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

GLRA3 (O75311) - Overview - Molecular Target Synopsis

Protein


GLRA3, Glycine receptor subunit alpha-3
UniProt O75311

Also Known as GLRA3_HUMAN, GLRA3

Glycine receptors are ligand-gated chloride channels. Channel opening is triggered by extracellular glycine (PubMed:9677400, PubMed:26416729). Channel characteristics depend on the subunit composition; heteropentameric channels display faster channel closure (By similarity). Plays an important role in the down-regulation of neuronal excitability (By similarity). Contributes to the generation of inhibitory postsynaptic currents (By similarity). Contributes to increased pain perception in response to increased prostaglandin E2 levels (By similarity). Plays a role in cellular responses to ethanol. Homopentamer (in vitro) (PubMed:26416729). Heteropentamer composed of GLRA3 and GLRB. Both homopentamers and heteropentamers form functional ion channels, but their characteristics are subtly different.

5VDH
CRYSTAL STRUCTURE OF HUMAN GLYCINE RECEPTOR ALPHA-3 BOUND TO AM-3607, GLYCINE, AND IVERMECTIN
RCSB/PDB
Inspect Structure
See all 3D Structures for GLRA3

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
464ENSG00000145451ENST00000274093ENSP00000274093O75311-1
449ENSG00000145451ENST00000340217ENSP00000345284O75311-2

Sub-cellular localization


UniProt: GLRA3 is active in the following subcellular-locations: cell junction, cell membrane, cell projection, dendrite, perikaryon, postsynaptic cell membrane, synapse.
GO terms: GLRA3 is active in the following subcellular-locations: cell junction, dendrite, glycine-gated chloride channel complex, integral component of plasma membrane, neuron projection, perikaryon, plasma membrane, postsynaptic membrane, synapse.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project GLRA3 has gain in 0 cell-lines, loss in 14 cell-lines and no signal in 991 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: MCF7, SK_OV_3, TK_10

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: Hs 746T, LN-18, HCC12

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, NHLF, HSMM

(see details)

3D Structures


For GLRA3 there are:
5 structures (25 chains) solved
5 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


GLRA3 has been screened with 14 compounds (26 bioactivities). (see details)