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

GABRE (P78334) - Overview - Molecular Target Synopsis

Protein


GABRE, Gamma-aminobutyric acid receptor subunit epsilon
UniProt P78334

Also Known as GBRE_HUMAN, GABRE

GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel. Generally pentameric. Associates with alpha and beta subunits.

Isoforms / Transcripts (Protein Coding)


Drugs


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

Sub-cellular localization


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



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project GABRE has gain in 1 cell-lines, loss in 21 cell-lines and no signal in 983 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: HT29, K_562, BT_549

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: NCI-H596, JHH-2, ABC-1

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: K562, SK-N-SH, A549

(see details)

3D Structures


At greater than 50% identity similarity to GABRE there are:
5 structures (9 chains) solved
2 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


GABRE has been screened with 642 compounds (850 bioactivities), 267 compounds have bioactivities that show binding affinity of <= 500nM (324 bioactivities). (see details)