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Current View of Ligand and Lipid Recognition by the Menthol Receptor TRPM8.

Publication ,  Journal Article
Yin, Y; Lee, S-Y
Published in: Trends Biochem Sci
September 2020

Transient receptor potential (TRP) melastatin member 8 (TRPM8), which is a calcium-permeable ion channel, functions as the primary molecular sensor of cold and menthol in humans. Recent cryoelectron microscopy (cryo-EM) studies of TRPM8 have shown distinct structural features in its architecture and domain assembly compared with the capsaicin receptor TRP vanilloid member 1 (TRPV1). Moreover, ligand-bound TRPM8 structures have uncovered unforeseen binding sites for both cooling agonists and membrane lipid phosphatidylinositol 4,5-bisphosphate [PI(4,5)P2]. These complex structures unveil the molecular basis of cooling agonist sensing by TRPM8 and the allosteric role of PI(4,5)P2 in agonist binding for TRPM8 activation. Here, we review the recent advances in TRPM8 structural biology and investigate the molecular principles governing the distinguishing role of TRPM8 as the evolutionarily conserved menthol receptor.

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Published In

Trends Biochem Sci

DOI

ISSN

0968-0004

Publication Date

September 2020

Volume

45

Issue

9

Start / End Page

806 / 819

Location

England

Related Subject Headings

  • TRPM Cation Channels
  • Phosphatidylinositols
  • Menthol
  • Ligands
  • Humans
  • Developmental Biology
  • Cryoelectron Microscopy
  • 3404 Medicinal and biomolecular chemistry
  • 3205 Medical biochemistry and metabolomics
  • 3101 Biochemistry and cell biology
 

Citation

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Yin, Y., & Lee, S.-Y. (2020). Current View of Ligand and Lipid Recognition by the Menthol Receptor TRPM8. Trends Biochem Sci, 45(9), 806–819. https://doi.org/10.1016/j.tibs.2020.05.008
Yin, Ying, and Seok-Yong Lee. “Current View of Ligand and Lipid Recognition by the Menthol Receptor TRPM8.Trends Biochem Sci 45, no. 9 (September 2020): 806–19. https://doi.org/10.1016/j.tibs.2020.05.008.
Yin Y, Lee S-Y. Current View of Ligand and Lipid Recognition by the Menthol Receptor TRPM8. Trends Biochem Sci. 2020 Sep;45(9):806–19.
Yin, Ying, and Seok-Yong Lee. “Current View of Ligand and Lipid Recognition by the Menthol Receptor TRPM8.Trends Biochem Sci, vol. 45, no. 9, Sept. 2020, pp. 806–19. Pubmed, doi:10.1016/j.tibs.2020.05.008.
Yin Y, Lee S-Y. Current View of Ligand and Lipid Recognition by the Menthol Receptor TRPM8. Trends Biochem Sci. 2020 Sep;45(9):806–819.
Journal cover image

Published In

Trends Biochem Sci

DOI

ISSN

0968-0004

Publication Date

September 2020

Volume

45

Issue

9

Start / End Page

806 / 819

Location

England

Related Subject Headings

  • TRPM Cation Channels
  • Phosphatidylinositols
  • Menthol
  • Ligands
  • Humans
  • Developmental Biology
  • Cryoelectron Microscopy
  • 3404 Medicinal and biomolecular chemistry
  • 3205 Medical biochemistry and metabolomics
  • 3101 Biochemistry and cell biology