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

GABRA1 (P14867) - Overview - Molecular Target Synopsis

Protein


GABRA1, Gamma-aminobutyric acid receptor subunit alpha-1
UniProt P14867

Also Known as GBRA1_HUMAN, GABRA1

Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine. Functions as receptor for diazepines and various anesthetics, such as pentobarbital; these are bound at a separate allosteric effector binding site. Functions as ligand-gated chloride channel. Heteropentamer, formed by a combination of alpha, beta, gamma, delta and rho chains. Interacts with UBQLN1. Interacts with TRAK1. Interacts with KIF21B. Identified in a complex of 720 kDa composed of LHFPL4, NLGN2, GABRA1, GABRB2, GABRG2 and GABRB3 (By similarity). Interacts with LHFPL4 (PubMed:28978485, PubMed:29742426). Interacts with NLGN2.

6I53
CRYO-EM STRUCTURE OF THE HUMAN SYNAPTIC ALPHA1-BETA3-GAMMA2 GABAA RECEPTOR IN COMPLEX WITH MEGABODY38 IN A LIPID NANODISC
RCSB/PDB
Inspect Structure
See all 3D Structures for GABRA1

Isoforms / Transcripts (Protein Coding)


Drugs


GABRA1 is targeted by Approved Drugs Glutethimide, Thiamylal, Enflurane, Propofol, Clonazepam, Propiomazine, Meprobamate, Flumazenil, Triclofos, Midazolam, Talbutal, Butabarbital, Acamprosate, Ethchlorvynol, Butalbital, Clobazam, Eszopiclone, Secobarbital, Primidone, Halothane, Isoflurane, Oxazepam, Prazepam, Halazepam, Triazolam, Topiramate, Alprazolam, Methyprylon, Chlordiazepoxide, Flurazepam, Diazepam, Estazolam, Metharbital, Sevoflurane, Quazepam, Temazepam, Lorazepam, Pentobarbital, Desflurane, Zaleplon, Thiopental, Zolpidem, Methoxyflurane. (see details)
Glutethimide
Thiamylal
Enflurane
Propofol
Clonazepam
Propiomazine
Meprobamate
Flumazenil
Triclofos
Midazolam
Talbutal
Butabarbital
Acamprosate
Ethchlorvynol
Butalbital
Clobazam
Eszopiclone
Secobarbital
Primidone
Halothane
Isoflurane
Oxazepam
Prazepam
Halazepam
Triazolam
Topiramate
Alprazolam
Methyprylon
Chlordiazepoxide
Flurazepam
Diazepam
Estazolam
Metharbital
Sevoflurane
Quazepam
Temazepam
Lorazepam
Pentobarbital
Desflurane
Zaleplon
Thiopental
Zolpidem
Methoxyflurane

Sub-cellular localization


UniProt: GABRA1 is active in the following subcellular-locations: cell junction, cell membrane, cytoplasmic vesicle membrane, postsynaptic cell membrane, synapse.
GO terms: GABRA1 is active in the following subcellular-locations: cell junction, chloride channel complex, cytoplasmic vesicle membrane, dendrite membrane, GABA receptor complex, GABA-A receptor complex, GABA-ergic synapse, integral component of plasma membrane, integral component of postsynaptic specialization membrane, neuron projection, plasma membrane, postsynapse, synapse.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project GABRA1 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: TK_10, KM12, HS578T

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: DU4475, Hs 746T, 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 GABRA1 there are:
12 structures (40 chains) solved
11 are solved in complex with at least one small molecule ligand
2 are solved with an approved drug

GABRA1 is solved in complex with the approved drug(s):

08H/ALPRAZOLAM (6HUO_D),
DZP/DIAZEPAM (6HUP_D).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


GABRA1 has been screened with 1981 compounds (3513 bioactivities), 910 compounds have bioactivities that show binding affinity of <= 500nM (1277 bioactivities). (see details)