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Structural snapshots of TRPV1 reveal mechanism of polymodal functionality.

Zhang K, Julius D, Cheng Y
Cell 184 5138-5150.e12 (2021)
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Cited: 62 times
EuropePMC logo PMID: 34496225

Abstract

Many transient receptor potential (TRP) channels respond to diverse stimuli and conditionally conduct small and large cations. Such functional plasticity is presumably enabled by a uniquely dynamic ion selectivity filter that is regulated by physiological agents. What is currently missing is a "photo series" of intermediate structural states that directly address this hypothesis and reveal specific mechanisms behind such dynamic channel regulation. Here, we exploit cryoelectron microscopy (cryo-EM) to visualize conformational transitions of the capsaicin receptor, TRPV1, as a model to understand how dynamic transitions of the selectivity filter in response to algogenic agents, including protons, vanilloid agonists, and peptide toxins, permit permeation by small and large organic cations. These structures also reveal mechanisms governing ligand binding substates, as well as allosteric coupling between key sites that are proximal to the selectivity filter and cytoplasmic gate. These insights suggest a general framework for understanding how TRP channels function as polymodal signal integrators.

Reviews - 7l2l mentioned but not cited (3)

  1. Ligand-Binding Sites in Vanilloid-Subtype TRP Channels. Yelshanskaya MV, Sobolevsky AI. Front Pharmacol 13 900623 (2022)
  2. 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)
  3. Centipede Venom: A Potential Source of Ion Channel Modulators. Luo A, Wang A, Kamau PM, Lai R, Luo L. Int J Mol Sci 23 7105 (2022)

Articles - 7l2l mentioned but not cited (2)

  1. Structural snapshots of TRPV1 reveal mechanism of polymodal functionality. Zhang K, Julius D, Cheng Y. Cell 184 5138-5150.e12 (2021)
  2. Opening of capsaicin receptor TRPV1 is stabilized equally by its four subunits. Li S, Nguyen PT, Vu S, Yarov-Yarovoy V, Zheng J. J Biol Chem 299 104828 (2023)


Reviews citing this publication (24)

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Articles citing this publication (33)

  1. Structural insights into TRPV2 activation by small molecules. Pumroy RA, Protopopova AD, Fricke TC, Lange IU, Haug FM, Nguyen PT, Gallo PN, Sousa BB, Bernardes GJL, Yarov-Yarovoy V, Leffler A, Moiseenkova-Bell VY. Nat Commun 13 2334 (2022)
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  4. Applications of Cryo-EM in small molecule and biologics drug design. Lees JA, Dias JM, Han S. Biochem Soc Trans 49 2627-2638 (2021)
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  12. Anti-Inflammatory Effect of Beta-Caryophyllene Mediated by the Involvement of TRPV1, BDNF and trkB in the Rat Cerebral Cortex after Hypoperfusion/Reperfusion. Serra MP, Boi M, Carta A, Murru E, Carta G, Banni S, Quartu M. Int J Mol Sci 23 3633 (2022)
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  14. In Silico Drug Repurposing Framework Predicts Repaglinide, Agomelatine and Protokylol as TRPV1 Modulators with Analgesic Activity. Andrei C, Mihai DP, Zanfirescu A, Nitulescu GM, Negres S. Pharmaceutics 14 2563 (2022)
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  20. Pepper Fruit Extracts Show Anti-Proliferative Activity against Tumor Cells Altering Their NADPH-Generating Dehydrogenase and Catalase Profiles. Rodríguez-Ruiz M, Ramos MC, Campos MJ, Díaz-Sánchez I, Cautain B, Mackenzie TA, Vicente F, Corpas FJ, Palma JM. Antioxidants (Basel) 12 1461 (2023)
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  22. Anti-Nociceptive Effects of Sphingomyelinase and Methyl-Beta-Cyclodextrin in the Icilin-Induced Mouse Pain Model. Horváth Á, Steib A, Nehr-Majoros A, Kántás B, Király Á, Racskó M, Tóth BI, Szánti-Pintér E, Kudová E, Skoda-Földes R, Helyes Z, Szőke É. Int J Mol Sci 25 4637 (2024)
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