neurons. Pharmacol Rev, 43(2):143-201. ![]() [44]HouNY, HeXL, YangYH, et al., 2019. TRPV1 induced apoptosis of colorectal cancer cells by activating calcineurin-NFAT2-p53 signaling pathway. Biomed Res Int, 2019:6712536. ![]() [45]HuF, SunWW, ZhaoXT, et al., 2008. TRPV1 mediates cell death in rat synovial fibroblasts through calcium entry-dependent ROS production and mitochondrial depolarization. Biochem Biophys Res Commun, 369(4):989-993. ![]() [46]JambrinaE, AlonsoR, AlcaldeM, et al., 2003. Calcium influx through receptor-operated channel induces mitochondria-triggered paraptotic cell death. J Biol Chem, 278(16):14134-14145. ![]() [47]JiangXH, WangCH, KeZL, et al., 2022. The ion channel TRPV1 gain-of-function reprograms the immune microenvironment to facilitate colorectal tumorigenesis. Cancer Lett, 527:95-106. ![]() [48]JordtSE, JuliusD, 2002. Molecular basis for species-specific sensitivity to “hot” chili peppers. Cell, 108(3):421-430. ![]() [49]JordtSE, TominagaM, JuliusD, 2000. Acid potentiation of the capsaicin receptor determined by a key extracellular site. Proc Natl Acad Sci USA, 97(14):8134-8139. ![]() [50]KangMS, LeeGH, ChoiGE, et al., 2020. Neuroprotective effect of Nypa fruticans wurmb by suppressing TRPV1 following sciatic nerve crush injury in a rat. Nutrients, 12(9):2618. ![]() [51]KitaharaT, LiHS, BalabanCD, 2005. Changes in transient receptor potential cation channel superfamily V (TRPV) mRNA expression in the mouse inner ear ganglia after kanamycin challenge. Hear Res, 201(1-2):132-144. ![]() [52]KleinRM, Ufret-VincentyCA, HuaL, et al., 2008. Determinants of molecular specificity in phosphoinositide regulation: PHOSPHATIDYLINOSITOL (4,5)-BISPHOSPHATE (PI(4,5)P2) IS THE ENDOGENOUS LIPID REGULATING TRPV1. J Biol Chem, 283(38):26208-26216. ![]() [53]KnappO, McArthurJR, AdamsDJ, 2012. Conotoxins targeting neuronal voltage-gated sodium channel subtypes: potential analgesics? Toxins, 4(11):1236-1260. ![]() [54]KongWL, PengYY, PengBW, 2017. Modulation of neuroinflammation: role and therapeutic potential of TRPV1 in the neuro-immune axis. Brain Behav Immun, 64:354-366. ![]() [55]KornilovP, PeretzA, LeeY, et al., 2014. Promiscuous gating modifiers target the voltage sensor of Kv7.2, TRPV1, and Hv1 cation channels. FASEB J, 28(6):2591-2602. ![]() [56]KwonDH, ZhangF, SuoY, et al., 2021. Heat-dependent opening of TRPV1 in the presence of capsaicin. Nat Struct Mol Biol, 28:554-563. ![]() [57]KwonDH, ZhangF, FedorJG, et al., 2022. Vanilloid-dependent TRPV1 opening trajectory from cryoem ensemble analysis. Nat Commun, 13:2874. ![]() [58]Ladrón-de-GuevaraE, DominguezL, Rangel-YescasGE, et al., 2020. The contribution of the ankyrin repeat domain of TRPV1 as a thermal module. Biophys J, 118(4):836-845. ![]() [59]LapointeTK, BassoL, IftincaMC, et al., 2015. TRPV1 sensitization mediates postinflammatory visceral pain following acute colitis. Am J Physiol Gastrointest Liver Physiol, 309(2):G87-G99. ![]() [60]LeoM, SchulteM, SchmittLI, et al., 2017. Intrathecal resiniferatoxin modulates TRPV1 in DRG neurons and reduces TNF-induced pain-related behavior. Mediators