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

TRPM4 (Q8TD43) - Overview - Molecular Target Synopsis

Protein


TRPM4, Transient receptor potential cation channel subfamily M member 4
UniProt Q8TD43

Also Known as TRPM4_HUMAN, TRPM4, LTRPC4

Calcium-activated non selective (CAN) cation channel that mediates membrane depolarization (PubMed:12015988, PubMed:29211723). While it is activated by increase in intracellular Ca(2+), it is impermeable to it (PubMed:12015988). Mediates transport of monovalent cations (Na(+) > K(+) > Cs(+) > Li(+)), leading to depolarize the membrane. It thereby plays a central role in cadiomyocytes, neurons from entorhinal cortex, dorsal root and vomeronasal neurons, endocrine pancreas cells, kidney epithelial cells, cochlea hair cells etc. Participates in T-cell activation by modulating Ca(2+) oscillations after T lymphocyte activation, which is required for NFAT-dependent IL2 production. Involved in myogenic constriction of cerebral arteries. Controls insulin secretion in pancreatic beta-cells. May also be involved in pacemaking or could cause irregular electrical activity under conditions of Ca(2+) overload. Affects T-helper 1 (Th1) and T-helper 2 (Th2) cell motility and cytokine production through differential regulation of calcium signaling and NFATC1 localization. Enhances cell proliferation through up-regulation of the beta-catenin signaling pathway. Homotetramer.

6BWI
3.7 ANGSTROM CRYOEM STRUCTURE OF FULL LENGTH HUMAN TRPM4
RCSB/PDB
Inspect Structure
See all 3D Structures for TRPM4

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: TRPM4 is active in the following subcellular-locations: cell membrane, endoplasmic reticulum, golgi apparatus.
GO terms: TRPM4 is active in the following subcellular-locations: cytosol, endoplasmic reticulum, Golgi apparatus, neuronal cell body, nucleoplasm, plasma membrane, sodium channel complex, spanning component of membrane, spanning component of plasma membrane.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project TRPM4 has gain in 2 cell-lines, loss in 2 cell-lines and no signal in 999 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: HL_60, SR, T47D

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: NCI-H1781, NCI-H2126, HCC1263

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, K562, HUVEC

(see details)

3D Structures


For TRPM4 there are:
4 structures (16 chains) solved
4 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


TRPM4 has been screened with 1 compounds (1 bioactivities). (see details)