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Structure of the cold- and menthol-sensing ion channel TRPM8.

Yin Y, Wu M, Zubcevic L, Borschel WF, Lander GC, Lee SY
Science 359 237-241 (2018)
Cited: 158 times
EuropePMC logo PMID: 29217583

Abstract

Transient receptor potential melastatin (TRPM) cation channels are polymodal sensors that are involved in a variety of physiological processes. Within the TRPM family, member 8 (TRPM8) is the primary cold and menthol sensor in humans. We determined the cryo-electron microscopy structure of the full-length TRPM8 from the collared flycatcher at an overall resolution of ~4.1 ångstroms. Our TRPM8 structure reveals a three-layered architecture. The amino-terminal domain with a fold distinct among known TRP structures, together with the carboxyl-terminal region, forms a large two-layered cytosolic ring that extensively interacts with the transmembrane channel layer. The structure suggests that the menthol-binding site is located within the voltage-sensor-like domain and thus provides a structural glimpse of the design principle of the molecular transducer for cold and menthol sensation.

Reviews - 6bpq mentioned but not cited (10)

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Articles - 6bpq mentioned but not cited (23)

  1. Structure of the cold- and menthol-sensing ion channel TRPM8. Yin Y, Wu M, Zubcevic L, Borschel WF, Lander GC, Lee SY. Science 359 237-241 (2018)
  2. Structural basis of cooling agent and lipid sensing by the cold-activated TRPM8 channel. Yin Y, Le SC, Hsu AL, Borgnia MJ, Yang H, Lee SY. Science 363 eaav9334 (2019)
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  13. Structural and in Vitro Functional Characterization of a Menthyl TRPM8 Antagonist Indicates Species-Dependent Regulation. Journigan VB, Alarcón-Alarcón D, Feng Z, Wang Y, Liang T, Dawley DC, Amin ARMR, Montano C, Van Horn WD, Xie XQ, Ferrer-Montiel A, Fernández-Carvajal A. ACS Med Chem Lett 12 758-767 (2021)
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  15. β-Lactam TRPM8 Antagonist RGM8-51 Displays Antinociceptive Activity in Different Animal Models. Martín-Escura C, Medina-Peris A, Spear LA, de la Torre Martínez R, Olivos-Oré LA, Barahona MV, González-Rodríguez S, Fernández-Ballester G, Fernández-Carvajal A, Artalejo AR, Ferrer-Montiel A, González-Muñiz R. Int J Mol Sci 23 2692 (2022)
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  17. Dual amplification strategy turns TRPM2 channels into supersensitive central heat detectors. Bartók Á, Csanády L. Proc Natl Acad Sci U S A 119 e2212378119 (2022)
  18. Non-canonical helical transitions and conformational switching are associated with characteristic flexibility and disorder indices in TRP and Kv channels. García-Morales A, Balleza D. Channels (Austin) 17 2212349 (2023)
  19. Phenylalanine-Derived β-Lactam TRPM8 Modulators. Configuration Effect on the Antagonist Activity. Bonache MÁ, Llabrés PJ, Martín-Escura C, De la Torre-Martínez R, Medina-Peris A, Butrón L, Gómez-Monterrey I, Roa AM, Fernández-Ballester G, Ferrer-Montiel A, Fernández-Carvajal A, González-Muñiz R. Int J Mol Sci 22 2370 (2021)
  20. Differential Activation of TRPM8 by the Stereoisomers of Menthol. Chen X, Xu L, Zhang H, Wen H, Yang F. Front Pharmacol 13 898670 (2022)
  21. Human mutations highlight an intersubunit cation-π bond that stabilizes the closed but not open or inactivated states of TRPV channels. Teng J, Anishkin A, Kung C, Blount P. Proc Natl Acad Sci U S A 116 9410-9416 (2019)
  22. [Structural modeling of selectivity filter in transient receptor pontential melastatin 8 ion channel]. Xu L, Yang F. Zhejiang Da Xue Xue Bao Yi Xue Ban 48 19-24 (2019)
  23. β-Lactam TRPM8 Antagonists Derived from Phe-Phenylalaninol Conjugates: Structure-Activity Relationships and Antiallodynic Activity. Martín-Escura C, Bonache MÁ, Medina JA, Medina-Peris A, De Andrés-López J, González-Rodríguez S, Kerselaers S, Fernández-Ballester G, Voets T, Ferrer-Montiel A, Fernández-Carvajal A, González-Muñiz R. Int J Mol Sci 24 14894 (2023)


Reviews citing this publication (53)

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Articles citing this publication (72)

  1. Structure and gating mechanism of the transient receptor potential channel TRPV3. Singh AK, McGoldrick LL, Sobolevsky AI. Nat Struct Mol Biol 25 805-813 (2018)
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