Inflamm, 2017:2786427. ![]() [61]LiaoMF, CaoEH, JuliusD, et al., 2013. Structure of the TRPV1 ion channel determined by electron cryo-microscopy. Nature, 504:107-112. ![]() [62]LiuBY, HuiK, QinF, 2003. Thermodynamics of heat activation of single capsaicin ion channels VR1. Biophys J, 85(5):2988-3006. ![]() [63]LiuJ, HuangSY, YuRX, et al., 2022. TRPV1+ sensory nerves modulate corneal inflammation after epithelial abrasion via RAMP1 and SSTR5 signaling. Mucosal Immunol, 15(5):867-881. ![]() [64]LiuT, WangG, TaoHH, et al., 2016. Capsaicin mediates caspases activation and induces apoptosis through P38 and JNK MAPK pathways in human renal carcinoma. BMC Cancer, 16:790. ![]() [65]LuW, LiJ, GongLP, et al., 2014. H2S modulates duodenal motility in male rats via activating TRPV1 and KATP channels. Br J Pharmacol, 171(6):1534-1550. ![]() [66]LuoZD, MaLQ, ZhaoZG, et al., 2012. TRPV1 activation improves exercise endurance and energy metabolism through PGC-1α upregulation in mice. Cell Res, 22(3):551-564. ![]() [67]LyallV, HeckGL, VinnikovaAK, et al., 2004. The mammalian amiloride‐insensitive non‐specific salt taste receptor is a vanilloid receptor‐1 variant. J Physiol, 558:147-159. ![]() [68]Marek-JozefowiczL, NedoszytkoB, GrochockaM, et al., 2023. Molecular mechanisms of neurogenic inflammation of the skin. Int J Mol Sci, 24(5):5001. ![]() [69]MatsumotoK, KurosawaE, TeruiH, et al., 2009. Localization of TRPV1 and contractile effect of capsaicin in mouse large intestine: high abundance and sensitivity in rectum and distal colon. Am J Physiol Gastrointest Liver Physiol, 297(2):G348-G360. ![]() [70]MattaJA, AhernGP, 2007. Voltage is a partial activator of rat thermosensitive TRP channels. J Physiol, 585(2):469-482. ![]() [71]MazetoTK, PicadaJN, CorreaÁP, et al., 2020. Antinociceptive and genotoxic assessments of the antagonist TRPV1 receptor SB-366791 on morphine-induced tolerance in mice. Naunyn Schmiedeberg’s Arch Pharmacol, 393(3):481-490. ![]() [72]Moiseenkova-BellVY, StanciuLA, SeryshevaII, et al., 2008. Structure of TRPV1 channel revealed by electron cryomicroscopy. Proc Natl Acad Sci USA, 105(21):7451-7455. ![]() [73]MontellC, BirnbaumerL, FlockerziV, et al., 2002. A unified nomenclature for the superfamily of TRP cation channels. Mol Cell, 9(2):229-231. ![]() [74]MoroniM, Servin-VencesMR, FleischerR, et al., 2018. Voltage gating of mechanosensitive PIEZO channels. Nat Commun, 9:1096. ![]() [75]MugoA, ChouRY, ChinF, et al., 2023. A suicidal mechanism for the exquisite temperature sensitivity of TRPV1. Proc Natl Acad Sci USA, 120(36):e2300305120. ![]() [76]NadezhdinKD, NeubergerA, NikolaevYA, et al., 2021. Extracellular cap domain is an essential component of the TRPV1 gating mechanism. Nat Commun, 12:2154. ![]() [77]NeubergerA, OdaM, NikolaevYA, et al., 2023. Human TRPV1 structure and inhibition by the analgesic SB-366791. Nat Commun, 14:2451. ![]() [78]NieRF, LiuQ, WangXS, 2022. TRPV1 is a potential tumor suppressor for its negative association with tumor proliferation and positive association with antitumor immune responses in pan-cancer. J Oncol, 