Names & Taxonomy

Uniprot ID:
Q8NER1
Entry Name:
TRPV1_HUMAN
Status:
reviewed
Protein Names:
Transient receptor potential cation channel subfamily V member 1 (TrpV1) (Capsaicin receptor) (Osm-9-like TRP channel 1) (OTRPC1) (Vanilloid receptor 1)
Gene Names:
TRPV1 VR1
Gene Names Primary:
TRPV1
Organism:
Homo sapiens (Human)

Structure

Length:
839
Sequence:
MKKWSSTDLGAAADPLQKDTCPDPLDGDPNSRPPPAKPQLSTAKSRTRLFGKGDSEEAFPVDCPHEEGELDSCPTITVSPVITIQRPGDGPTGARLLSQDSVAASTEKTLRLYDRRSIFEAVAQNNCQDLESLLLFLQKSKKHLTDNEFKDPETGKTCLLKAMLNLHDGQNTTIPLLLEIARQTDSLKELVNASYTDSYYKGQTALHIAIERRNMALVTLLVENGADVQAAAHGDFFKKTKGRPGFYFGELPLSLAACTNQLGIVKFLLQNSWQTADISARDSVGNTVLHALVEVADNTADNTKFVTSMYNEILMLGAKLHPTLKLEELTNKKGMTPLALAAGTGKIGVLAYILQREIQEPECRHLSRKFTEWAYGPVHSSLYDLSCIDTCEKNSVLEVIAYSSSETPNRHDMLLVEPLNRLLQDKWDRFVKRIFYFNFLVYCLYMIIFTMAAYYRPVDGLPPFKMEKTGDYFRVTGEILSVLGGVYFFFRGIQYFLQRRPSMKTLFVDSYSEMLFFLQSLFMLATVVLYFSHLKEYVASMVFSLALGWTNMLYYTRGFQQMGIYAVMIEKMILRDLCRFMFVYIVFLFGFSTAVVTLIEDGKNDSLPSESTSHRWRGPACRPPDSSYNSLYSTCLELFKFTIGMGDLEFTENYDFKAVFIILLLAYVILTYILLLNMLIALMGETVNKIAQESKNIWKLQRAITILDTEKSFLKCMRKAFRSGKLLQVGYTPDGKDDYRWCFRVDEVNWTTWNTNVGIINEDPGNCEGVKRTLSFSLRSSRVSGRHWKNFALVPLLREASARDRQSAQPEEVYLRQFSGSLKPEDAEVFKSPAASGEK
Proteomes:
UP000005640

Subcellular location

Subcellular Location:
Cell junction, synapse, postsynaptic cell membrane
Intramembrane:
INTRAMEM 628 650 Pore-forming.

Function

Function:
Ligand-activated non-selective calcium permeant cation channel involved in detection of noxious chemical and thermal stimuli. Seems to mediate proton influx and may be involved in intracellular acidosis in nociceptive neurons. Involved in mediation of inflammatory pain and hyperalgesia. Sensitized by a phosphatidylinositol second messenger system activated by receptor tyrosine kinases, which involves PKC isozymes and PCL. Can be activated by endogenous compounds, including 12-hydroperoxytetraenoic acid and bradykinin. Acts as ionotropic endocannabinoid receptor with central neuromodulatory effects. Triggers a form of long-term depression (TRPV1-LTD) mediated by the endocannabinoid anandamine in the hippocampus and nucleus accumbens by affecting AMPA receptors endocytosis (By similarity). Activation by vanilloids, like capsaicin, and temperatures higher than 42 degrees Celsius, exhibits a time- and Ca(2+)-dependent outward rectification, followed by a long-lasting refractory state. Mild extracellular acidic pH (6.5) potentiates channel activation by noxious heat and vanilloids, whereas acidic conditions (pH <6) directly activate the channel.
Enzyme Regulation:
ENZYME REGULATION: Channel activity is activated via the interaction with PIRT and phosphatidylinositol 4,5-bisphosphate (PIP2). Both PIRT and PIP2 are required to activate channel activity (By similarity). The channel is sensitized by ATP binding. Repeated stimulation with capsaicin gives rise to progressively smaller responses, due to desensitization. This desensitization is triggered by the influx of calcium ions and is inhibited by elevated ATP levels. Ca(2+) and CALM displace ATP from its binding site and trigger a conformation change that leads to a closed, desensitized channel. Intracellular PIP2 inhibits desensitization. The double-knot toxin (DkTx) from the Chinese earth tiger tarantula activates the channel and traps it in an open conformation (By similarity).
Cross Reference Drug Bank:
DB00132 DB00168 DB06774 DB00159
Gene Ontology Go:
cell junction
dendritic spine membrane
integral component of membrane
integral component of plasma membrane
intracellular
intrinsic component of plasma membrane
plasma membrane
postsynaptic membrane
ATP binding
calcium channel activity
calcium-release channel activity
excitatory extracellular ligand-gated ion channel activity
phosphoprotein binding
transmembrane signaling receptor activity
calcium ion transmembrane transport
cell surface receptor signaling pathway
cellular response to alkaloid
cellular response to ATP
chemosensory behavior
ion transmembrane transport
release of sequestered calcium ion into cytosol
thermoception
transmembrane transport
transport
Gene Ontology Biological Process:
calcium ion transmembrane transport
cell surface receptor signaling pathway
cellular response to alkaloid
cellular response to ATP
chemosensory behavior
ion transmembrane transport
release of sequestered calcium ion into cytosol
thermoception
transmembrane transport
transport
Gene Ontology Molecular Function:
ATP binding
calcium channel activity
calcium-release channel activity
excitatory extracellular ligand-gated ion channel activity
phosphoprotein binding
transmembrane signaling receptor activity
Gene Ontology Cellular Component:
cell junction
dendritic spine membrane
integral component of membrane
integral component of plasma membrane
intracellular
intrinsic component of plasma membrane
plasma membrane
postsynaptic membrane
Keywords:
ANK repeat
ATP-binding
Alternative splicing
Calcium
Calcium channel
Calcium transport
Calmodulin-binding
Cell junction
Cell membrane
Cell projection
Complete proteome
Glycoprotein
Ion channel
Ion transport
Membrane
Nucleotide-binding
Phosphoprotein
Polymorphism
Postsynaptic cell membrane
Reference proteome
Repeat
Synapse
Transmembrane
Transmembrane helix
Transport

Publication

PubMed ID:
11050376 11243859 11226139 11230166 16625196 15489334 12077606 14987252 14996838