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

GABRA6 (Q16445) - Overview - Molecular Target Synopsis

Protein


GABRA6, Gamma-aminobutyric acid receptor subunit alpha-6
UniProt Q16445

Also Known as GBRA6_HUMAN, GABRA6

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. Binds UBQLN1 (By similarity). Generally pentameric. There are five types of GABA(A) receptor chains: alpha, beta, gamma, delta, and rho.

Isoforms / Transcripts (Protein Coding)


Drugs


GABRA6 is targeted by Approved Drugs Ethchlorvynol, Clobazam, Eszopiclone. (see details)
Ethchlorvynol
Clobazam
Eszopiclone

Sub-cellular localization


UniProt: GABRA6 is active in the following subcellular-locations: cell junction, cell membrane, postsynaptic cell membrane, synapse.
GO terms: GABRA6 is active in the following subcellular-locations: cell junction, cerebellar Golgi cell to granule cell synapse, chloride channel complex, dendrite membrane, GABA-A receptor complex, 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 GABRA6 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: MCF7, SK_OV_3, UACC_62

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: NCI-H209, LN-18, Hs 746T

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 50% identity similarity to GABRA6 there are:
16 structures (40 chains) solved
13 are solved in complex with at least one small molecule ligand
4 are solved with an approved drug

GABRA6 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


GABRA6 has been screened with 927 compounds (1399 bioactivities), 338 compounds have bioactivities that show binding affinity of <= 500nM (490 bioactivities). (see details)