2022:6964550. ![]() [79]NLM, 2009. Resiniferatoxin to treat severe pain associated with advanced cancer. https://clinicaltrials.gov/study/NCT00804154 ![]() [80]NLM, 2020. A phase 3 study to evaluate the efficacy and safety of resiniferatoxin for pain due to osteoarthritis of the knee. https://clinicaltrials.gov/study/NCT04044742 ![]() [81]NLM, 2021. Pleiotropic role of TRPV1 in psoriasis inflammation (TRIP). https://clinicaltrials.gov/study/NCT04848194 ![]() [82]OliveiraSM, SilvaCR, TrevisanG, et al., 2016. Antinociceptive effect of a novel armed spider peptide Tx3-5 in pathological pain models in mice. Pflugers Arch Eur J Physiol, 468(5):881-894. ![]() [83]O'NeillJ, BrockC, OlesenAE, et al., 2012. Unravelling the mystery of capsaicin: a tool to understand and treat pain. Pharmacol Rev, 64(4):939-971. ![]() [84]OtzenD, 2014. Membrane protein folding and stability. Arch Biochem Biophys, 564:262-264. ![]() [85]Öz-ArslanD, YavuzM, KanB, 2024. Exploring orphan GPCRs in neurodegenerative diseases. Front Pharmacol, 15:1394516. ![]() [86]PayritsM, ZsidóBZ, Nehr-MajorosAK, et al., 2024. Lipid raft disruption inhibits the activation of transient receptor potential vanilloid 1, but not TRP Melastatin 3 and the voltage-gated L-type calcium channels in sensory neurons. Front Cell Dev Biol, 12:1452306. ![]() [87]PintérE, HelyesZ, SzőkeÉ, et al., 2023. The triple function of the capsaicin-sensitive sensory neurons: in memoriam János Szolcsányi. Temperature, 10(1):13-34. ![]() [88]PremkumarLS, 2010. Targeting TRPV1 as an alternative approach to narcotic analgesics to treat chronic pain conditions. AAPS J, 12(3):361-370. ![]() [89]RieraCE, HuisingMO, FollettP, et al., 2014. TRPV1 pain receptors regulate longevity and metabolism by neuropeptide signaling. Cell, 157(5):1023-1036. ![]() [90]RosenbaumT, AwayaM, GordonSE, 2002. Subunit modification and association in VR1 ion channels. BMC Neurosci, 3:4. ![]() [91]RowbothamMC, NothaftW, DuanRW, et al., 2011. Oral and cutaneous thermosensory profile of selective TRPV1 inhibition by ABT-102 in a randomized healthy volunteer trial. Pain, 152(5):1192-1200. ![]() [92]SakamotoK, KurokiT, OkunoY, et al., 2014. Activation of the TRPV1 channel attenuates N-methyl-d-aspartic acid-induced neuronal injury in the rat retina. Eur J Pharmacol, 733:13-22. ![]() [93]SałatK, JakubowskaA, KuligK, 2014. Zucapsaicin for the treatment of neuropathic pain. Expert Opin Investig Drugs, 23(10):1433-1440. ![]() [94]SánchezMG, SánchezAM, ColladoB, et al., 2005. Expression of the transient receptor potential vanilloid 1 (TRPV1) in LNCaP and PC-3 prostate cancer cells and in human prostate tissue. Eur J Pharmacol, 515(1-3):20-27. ![]() [95]SappingtonRM, SidorovaT, LongDJ, et al., 2009. TRPV1: contribution to retinal ganglion cell apoptosis and increased intracellular Ca2+ with exposure to hydrostatic pressure. Invest Ophthalmol Vis Sci, 50(2):717-728. ![]() [96]SeabrookGR, SuttonKG, JarolimekW, et al., 2002. Functional properties of the high-affinity TRPV1 (VR1) vanilloid receptor antagonist (4-hydroxy-5-iodo-3-methoxyphenylacetate ester) iodo-resiniferatoxin. J Pharmacol