TRPM8 | Transient Receptor Potential Cation Channel M8

Family:
Transient  receptor potential channels

Subgroups:
TRPC (TRPC1–TRPC7), TRPV (TRPV1-TRPV6), TRPA1, TRPM (TRPM1–TRPM8), TRPP (TRPP1–TRPP3, PKD1, PKDREJ, PKDL1–PKDL3), TRPML (TRPML1–TRPML3), TRPN

Topology:
Most TRP channels are composed of 6 transmembrane domains (helices) with intracellular N- and C-termini, non-selectively permeable to various cations

TRPM8: Background information

TRPM8, also known as the cold and menthol receptor 1 (CMR1) is the primary transducer of cold somatosensation in humans. The TRPM8 channel is a homotetramer, composed of four identical subunits with a transmembrane domain with six helices (S1–6). TRPM8 is an ion channel, upon activation it allows the entry of Na+ and Ca2+ ions to the cell that leads to depolarization and the generation of an action potential and it is activated by cold temperatures and cooling agents, such as menthol and icilin.

Gene:
TRPM8

Human Protein:
UniProt Q7Z2W7

Tissue:
Sensory neurons, dorsal root ganglia neurons, prostate, lung, bladder, prostatae tumors

Function/ Application:
Temperature transducer for ‘‘cold’’, proliferation, generation of an action potential

Pathology:
Cancer, thermoception, neuropathic pain, migrane, dentin sensitivity

Interaction:
TCAF1, PIP2, Gαq, Protein phosphatase 1, Ubiquitin specific peptidase 10

Modulator:
Cilin, eucalyptol, menthol, capsaicin, ethanol, linalool, geraniol, capsazepine , BCTC, cannabidiol

Assays:
Patch Clamp: whole cell, room temperature, State- and use-dependence

Particularities:
TRPM8 is a ligand-gated, intracellular pH- and thermo-sensitive ion channel

Recommended Reviews:
International Union of Pharmacology. XLIII. Compendium of voltage-gated ion channels: transient receptor potential channels., Pharmacol Rev 55(4):591-6 Clapham, et al. 2003  

Data and Applications

TRPM8 / TRPV1 - Pharmacology

icon pap   Port-a-Patch data and applications:p15 1 TRP 
TRPV1 data were kindly supplied by Dr. David Cohen, Oregon Health and Service University, Portland, OR, USA.

TRP channels recorded in HEK293 cells. Menthol (dark blue) activated the TRPM8 channels (shown on the left) and could be inhibited by genistein (blue). TRPV1 channels expressed in HEK293 cells (right) were stimulated by application of capsaicin.

TRPM8 - Activated by Menthol

AN Port a Patch TRPV1M8 2icon pap   Port-a-Patch data and applications:

External application of 300 µM menthol activated the TRPM8 channels expressed in HEK293 cells.

 

 

 

Application Notes

Publications

2018 - Vascular Endothelial Growth Factor (VEGF) Induced Downstream Responses to Transient Receptor Potential Vanilloid 1 (TRPV1) and 3-Iodothyronamine (3-T1AM) in Human Corneal Keratocytes

icon pap   Port-a-Patch publication in Frontiers in Pharmacology (2018)

Authors:
Türker, E., Garreis, F., Khajavi, N., Reinach, P.S., Joshi, P., Brockmann, T., Lucius, A., Ljubojevic, N., Turan, E., Cooper, D., Schick, F., Reinholz, R., Pleyer, U., Köhrle, J., Mergler, S.

2018 - TRPM8 Activation via 3-Iodothyronamine Blunts VEGF-Induced Transactivation of TRPV1 in Human Uveal Melanoma Cells

icon pap   Port-a-Patch publication in Frontiers in Pharmacology (2018)

Authors:
Walcher, L., Budde, C., Böhm, A., Reinach, P.S., Dhandapani, P., Ljubojevic, N., Schweiger, M.W., von der Waydbrink, H., Reimers, I., Köhrle, J., Mergler, S.

2018 - 3-Iodothyronamine Activates a Set of Membrane Proteins in Murine Hypothalamic Cell Lines

icon pap   Port-a-Patch publication in Frontiers in Endocrinology (2018)

Authors:
Bräunig J., Mergler S., Jyrch S., Hoefig C.S., Rosowski M., Mittag J., Biebermann H., Khajavi N.

2014 - Calcium regulation by temperature-sensitive transient receptor potential channels in human uveal melanoma cells

icon pap  Port-a-Patch publication in Cellular Signalling (2014)

Authors:
Mergler S., Derckx R., Reinach P.S., Garreis F., Böhm A., Schmelzer L., Skosyrski S., Ramesh N., Abdelmessih S., Polat O.K., Khajavi N., Riechardt A.I.

2013 - Functional significance of thermosensitive transient receptor potential melastatin channel 8 (TRPM8) expression in immortalized human corneal endothelial cells

icon pap  Port-a-Patch publication in Experimental Eye Research (2013)

Authors: 
Mergler S., Mertens C., Valtink M., Reinach P.S., Castelo Székely V., Slavi N., Abdelmessih S., Türker E., Fels G., Pleyer U.

Subgroups
%MCEPASTEBIN%
selectively permeable
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