Tclin TRPM8 Transient receptor potential cation channel subfamily M member 8

Protein Summary

Description

Receptor-activated non-selective cation channel involved in detection of sensations such as coolness, by being activated by cold temperature below 25 degrees Celsius. Activated by icilin, eucalyptol, menthol, cold and modulation of intracellular pH. Involved in menthol sensation. Permeable for monovalent cations sodium, potassium, and cesium and divalent cation calcium. Temperature sensing is tightly linked to voltage-dependent gating. Activated upon depolarization, changes in temperature resulting in graded shifts of its voltage-dependent activation curves. The chemical agonist menthol functions as a gating modifier, shifting activation curves towards physiological membrane potentials. Temperature sensitivity arises from a tenfold difference in the activation energies associated with voltage-dependent opening and closing. In prostate cancer cells, shows strong inward rectification and high calcium selectivity in contrast to its behavior in normal cells which is characterized by outward rectification and poor cationic selectivity. Plays a role in prostate cancer cell migration (PubMed:25559186). Isoform 2 and isoform 3 negatively regulate menthol- and cold-induced channel activity by stabilizing the closed state of the channel.

Uniprot Accession IDs

• Q7Z2W7
• A0AVG2
• Q3YFM7
• Q6QNH9
• Q8TAC3
• Q8TDX8
• Q9BVK1

Gene Name

• TRPM8

Ensembl ID

• ENST00000324695
• ENSP00000323926
• ENSG00000144481
• ENST00000409625
• ENSP00000386771

Symbol

• LTRPC6
• TRPP8
• TRPP8
• LTRPC6
• trp-p8
• LTrpC-6

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
ligand (chemical)	0.89
cellular component	0.81
molecular function	0.76
biological term	0.58
cell type or tissue	0.57

Protein Classes

PANTHER Classes

Protein / Transporter / Ion Channel / Transient Receptor Potential Cation Channel Subfamily M Member 8

Protein / Receptor / Transient Receptor Potential Cation Channel Subfamily M Member 8

DTO Classes

Protein / Ion Channel / Transient Receptor Potential Calcium Channel (Trp-cc) Family / Ltrpc Subfamily / Trpm8 Sub-subfamily / Transient Receptor Potential Cation Channel Subfamily M Member 8

IDG Development Level Summary

Tdark

These are targets about which virtually nothing is known. They do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 873.12   (req: < 5)

Gene RIFs: 161   (req: <= 3)

Antibodies: 456   (req: <= 50)

Tbio

These targets do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 873.12   (req: >= 5)

Gene RIFs: 161   (req: > 3)

Antibodies: 456   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 10

Tchem

Target has at least one ChEMBL compound with an activity cutoff of < 30 nM - AND - satisfies the preceding conditions

Active Ligands: 517

Tclin

Target has at least one approved drug - AND - satisfies the preceding conditions

Active Drug: 1