Exp Ther, 303(3):1052-1060. ![]() [97]SendelM, DunstA, ForstenpointnerJ, et al., 2023. Capsaicin treatment in neuropathic pain: axon reflex vasodilatation after 4 weeks correlates with pain reduction. Pain, 164(3):534-542. ![]() [98]SendetskiM, WedelS, FurutaniK, et al., 2024. Oleic acid released by sensory neurons inhibits TRPV1-mediated thermal hypersensitivity via GPR40. iScience, 27(8):110552. ![]() [99]SenningEN, CollinsMD, StratiievskaA, et al., 2014. Regulation of TRPV1 ion channel by phosphoinositide (4,5)-bisphosphate. J Biol Chem, 289(16):10999-11006. ![]() [100]ShamsiF, PiperM, HoLL, et al., 2021. Vascular smooth muscle-derived TRPV1+ progenitors are a source of cold-induced thermogenic adipocytes. Nat Metab, 3:485-495. ![]() [101]ShirakawaH, YamaokaT, SanpeiK, et al., 2008. TRPV1 stimulation triggers apoptotic cell death of rat cortical neurons. Biochem Biophys Res Commun, 377(4):1211-1215. ![]() [102]SiemensJ, ZhouS, PiskorowskiR, et al., 2006. Spider toxins activate the capsaicin receptor to produce inflammatory pain. Nature, 444:208-212. ![]() [103]SilvestriC, di MarzoV, 2013. The endocannabinoid system in energy homeostasis and the etiopathology of metabolic disorders. Cell Metab, 17(4):475-490. ![]() [104]SintsovaO, GladkikhI, KlimovichA, et al., 2021. TRPV1 blocker HCRG21 suppresses TNF-α production and prevents the development of edema and hypersensitivity in carrageenan-induced acute local inflammation. Biomedicines, 9(7):716. ![]() [105]Sosa-PagánJO, IversenES, GrandlJ, 2017. TRPV1 temperature activation is specifically sensitive to strong decreases in amino acid hydrophobicity. Sci Rep, 7:549. ![]() [106]StockK, KumarJ, SynowitzM, et al., 2012. Neural precursor cells induce cell death of high-grade astrocytomas through stimulation of TRPV1. Nat Med, 18:1232-1238. ![]() [107]SultanaA, SinglaRK, HeXF, et al., 2021. Topical capsaicin for the treatment of neuropathic pain. Curr Drug Metab, 22(3):198-207. ![]() [108]SunJX, ZhuKY, WangYM, et al., 2023. Activation of TRPV1 receptor facilitates myelin repair following demyelination via the regulation of microglial function. Acta Pharmacol Sin, 44(4):766-779. ![]() [109]SunZW, HanJ, ZhaoWT, et al., 2014. TRPV1 activation exacerbates hypoxia/reoxygenation-induced apoptosis in H9C2 cells via calcium overload and mitochondrial dysfunction. Int J Mol Sci, 15(10):18362-18380. ![]() [110]SwansonDM, DubinAE, ShahC, et al., 2005. Identification and biological evaluation of 4-(3-trifluoromethylpyridin-2-yl)piperazine-1-carboxylic acid (5-trifluoromethylpyridin-2-yl)amide, a high affinity TRPV1 (VR1) vanilloid receptor antagonist. J Med Chem, 48(6):1857-1872. ![]() [111]SzallasiA, 2023. Resiniferatoxin: nature’s precision medicine to silence TRPV1-positive afferents. Int J Mol Sci, 24(20):15042. ![]() [112]SzallasiA, 2024. Targeting TRPV1 for cancer pain relief: can it work? Cancers, 16(3):648. ![]() [113]SzolcsányiJ, Jancsó-GáborA, 1975. Sensory effects of capsaicin congeners I. Relationship between chemical structure and pain-producing potency of pungent agents. Arzneimittelforschung, 