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

GLRA2 (P23416) - Overview - Molecular Target Synopsis

Protein


GLRA2, Glycine receptor subunit alpha-2
UniProt P23416

Also Known as GLRA2_HUMAN, GLRA2

Glycine receptors are ligand-gated chloride channels. Channel opening is triggered by extracellular glycine (PubMed:2155780, PubMed:15302677, PubMed:16144831, PubMed:23895467, PubMed:25445488). Channel opening is also triggered by taurine and beta-alanine (PubMed:15302677). Plays a role in the down-regulation of neuronal excitability. Contributes to the generation of inhibitory postsynaptic currents (PubMed:25445488). Plays a role in cellular responses to ethanol (PubMed:23895467). Homopentamer (in vitro). Interacts with GLRB (PubMed:16144831). Heteropentamer composed of GLRA2 and GLRB. Both homopentamers and heteropentamers form functional ion channels, but their characteristics are subtly different (PubMed:15302677).

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: GLRA2 is active in the following subcellular-locations: cell junction, cell membrane, cell projection, postsynaptic cell membrane, synapse.
GO terms: GLRA2 is active in the following subcellular-locations: cell junction, chloride channel complex, glycinergic synapse, integral component of plasma membrane, neuron projection, plasma membrane, postsynaptic membrane, synapse.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project GLRA2 has gain in 1 cell-lines, loss in 52 cell-lines and no signal in 952 cell-lines. (see details)

Gene Expression


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

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: NCI-H716, Hs 746T, 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, NHLF, HSMM

(see details)

3D Structures


At greater than 90% identity similarity to GLRA2 there are:
8 structures (40 chains) solved
8 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


GLRA2 has been screened with 38 compounds (49 bioactivities). (see details)