Proteins > Transient receptor potential cation channel subfamily M member 8
Page last updated: 2024-08-07 18:45:17
Transient receptor potential cation channel subfamily M member 8
A transient receptor potential cation channel TRPM8 that is encoded in the genome of human. [PRO:CNA, UniProtKB:Q7Z2W7]
Synonyms
Long transient receptor potential channel 6;
LTrpC-6;
LTrpC6;
Transient receptor potential p8;
Trp-p8
Research
Bioassay Publications (13)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 2 (15.38) | 29.6817 |
2010's | 8 (61.54) | 24.3611 |
2020's | 3 (23.08) | 2.80 |
Compounds (19)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
menthol | Homo sapiens (human) | EC50 | 122.3667 | 9 | 9 |
menthol | Homo sapiens (human) | Kd | 14.4000 | 1 | 1 |
menthol | Homo sapiens (human) | EC50 | 10.1000 | 1 | 1 |
ag 3-5 | Homo sapiens (human) | EC50 | 0.1800 | 2 | 2 |
geraniol | Homo sapiens (human) | EC50 | 5,900.0000 | 1 | 1 |
Drugs with Other Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
menthol | Homo sapiens (human) | Activity | 10.0000 | 1 | 1 |
eucalyptol | Homo sapiens (human) | Activity | 100.0000 | 1 | 1 |
ag 3-5 | Homo sapiens (human) | Activity | 0.0990 | 1 | 1 |
Serendipity in drug-discovery: a new series of 2-(benzyloxy)benzamides as TRPM8 antagonists.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 23, Issue:22, 2013
TRPM8 voltage sensor mutants reveal a mechanism for integrating thermal and chemical stimuli.Nature chemical biology, , Volume: 3, Issue:3, 2007
Sensing with TRP channels.Nature chemical biology, , Volume: 1, Issue:2, 2005
Serendipity in drug-discovery: a new series of 2-(benzyloxy)benzamides as TRPM8 antagonists.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 23, Issue:22, 2013
Transient receptor potential ankyrin 1 (TRPA1) channel as emerging target for novel analgesics and anti-inflammatory agents.Journal of medicinal chemistry, , Jul-22, Volume: 53, Issue:14, 2010
Sensing with TRP channels.Nature chemical biology, , Volume: 1, Issue:2, 2005
The Discovery of Novel ACA Derivatives as Specific TRPM2 Inhibitors that Reduce Ischemic Injury Both In Vitro and In Vivo.Journal of medicinal chemistry, , 04-08, Volume: 64, Issue:7, 2021
Design, synthesis and biological activities of 2,3-dihydroquinazolin-4(1H)-one derivatives as TRPM2 inhibitors.European journal of medicinal chemistry, , May-25, Volume: 152, 2018
Identification of a Potent Tryptophan-Based TRPM8 Antagonist With in Vivo Analgesic Activity.Journal of medicinal chemistry, , Jul-26, Volume: 61, Issue:14, 2018
Synthesis and pharmacological evaluation of novel N-aryl-3,4-dihydro-1'H-spiro[chromene-2,4'-piperidine]-1'-carboxamides as TRPM8 antagonists.Bioorganic & medicinal chemistry, , Nov-01, Volume: 21, Issue:21, 2013
Enables
This protein enables 4 target(s):
Target | Category | Definition |
calcium channel activity | molecular function | Enables the facilitated diffusion of a calcium ion (by an energy-independent process) involving passage through a transmembrane aqueous pore or channel without evidence for a carrier-mediated mechanism. [GOC:mtg_transport, GOC:pr, ISBN:0815340729] |
protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
identical protein binding | molecular function | Binding to an identical protein or proteins. [GOC:jl] |
ligand-gated calcium channel activity | molecular function | Enables the transmembrane transfer of a calcium ions by a channel that opens when a specific ligand has been bound by the channel complex or one of its constituent parts. [GOC:dos] |
Located In
This protein is located in 4 target(s):
Target | Category | Definition |
endoplasmic reticulum membrane | cellular component | The lipid bilayer surrounding the endoplasmic reticulum. [GOC:mah] |
plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
external side of plasma membrane | cellular component | The leaflet of the plasma membrane that faces away from the cytoplasm and any proteins embedded or anchored in it or attached to its surface. [GOC:dos, GOC:tb] |
membrane raft | cellular component | Any of the small (10-200 nm), heterogeneous, highly dynamic, sterol- and sphingolipid-enriched membrane domains that compartmentalize cellular processes. Small rafts can sometimes be stabilized to form larger platforms through protein-protein and protein-lipid interactions. [PMID:16645198, PMID:20044567] |
Active In
This protein is active in 1 target(s):
Target | Category | Definition |
plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
Involved In
This protein is involved in 6 target(s):
Target | Category | Definition |
intracellular calcium ion homeostasis | biological process | A homeostatic process involved in the maintenance of a steady state level of calcium ions within a cell. [GOC:ceb, GOC:mah] |
response to cold | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a cold stimulus, a temperature stimulus below the optimal temperature for that organism. [GOC:lr] |
calcium-mediated signaling | biological process | Any intracellular signal transduction in which the signal is passed on within the cell via calcium ions. [GOC:signaling] |
thermoception | biological process | The series of events required for an organism to receive a temperature stimulus, convert it to a molecular signal, and recognize and characterize the signal. Thermoception in larger animals is mainly done in the skin; mammals have at least two types of sensor, for detecting heat (temperatures above body temperature) and cold (temperatures below body temperature). [GOC:ai, Wikipedia:Thermoception] |
calcium ion transmembrane transport | biological process | A process in which a calcium ion is transported from one side of a membrane to the other by means of some agent such as a transporter or pore. [GOC:mah] |
positive regulation of cold-induced thermogenesis | biological process | Any process that activates or increases the frequency, rate or extent of cold-induced thermogenesis. [PMID:27876809] |