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

GABRB2 (P47870) - Overview - Molecular Target Synopsis

Protein


GABRB2, Gamma-aminobutyric acid receptor subunit beta-2
UniProt P47870

Also Known as GBRB2_HUMAN, GABRB2

Ligand-gated chloride channel which is a component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the brain (PubMed:8264558, PubMed:19763268, PubMed:27789573, 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 alpha2/beta2/gamma2 receptor exhibit synaptogenic activity (PubMed:23909897, PubMed:25489750). Functions also as histamine receptor and mediates cellular responses to histamine. Heteropentamer, formed by a combination of alpha, beta, gamma, delta and rho chains (PubMed:8264558, PubMed:29950725). Interacts with UBQLN1 (By similarity). Interacts with KCTD8, KCTD12 and KCTD16; this interaction determines the pharmacology and kinetics of the receptor response, the KCTD proteins markedly accelerating the GABA-B response, although to different extents (By similarity). May interact with KIF21B (By similarity). Identified in a complex of 720 kDa composed of LHFPL4, NLGN2, GABRA1, GABRB2, GABRG2 and GABRB3.

6D6T
HUMAN GABA-A RECEPTOR ALPHA1-BETA2-GAMMA2 SUBTYPE IN COMPLEX WITH GABA AND FLUMAZENIL, CONFORMATION B
RCSB/PDB
Inspect Structure
See all 3D Structures for GABRB2

Isoforms / Transcripts (Protein Coding)


Drugs


GABRB2 is targeted by Approved Drugs Ethchlorvynol, Clobazam, Eszopiclone. (see details)
Ethchlorvynol
Clobazam
Eszopiclone

Sub-cellular localization


UniProt: GABRB2 is active in the following subcellular-locations: cell junction, cell membrane, cytoplasmic vesicle membrane, postsynaptic cell membrane, synapse.
GO terms: GABRB2 is active in the following subcellular-locations: cell junction, chloride channel complex, cytoplasmic vesicle membrane, cytosol, extracellular exosome, GABA-A receptor complex, GABA-ergic synapse, integral component of plasma membrane, integral component of postsynaptic specialization membrane, neuron projection, plasma membrane, synapse.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project GABRB2 has gain in 0 cell-lines, loss in 2 cell-lines and no signal in 1003 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: SW_620, NCI_H460, RPMI_8226

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: NCI-N417, NCI-H446, SCLC-21H

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, HMEC

(see details)

3D Structures


For GABRB2 there are:
2 structures (4 chains) solved
2 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


GABRB2 has been screened with 1261 compounds (2168 bioactivities), 356 compounds have bioactivities that show binding affinity of <= 500nM (504 bioactivities). (see details)