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

TRPA1 (O75762) - Overview - Molecular Target Synopsis

Protein


TRPA1, Transient receptor potential cation channel subfamily A member 1
UniProt O75762

Also Known as TRPA1_HUMAN, TRPA1, ANKTM1

Receptor-activated non-selective cation channel involved in detection of pain and possibly also in cold perception and inner ear function (PubMed:25389312, PubMed:25855297). Has a central role in the pain response to endogenous inflammatory mediators and to a diverse array of volatile irritants, such as mustard oil, cinnamaldehyde, garlic and acrolein, an irritant from tears gas and vehicule exhaust fumes (PubMed:25389312, PubMed:20547126). Is also activated by menthol (in vitro)(PubMed:25389312). Acts also as an ionotropic cannabinoid receptor by being activated by delta(9)-tetrahydrocannabinol (THC), the psychoactive component of marijuana (PubMed:25389312). May be a component for the mechanosensitive transduction channel of hair cells in inner ear, thereby participating in the perception of sounds. Probably operated by a phosphatidylinositol second messenger system (By similarity). Homotetramer (PubMed:25389312, PubMed:25855297). Interacts with TMEM100 (By similarity).

6HC8
16 RESIDUE FRAGMENT OF
TRANSIENT RECEPTOR POTENTIAL CATION CHANNEL SUBFAMILY AMEMBER 1
IN THE STRUCTURE OF
FACTOR INHIBITING HIF (FIH) IN COMPLEX WITH ZINC, NOG AND TRPA1 (313- 339)
RCSB/PDB
Inspect Structure
See all 3D Structures for TRPA1

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
1119ENSG00000104321ENST00000262209ENSP00000262209O75762-1
916ENSG00000104321ENST00000523582ENSP00000428151

Drugs


TRPA1 is targeted by Approved Drug Menthol. (see details)
Menthol

Sub-cellular localization


UniProt: TRPA1 is active in the following subcellular-locations: cell membrane.
GO terms: TRPA1 is active in the following subcellular-locations: integral component of plasma membrane, plasma membrane, stereocilium bundle.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project TRPA1 has gain in 13 cell-lines, loss in 3 cell-lines and no signal in 988 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: SF_295, HS578T, SF_539

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: Hs 675.T, NCI-H1623, Hs 895.T

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: AG445, NHLF, SK-N-SH

(see details)

3D Structures


For TRPA1 there are:
2 structures (5 chains) solved
0 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


TRPA1 has been screened with 791 compounds (1273 bioactivities), 293 compounds have bioactivities that show binding affinity of <= 500nM (342 bioactivities). (see details)