25(12):1877-1881. ![]() [114]SzolcsányiJ, SándorZ, 2012. Multisteric TRPV1 nocisensor: a target for analgesics. Trends Pharmacol Sci, 33(12):646-655. ![]() [115]TanakaM, HayakawaK, OgawaN, et al., 2020. Structure determination of the human TRPV1 ankyrin-repeat domain under nonreducing conditions. Acta Crystallogr F Struct Biol Commun, 76(Pt 3):130-137. ![]() [116]TominagaM, CaterinaMJ, MalmbergAB, et al., 1998. The cloned capsaicin receptor integrates multiple pain-producing stimuli. Neuron, 21(3):531-543. ![]() [117]TsaiST, WeiTH, YangYW, et al., 2021. Transient receptor potential V1 modulates neuroinflammation in Parkinson’s disease dementia: molecular implications for electroacupuncture and rivastigmine. Iran J Basic Med Sci, 24(10):1336-1345. ![]() [118]TsvetkovEA, PotatievaNN, BolshakovKV, 2017. Voltage-dependent interaction of capsaicine and protons on TRPV1-receptors. Acta Naturae, 9(1):75-80. ![]() [119]ValdesAM, de WildeG, DohertySA, et al., 2011. The Ile585Val TRPV1 variant is involved in risk of painful knee osteoarthritis. Ann Rheum Dis, 70(9):1556-1561. ![]() [120]VercelliC, BarberoR, CunibertiB, et al., 2015. Expression and functionality of TRPV1 receptor in human MCF-7 and canine CF.41 cells. Vet Comp Oncol, 13(2):133-142. ![]() [121]VlachováV, TeisingerJ, SušánkováK, et al., 2003. Functional role of C-terminal cytoplasmic tail of rat vanilloid receptor 1. J Neurosci, 23(4):1340-1350. ![]() [122]VoetsT, DroogmansG, WissenbachU, et al., 2004. The principle of temperature-dependent gating in cold- and heat-sensitive TRP channels. Nature, 430:748-754. ![]() [123]VoightEA, GomtsyanAR, DaanenJF, et al., 2014. Discovery of (R)-1-(7-chloro-2,2-bis(fluoromethyl)chroman-4-yl)-3-(3-methylisoquinolin-5-yl)urea (A-1165442): a temperature-neutral transient receptor potential vanilloid-1 (TRPV1) antagonist with analgesic efficacy. J Med Chem, 57(17):7412-7424. ![]() [124]WangCF, LuJ, ShaXD, et al., 2023. TRPV1 regulates ApoE4-disrupted intracellular lipid homeostasis and decreases synaptic phagocytosis by microglia. Exp Mol Med, 55(2):347-363. ![]() [125]WangWX, SunT, 2023. Impact of TRPV1 on pathogenesis and therapy of neurodegenerative diseases. Molecules, 29:181. ![]() [126]WangY, ZhangY, OuyangJ, et al., 2024. TRPV1 inhibition suppresses non-small cell lung cancer progression by inhibiting tumour growth and enhancing the immune response. Cell Oncol, 47(3):779-791. ![]() [127]WatsonPNC, EvansRJ, 1992. The postmastectomy pain syndrome and topical capsaicin: a randomized trial. Pain, 51(3):375-379. ![]() [128]WoodJN, WinterJ, JamesIF, et al., 1988. Capsaicin-induced ion fluxes in dorsal root ganglion cells in culture. J Neurosci, 8(9):3208-3220. ![]() [129]XuMM, ZhangYB, WangMY, et al., 2019. TRPV1 and TRPA1 in lung inflammation and airway hyperresponsiveness induced by fine particulate matter (PM2.5). Oxid Med Cell Longev, 2019:7450151. ![]() [130]YangF, CuiYY, WangKW, et al., 2010. Thermosensitive TRP channel pore turret is part of the temperature activation pathway. Proc Natl Acad Sci USA, 107(15):7083-7088. ![]() [131]YangF, MaLL, CaoX, et al., 2014. Divalent cations activate