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

GABRA2 (P47869) - Overview - Molecular Target Synopsis

Protein


GABRA2, Gamma-aminobutyric acid receptor subunit alpha-2
UniProt P47869

Also Known as GBRA2_HUMAN, GABRA2

Ligand-gated chloride channel which is a component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the brain (By similarity). Plays an important role in the formation of functional inhibitory GABAergic synapses in addition to mediating synaptic inhibition as a GABA-gated ion channel (By similarity). The gamma2 subunit is necessary but not sufficient for a rapid formation of active synaptic contacts and the synaptogenic effect of this subunit is influenced by the type of alpha and beta subunits present in the receptor pentamer (By similarity). The alpha2/beta2/gamma2 receptor exhibits synaptogenic activity whereas the alpha2/beta3/gamma2 receptor shows very little or no synaptogenic activity (By similarity). Heteropentamer, formed by a combination of alpha, beta, gamma, delta and rho chains (By similarity). Interacts with UBQLN1 (By similarity). Interacts with KIF21B (By similarity). Interacts with LHFPL4 (By similarity).

Isoforms / Transcripts (Protein Coding)


Drugs


GABRA2 is targeted by Approved Drugs Eszopiclone, Ethchlorvynol, Methohexital, Clobazam. (see details)
Eszopiclone
Ethchlorvynol
Methohexital
Clobazam

Sub-cellular localization


UniProt: GABRA2 is active in the following subcellular-locations: cell junction, cell membrane, cell projection, cytoplasmic vesicle membrane, dendrite, postsynaptic cell membrane, synapse.
GO terms: GABRA2 is active in the following subcellular-locations: cell junction, chloride channel complex, dendrite membrane, GABA-A receptor complex, integral component of plasma membrane, integral component of synaptic vesicle membrane, neuron projection, plasma membrane, postsynapse, postsynaptic membrane, synapse.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project GABRA2 has gain in 0 cell-lines, loss in 6 cell-lines and no signal in 999 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: SF_295, HOP_62, MCF7

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: PSN1, Hs 675.T, SNU-182

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 75% identity similarity to GABRA2 there are:
13 structures (31 chains) solved
13 are solved in complex with at least one small molecule ligand
4 are solved with an approved drug

GABRA2 is solved in complex with the approved drug(s):

FYP/FLUMAZENIL (6D6T_D, 6D6U_D),
08H/ALPRAZOLAM (6HUO_D),
DZP/DIAZEPAM (6HUP_D).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


GABRA2 has been screened with 1489 compounds (2278 bioactivities), 814 compounds have bioactivities that show binding affinity of <= 500nM (1067 bioactivities). (see details)