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Ligand stoichiometry of the cold‐ and menthol‐activated channel TRPM8
Author(s) -
Janssens Annelies,
Voets Thomas
Publication year - 2011
Publication title -
the journal of physiology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.802
H-Index - 240
eISSN - 1469-7793
pISSN - 0022-3751
DOI - 10.1113/jphysiol.2011.216523
Subject(s) - trpm8 , transient receptor potential channel , chemistry , menthol , ligand (biochemistry) , ion channel , stoichiometry , biophysics , ligand gated ion channel , receptor , biochemistry , biology , trpv1 , organic chemistry
Non‐Technical Summary The ion channel TRPM8, which is present in nerves that innervate the skin and mouth, mediates the sensation of cold temperatures and of chemical substances that evoke a cold sensation, such as menthol or eucalyptol. The molecular structures and biophysical mechanisms that allow this and related channels to integrate thermal and chemical information are poorly understood. In this work, we demonstrate that TRPM8 is able to bind up to four menthol molecules, and that every bound menthol molecule causes an equivalent stabilization of the open state of the channel. These results provide important fundamental insight into the working mechanism of temperature‐sensitive channels, and may assist in the development of drugs to treat oversensitivity to cold temperatures and pain.