TRPV1 through promoting conformational change of the extracellular region. J Gen Physiol, 143(1):91-103. ![]() [132]YangF, XiaoX, ChengW, et al., 2015. Structural mechanism underlying capsaicin binding and activation of the TRPV1 ion channel. Nat Chem Biol, 11:518-524. ![]() [133]YangF, XuLZ, LeeBH, et al., 2020. An unorthodox mechanism underlying voltage sensitivity of TRPV1 ion channel. Adv Sci, 7(20):2000575. ![]() [134]YangSL, YangF, WeiNN, et al., 2015. A pain-inducing centipede toxin targets the heat activation machinery of nociceptor TRPV1. Nat Commun, 6:8297. ![]() [135]YangY, GuXK, WengWJ, et al., 2024. Correction: SUMOylation-induced membrane localization of TRPV1 suppresses proliferation and migration in gastric cancer cells. Cell Commun Signal, 22:479. ![]() [136]YangYQ, GuoWN, MaJJ, et al., 2018. Downregulated TRPV1 expression contributes to melanoma growth via the calcineurin-ATF3-p53 pathway. J Invest Dermatol, 138(10):2205-2215. ![]() [137]YaoJ, LiuBY, QinF, 2010. Kinetic and energetic analysis of thermally activated TRPV1 channels. Biophys J, 99(6):1743-1753. ![]() [138]YekkiralaAS, RobersonDP, BeanBP, et al., 2017. Breaking barriers to novel analgesic drug development. Nat Rev Drug Discov, 16:545-564. ![]() [139]YoshidaA, FurubeE, MannariT, et al., 2016. TRPV1 is crucial for proinflammatory STAT3 signaling and thermoregulation-associated pathways in the brain during inflammation. Sci Rep, 6:26088. ![]() [140]ZhangF, Jara-OsegueraA, ChangTH, et al., 2018. Heat activation is intrinsic to the pore domain of TRPV1. Proc Natl Acad Sci USA, 115(2):E317-E324. ![]() [141]ZhangKH, JuliusD, ChengYF, 2021. Structural snapshots of TRPV1 reveal mechanism of polymodal functionality. Cell, 184(20):5138-5150.e12. ![]() [142]ZhangH, WangJ, YangF, 2024. Design, synthesis and functional validation of peptide inhibitors based on TRPV1 ion channel agonist RhTx. J Zhejiang Univ (Med Sci), 53(2):201-207 (in Chinese). ![]() [143]ZhangYH, HouBH, LiangPY, et al., 2021. TRPV1 channel mediates NLRP3 inflammasome-dependent neuroinflammation in microglia. Cell Death Dis, 12(12):1159. ![]() [144]ZhangZM, WuXL, ZhangLW, et al., 2020. Menthol relieves acid reflux inflammation by regulating TRPV1 in esophageal epithelial cells. Biochem Biophys Res Commun, 525(1):113-120. ![]() [145]ZhaoLM, ZhangXY, KuangHY, et al., 2013. Effect of TRPV1 channel on the proliferation and apoptosis in asthmatic rat airway smooth muscle cells. Exp Lung Res, 39(7):283-294. ![]() [146]ZhuC, WangMY, GuoJ, et al., 2022. Angelica dahurica extracts attenuate CFA-induced inflammatory pain via TRPV1 in mice. Evid Based Complement Alternat Med, 2022:4684830. ![]() [147]ZhuH, WangY, HeYB, et al., 2022. Inflammation-mediated macrophage polarization induces TRPV1/TRPA1 heteromers in endometriosis. Am J Transl Res, 14(5):3066-3078. ![]() Journal of Zhejiang University-SCIENCE, 38 Zheda Road, Hangzhou
310027, China
Tel: +86-571-87952783; E-mail: cjzhang@zju.edu.cn Copyright © 2000 - 2026 Journal of Zhejiang University-SCIENCE | ||||||||||||||


ORCID:
Open peer comments: Debate/Discuss/Question/Opinion
<1>