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

TRPV6 (Q9H1D0) - Overview - Molecular Target Synopsis

Protein


TRPV6, Transient receptor potential cation channel subfamily V member 6
UniProt Q9H1D0

Also Known as TRPV6_HUMAN, TRPV6, ECAC2

Calcium selective cation channel that mediates Ca(2+) uptake in various tissues, including the intestine (PubMed:11097838, PubMed:11278579, PubMed:11248124 PubMed:15184369, PubMed:23612980, PubMed:29258289). Important for normal Ca(2+) ion homeostasis in the body, including bone and skin (By similarity). The channel is activated by low internal calcium level, probably including intracellular calcium store depletion, and the current exhibits an inward rectification (PubMed:15184369). Inactivation includes both a rapid Ca(2+)-dependent and a slower Ca(2+)-calmodulin-dependent mechanism; the latter may be regulated by phosphorylation. In vitro, is slowly inhibited by Mg(2+) in a voltage-independent manner. Heteromeric assembly with TRPV5 seems to modify channel properties. TRPV5-TRPV6 heteromultimeric concatemers exhibit voltage-dependent gating. Homotetramer (PubMed:29258289). Probably forms also heterotetramers with TRPV5. Interacts with TRPV5. Interacts with S100A10 and probably with the ANAX2-S100A10 heterotetramer. The interaction with S100A10 is required for the trafficking to the plasma membrane. Interacts with BSPRY (By similarity). Interacts with TCAF1 and TCAF2 isoform 2 (PubMed:25559186). Interacts with calmodulin (PubMed:11248124).

6E2F
CRYO-EM STRUCTURE OF HUMAN TRPV6 IN COMPLEX WITH CALMODULIN
RCSB/PDB
Inspect Structure
See all 3D Structures for TRPV6

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: TRPV6 is active in the following subcellular-locations: cell membrane.
GO terms: TRPV6 is active in the following subcellular-locations: integral component of plasma membrane, plasma membrane.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project TRPV6 has gain in 5 cell-lines, loss in 0 cell-lines and no signal in 1000 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: T47D, NCI_H460, UACC_62

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: RT4, HCC1954, MDA-MB-361

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: K562, SK-N-SH, NHLF

(see details)

3D Structures


For TRPV6 there are:
6 structures (24 chains) solved
1 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


TRPV6 has been screened with 42 compounds (85 bioactivities). (see details)