Target Information
Target General Infomation | |||||
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Target ID |
T64213
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Former ID |
TTDR01160
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Target Name |
Transient receptor potential cation channel subfamily V member 4
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Gene Name |
TRPV4
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Synonyms |
OTRPC4; Osm-9-like TRP channel 4; TRP12; Transient receptor potential protein 12; TrpV4; VR-OAC; VRL-2; VRL2; VROAC; Vanilloid receptor-like channel 2; Vanilloid receptor-like protein 2; Vanilloid receptor-related osmotically-activated channel; TRPV4
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Target Type |
Research
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Function |
Non-selective calcium permeant cation channel probably involved in osmotic sensitivity and mechanosensitivity. Activation by exposure to hypotonicity within the physiological range exhibits an outward rectification. Also activated by low pH, citrate and phorbolesters. Increase of intracellular Ca(2+) potentiates currents. Channel activity seems to be regulated by a calmodulin-dependent mechanism with a negative feedback mechanism. Promotes cell-cell junction formation in skin keratinocytes and plays an important role in the formation and/or maintenance of functional intercellular barriers. Acts as a regulator of intracellular Ca(2+) in synoviocytes. Plays an obligatory role as a molecular component in the nonselective cation channel activation induced by 4-alpha-phorbol 12,13-didecanoate and hypotonic stimulation in synoviocytes and also regulates production of IL-8. {ECO:0000269|PubMed:11025659, ECO:0000269|PubMed:12724311, ECO:0000269|PubMed:19759329}.
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BioChemical Class |
Transient receptor family
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Target Validation |
T64213
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UniProt ID | |||||
Sequence |
MADSSEGPRAGPGEVAELPGDESGTPGGEAFPLSSLANLFEGEDGSLSPSPADASRPAGP
GDGRPNLRMKFQGAFRKGVPNPIDLLESTLYESSVVPGPKKAPMDSLFDYGTYRHHSSDN KRWRKKIIEKQPQSPKAPAPQPPPILKVFNRPILFDIVSRGSTADLDGLLPFLLTHKKRL TDEEFREPSTGKTCLPKALLNLSNGRNDTIPVLLDIAERTGNMREFINSPFRDIYYRGQT ALHIAIERRCKHYVELLVAQGADVHAQARGRFFQPKDEGGYFYFGELPLSLAACTNQPHI VNYLTENPHKKADMRRQDSRGNTVLHALVAIADNTRENTKFVTKMYDLLLLKCARLFPDS NLEAVLNNDGLSPLMMAAKTGKIGIFQHIIRREVTDEDTRHLSRKFKDWAYGPVYSSLYD LSSLDTCGEEASVLEILVYNSKIENRHEMLAVEPINELLRDKWRKFGAVSFYINVVSYLC AMVIFTLTAYYQPLEGTPPYPYRTTVDYLRLAGEVITLFTGVLFFFTNIKDLFMKKCPGV NSLFIDGSFQLLYFIYSVLVIVSAALYLAGIEAYLAVMVFALVLGWMNALYFTRGLKLTG TYSIMIQKILFKDLFRFLLVYLLFMIGYASALVSLLNPCANMKVCNEDQTNCTVPTYPSC RDSETFSTFLLDLFKLTIGMGDLEMLSSTKYPVVFIILLVTYIILTFVLLLNMLIALMGE TVGQVSKESKHIWKLQWATTILDIERSFPVFLRKAFRSGEMVTVGKSSDGTPDRRWCFRV DEVNWSHWNQNLGIINEDPGKNETYQYYGFSHTVGRLRRDRWSSVVPRVVELNKNSNPDE VVVPLDSMGNPRCDGHQQGYPRKWRTDDAPL |
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Structure |
4DX1; 4DX2
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Inhibitor | 4-Pyridin-2-yl-piperazine-1-carboxylic acid amide | Drug Info | [527001] | ||
CAPSAZEPINE | Drug Info | [526604] | |||
IODORESINIFERATOXIN | Drug Info | [527001] | |||
MK-056 | Drug Info | [526897] | |||
Pyrrolidin-1-yl-thiourea | Drug Info | [527001] | |||
SC-0030 | Drug Info | [526897] | |||
Activator | 4alpha-PDD | Drug Info | [526264] | ||
4alpha-PDH | Drug Info | [530069] | |||
5,6-epoxyeicosatrienoic acid | Drug Info | [526681] | |||
bisandrographolide | Drug Info | [528361] | |||
citric acid | Drug Info | [526597] | |||
GSK1016790A | Drug Info | [529487] | |||
phorbol 12-myristate 13-acetate | Drug Info | [526264] | |||
RN1747 | Drug Info | [530364] | |||
Blocker (channel blocker) | GSK2193874 | Drug Info | [532109] | ||
HC067047 | Drug Info | [531222] | |||
RN1734 | Drug Info | [530364] | |||
Pathways | |||||
KEGG Pathway | Inflammatory mediator regulation of TRP channels | ||||
Reactome | TRP channels | ||||
References | |||||
Ref 526264 | Activation of TRPV4 channels (hVRL-2/mTRP12) by phorbol derivatives. J Biol Chem. 2002 Apr 19;277(16):13569-77. Epub 2002 Feb 4. | ||||
Ref 526597 | Impaired pressure sensation in mice lacking TRPV4. J Biol Chem. 2003 Jun 20;278(25):22664-8. Epub 2003 Apr 13. | ||||
Ref 526604 | Bioorg Med Chem Lett. 2003 May 5;13(9):1549-52.Chain-branched acyclic phenethylthiocarbamates as vanilloid receptor antagonists. | ||||
Ref 526681 | Anandamide and arachidonic acid use epoxyeicosatrienoic acids to activate TRPV4 channels. Nature. 2003 Jul 24;424(6947):434-8. | ||||
Ref 526897 | Bioorg Med Chem Lett. 2003 Dec 15;13(24):4389-93.Novel non-vanilloid VR1 antagonist of high analgesic effects and its structural requirement for VR1 antagonistic effects. | ||||
Ref 527001 | Bioorg Med Chem Lett. 2004 Apr 5;14(7):1693-6.N-4-methansulfonamidobenzyl-N'-2-substituted-4-tert-butyl-benzyl thioureas as potent vanilloid receptor antagonistic ligands. | ||||
Ref 528361 | Bisandrographolide from Andrographis paniculata activates TRPV4 channels. J Biol Chem. 2006 Oct 6;281(40):29897-904. Epub 2006 Aug 9. | ||||
Ref 529487 | N-((1S)-1-{[4-((2S)-2-{[(2,4-dichlorophenyl)sulfonyl]amino}-3-hydroxypropanoyl)-1-piperazinyl]carbonyl}-3-methylbutyl)-1-benzothiophene-2-carboxamide (GSK1016790A), a novel and potent transient receptor potential vanilloid 4 channel agonist induces urinary bladder contraction and hyperactivity: Part I. J Pharmacol Exp Ther. 2008 Aug;326(2):432-42. | ||||
Ref 530069 | Modulation of the transient receptor potential vanilloid channel TRPV4 by 4alpha-phorbol esters: a structure-activity study. J Med Chem. 2009 May 14;52(9):2933-9. | ||||
Ref 530364 | Identification and characterization of novel TRPV4 modulators. Biochem Biophys Res Commun. 2009 Nov 20;389(3):490-4. |
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