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Heat-dependent opening of TRPV1 in the presence of capsaicin.

Kwon DH, Zhang F, Suo Y, Bouvette J, Borgnia MJ, Lee SY
Nat Struct Mol Biol 28 554-563 (2021)
Related entries: 7lp9, 7lpa, 7lpb, 7lpc, 7lpe

Cited: 69 times
EuropePMC logo PMID: 34239123

Abstract

Transient receptor potential vanilloid member 1 (TRPV1) is a Ca2+-permeable cation channel that serves as the primary heat and capsaicin sensor in humans. Using cryo-EM, we have determined the structures of apo and capsaicin-bound full-length rat TRPV1 reconstituted into lipid nanodiscs over a range of temperatures. This has allowed us to visualize the noxious heat-induced opening of TRPV1 in the presence of capsaicin. Notably, noxious heat-dependent TRPV1 opening comprises stepwise conformational transitions. Global conformational changes across multiple subdomains of TRPV1 are followed by the rearrangement of the outer pore, leading to gate opening. Solvent-accessible surface area analyses and functional studies suggest that a subset of residues form an interaction network that is directly involved in heat sensing. Our study provides a glimpse of the molecular principles underlying noxious physical and chemical stimuli sensing by TRPV1, which can be extended to other thermal sensing ion channels.

Reviews - 7lpd mentioned but not cited (2)

  1. Ligand-Binding Sites in Vanilloid-Subtype TRP Channels. Yelshanskaya MV, Sobolevsky AI. Front Pharmacol 13 900623 (2022)
  2. A journey from molecule to physiology and in silico tools for drug discovery targeting the transient receptor potential vanilloid type 1 (TRPV1) channel. Amaya-Rodriguez CA, Carvajal-Zamorano K, Bustos D, Alegría-Arcos M, Castillo K. Front Pharmacol 14 1251061 (2023)

Articles - 7lpd mentioned but not cited (3)



Reviews citing this publication (21)

  1. TRP (transient receptor potential) ion channel family: structures, biological functions and therapeutic interventions for diseases. Zhang M, Ma Y, Ye X, Zhang N, Pan L, Wang B. Signal Transduct Target Ther 8 261 (2023)
  2. TRP channels: a journey towards a molecular understanding of pain. Rosenbaum T, Morales-Lázaro SL, Islas LD. Nat Rev Neurosci 23 596-610 (2022)
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  4. Capsaicin and TRPV1 Channels in the Cardiovascular System: The Role of Inflammation. Munjuluri S, Wilkerson DA, Sooch G, Chen X, White FA, Obukhov AG. Cells 11 18 (2021)
  5. A molecular perspective on identifying TRPV1 thermosensitive regions and disentangling polymodal activation. Luu DD, Owens AM, Mebrat MD, Van Horn WD. Temperature (Austin) 10 67-101 (2023)
  6. Progress in the Structural Basis of thermoTRP Channel Polymodal Gating. Fernández-Ballester G, Fernández-Carvajal A, Ferrer-Montiel A. Int J Mol Sci 24 743 (2023)
  7. The Promise of Niacin in Neurology. Wuerch E, Urgoiti GR, Yong VW. Neurotherapeutics 20 1037-1054 (2023)
  8. A bibliometrics analysis and visualization study of TRPV1 channel. Gao N, Li M, Wang W, Liu Z, Guo Y. Front Pharmacol 14 1076921 (2023)
  9. Cryo-EM Analyses Permit Visualization of Structural Polymorphism of Biological Macromolecules. Chang WH, Huang SH, Lin HH, Chung SC, Tu IP. Front Bioinform 1 788308 (2021)
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  14. Binding interactions of fatty acyl lipid mediators within the vanilloid pocket of TRPV1: A molecular dynamics study. Birkic N, Visentin D, Svedružić Ž, Reynolds CA. Prostaglandins Other Lipid Mediat 169 106771 (2023)
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  16. Comprehensive review on the novel immunotherapy target: Leucine-rich repeat-containing 8A/volume-regulated anion channel. Hu Y, Qin J, Ma Y, Yang R, Liu X, Shi C. Int J Biol Sci 20 3881-3891 (2024)
  17. Research focus and thematic trends of transient receptor potential vanilloid member 1 research: a bibliometric analysis of the global publications (1990-2023). Liu X, Zhang M, He C, Jia S, Xiang R, Xu Y, Zhao M. Naunyn Schmiedebergs Arch Pharmacol 397 1327-1346 (2024)
  18. TRPV2: a universal regulator in cellular physiology with a yet poorly defined thermosensitivity. Fricke TC, Leffler A. J Physiol Sci 74 42 (2024)
  19. The dual role of TRPV1 in peripheral neuropathic pain: pain switches caused by its sensitization or desensitization. Gao N, Li M, Wang W, Liu Z, Guo Y. Front Mol Neurosci 17 1400118 (2024)
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Articles citing this publication (43)



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