Details of the Biological Target of DIG (DBT)

General Information of DBT (ID: ET00GTW)
Name
Transient receptor potential p8 (TRPM8)
Synonyms    Click to Show/Hide the Synonyms of This DBT
Long transient receptor potential channel 8; LTrpC-6; LTrpC6; Long transient receptor potential channel 6; TRPM8; TRPP8; Transient receptor potential cation channel subfamily M member 8; Transient receptor potential p8; Trp-p8; Cold menthol receptor 1
Family Transmembrane channel/porin (TC/P)  >>  Transient receptor potential Ca channel (TRP-CC)
Organism
Homo sapiens (Human)
Gene Name TRPM8 Gene ID
79054
UniProt ID TRPM8_HUMAN (click to find more protein-related data of this DBT)
TTD ID T41955 (click to find more therapeutic target data of this DBT)
   Click to Show/Hide the Molecular/Function Data (Sequence/Function) of This Target
Sequence
MSFRAARLSMRNRRNDTLDSTRTLYSSASRSTDLSYSESDLVNFIQANFKKRECVFFTKD
SKATENVCKCGYAQSQHMEGTQINQSEKWNYKKHTKEFPTDAFGDIQFETLGKKGKYIRL
SCDTDAEILYELLTQHWHLKTPNLVISVTGGAKNFALKPRMRKIFSRLIYIAQSKGAWIL
TGGTHYGLMKYIGEVVRDNTISRSSEENIVAIGIAAWGMVSNRDTLIRNCDAEGYFLAQY
LMDDFTRDPLYILDNNHTHLLLVDNGCHGHPTVEAKLRNQLEKYISERTIQDSNYGGKIP
IVCFAQGGGKETLKAINTSIKNKIPCVVVEGSGQIADVIASLVEVEDALTSSAVKEKLVR
FLPRTVSRLPEEETESWIKWLKEILECSHLLTVIKMEEAGDEIVSNAISYALYKAFSTSE
QDKDNWNGQLKLLLEWNQLDLANDEIFTNDRRWESADLQEVMFTALIKDRPKFVRLFLEN
GLNLRKFLTHDVLTELFSNHFSTLVYRNLQIAKNSYNDALLTFVWKLVANFRRGFRKEDR
NGRDEMDIELHDVSPITRHPLQALFIWAILQNKKELSKVIWEQTRGCTLAALGASKLLKT
LAKVKNDINAAGESEELANEYETRAVELFTECYSSDEDLAEQLLVYSCEAWGGSNCLELA
VEATDQHFIAQPGVQNFLSKQWYGEISRDTKNWKIILCLFIIPLVGCGFVSFRKKPVDKH
KKLLWYYVAFFTSPFVVFSWNVVFYIAFLLLFAYVLLMDFHSVPHPPELVLYSLVFVLFC
DEVRQWYVNGVNYFTDLWNVMDTLGLFYFIAGIVFRLHSSNKSSLYSGRVIFCLDYIIFT
LRLIHIFTVSRNLGPKIIMLQRMLIDVFFFLFLFAVWMVAFGVARQGILRQNEQRWRWIF
RSVIYEPYLAMFGQVPSDVDGTTYDFAHCTFTGNESKPLCVELDEHNLPRFPEWITIPLV
CIYMLSTNILLVNLLVAMFGYTVGTVQENNDQVWKFQRYFLVQEYCSRLNIPFPFIVFAY
FYMVVKKCFKCCCKEKNMESSVCCFKNEDNETLAWEGVMKENYLVKINTKANDTSEEMRH
RFRQLDTKLNDLKGLLKEIANKIK
Function
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.
Full List of Drug Inactive Ingredients (DIGs) Regulating This DBT
          DIG Name: Ethyl isovalerate Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Flavoring agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 > 500000 nM (tested by experiment) [1]
                   Tested Species Mus musculus (Mouse)
                   UniProt ID TRPM8_MOUSE
          DIG Name: Levomenthol Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Flavoring agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 = 10100 nM (tested by experiment) [2]
                   Tested Species Homo sapiens (Human)
                   UniProt ID TRPM8_HUMAN
          DIG Name: Menthol Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Flavoring agent
             Experiment (1) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 = 3000 nM (tested by experiment) [3]
                   Tested Species Homo sapiens (Human)
                   UniProt ID TRPM8_HUMAN
             Experiment (2) for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 = 75000 nM (tested by experiment) [4]
                   Tested Species Rattus norvegicus (Rat)
                   UniProt ID TRPM8_RAT
          DIG Name: Cinnamaldehyde Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Flavoring agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 > 500000 nM (tested by experiment) [1]
                   Tested Species Mus musculus (Mouse)
                   UniProt ID TRPM8_MOUSE
          DIG Name: Thymol Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Antioxidant; Flavoring agent; Penetration agent
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity EC50 = 52200 nM (tested by experiment) [5]
                   Tested Species Rattus norvegicus (Rat)
                   UniProt ID TRPM8_RAT
References
1 Activation and inhibition of thermosensitive TRP channels by voacangine, an alkaloid present in Voacanga africana, an African tree. J Nat Prod. 2014 Feb 28; 77(2):285-97.
2 Identification of a Novel TRPM8 Agonist from Nutmeg: A Promising Cooling Compound. ACS Med Chem Lett. 2017 May 31; 8(7):715-719.
3 Serendipity in drug-discovery: a new series of 2-(benzyloxy)benzamides as TRPM8 antagonists. Bioorg Med Chem Lett. 2013 Nov 15; 23(22):6118-22.
4 Tryptamine-Based Derivatives as Transient Receptor Potential Melastatin Type 8 (TRPM8) Channel Modulators. J Med Chem. 2016 Mar 10; 59(5):2179-91.
5 Modulation of thermo-transient receptor potential (thermo-TRP) channels by thymol-based compounds. Bioorg Med Chem Lett. 2012 May 15; 22(10):3535-9.

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