Molecular Target Synopsis
Overview
Domains and Structures
Drugs and Clinical Candidates
Druggability
Chemistry
Ligand Efficiency Plot
Pathways
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
RNAi
Mutations
Germline Genetics

TRPV1 (Q8NER1) - Overview - Molecular Target Synopsis

Protein


TRPV1, Transient receptor potential cation channel subfamily V member 1
UniProt Q8NER1

Also Known as TRPV1_HUMAN, TRPV1, VR1

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. 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. 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. Interacts with PIRT (By similarity). Homotetramer (By similarity). Interacts with TRPV3 and may also form a heteromeric channel with TRPV3 (PubMed:12077606). Interacts with CALM, PRKCM and CSK. Interacts with PRKCG and NTRK1, probably by forming a trimeric complex (By similarity). Interacts with the Scolopendra mutilans RhTx toxin (By similarity). Interacts with TMEM100 (By similarity). Interacts with PACS2 (PubMed:29656858).

Isoforms / Transcripts (Protein Coding)


Drugs


TRPV1 is targeted by Approved Drug Capsaicin. (see details)
Capsaicin

Sub-cellular localization


UniProt: TRPV1 is active in the following subcellular-locations: cell junction, cell membrane, cell projection, dendritic spine membrane, postsynaptic cell membrane, synapse.
GO terms: TRPV1 is active in the following subcellular-locations: cell junction, cytosol, dendritic spine membrane, external side of plasma membrane, integral component of membrane, integral component of plasma membrane, intrinsic component of plasma membrane, mitochondrion, neuronal cell body, plasma membrane, postsynaptic membrane.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project TRPV1 has gain in 0 cell-lines, loss in 3 cell-lines and no signal in 1002 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: HCT_15, CCRF_CEM, IGROV1

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: Hs 746T, NCI-H209, NCI-H209

In Array Express (RNA-seq of long poly adenylated RNA and long non poly adenylated RNA from ENCODE cell lines), the highest expressing cell lines are: SK-N-SH, SK-N-SH, NHLF

(see details)

3D Structures


At greater than 90% identity similarity to TRPV1 there are:
1 structures (1 chains) solved
0 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


TRPV1 has been screened with 3920 compounds (6230 bioactivities), 2435 compounds have bioactivities that show binding affinity of <= 500nM (3530 bioactivities). (see details)