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

GABRG2 (P18507) - Overview - Molecular Target Synopsis

Protein


GABRG2, Gamma-aminobutyric acid receptor subunit gamma-2
UniProt P18507

Also Known as GBRG2_HUMAN, GABRG2

Ligand-gated chloride channel which is a component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the brain (PubMed:2538761, PubMed:29950725). Plays an important role in the formation of functional inhibitory GABAergic synapses in addition to mediating synaptic inhibition as a GABA-gated ion channel (PubMed:23909897, PubMed:25489750). 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 alpha1/beta2/gamma2 receptor and the alpha1/beta3/gamma2 receptor exhibit synaptogenic activity (PubMed:23909897, PubMed:25489750). The alpha2/beta2/gamma2 receptor exhibits synatogenic activity whereas the alpha2/beta3/gamma2 receptor shows very little or no synaptogenic activity (By similarity). Functions also as histamine receptor and mediates cellular responses to histamine (By similarity). Heteropentamer, formed by a combination of alpha, beta, gamma, delta and rho chains (PubMed:2538761, PubMed:29950725). Interacts with GABARAP (PubMed:9892355). Interacts with KIF21B (By similarity). Identified in a complex of 720 kDa composed of LHFPL4, NLGN2, GABRA1, GABRB2, GABRG2 and GABRB3 (By similarity). Interacts with LHFPL4 (By similarity).

6HUK
CRYOEM STRUCTURE OF HUMAN FULL-LENGTH ALPHA1BETA3GAMMA2L GABA(A)R IN COMPLEX WITH BICUCULLINE AND MEGABODY MB38.
RCSB/PDB
Inspect Structure
See all 3D Structures for GABRG2

Isoforms / Transcripts (Protein Coding)


Drugs


GABRG2 is targeted by Approved Drugs Isoflurane, Ethchlorvynol, Enflurane, Desflurane, Methohexital, Clobazam, Eszopiclone, Meprobamate, Halothane, Methoxyflurane, Sevoflurane. (see details)
Isoflurane
Ethchlorvynol
Enflurane
Desflurane
Methohexital
Clobazam
Eszopiclone
Meprobamate
Halothane
Methoxyflurane
Sevoflurane

Sub-cellular localization


UniProt: GABRG2 is active in the following subcellular-locations: cell junction, cell membrane, cell projection, cytoplasmic vesicle membrane, dendrite, postsynaptic cell membrane, synapse.
GO terms: GABRG2 is active in the following subcellular-locations: axon, cell junction, chloride channel complex, cytoplasmic vesicle membrane, dendrite membrane, GABA-A receptor complex, GABA-ergic synapse, integral component of plasma membrane, neuron projection, plasma membrane, postsynapse, postsynaptic membrane, synapse.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project GABRG2 has gain in 0 cell-lines, loss in 2 cell-lines and no signal in 1001 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: MCF7, HL_60, UACC_62

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: DMS 53, NCI-H727, 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


For GABRG2 there are:
8 structures (8 chains) solved
8 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


GABRG2 has been screened with 2045 compounds (7122 bioactivities), 1141 compounds have bioactivities that show binding affinity of <= 500nM (3331 bioactivities). (see details)