Gamma-aminobutyric acid receptor subunit epsilon
Also known as: GABRE
Function
Epsilon subunit of the heteropentameric ligand-gated chloride channel gated by gamma-aminobutyric acid (GABA), a major inhibitory neurotransmitter in the brain. GABA-gated chloride channels, also named GABA(A) receptors (GABAAR), consist of five subunits arranged around a central pore and contain GABA active binding site(s) located at the alpha and beta subunit interfaces (By similarity). When activated by GABA, GABAARs selectively allow the flow of chloride anions across the cell membrane down their electrochemical gradient (By similarity). GABAARs containing epsilon subunits also permit spontaneous chloride channel activity while preserving the structural information required for GABA-gated openings. GABARs containing epsilon subunit may regulate cardiac function (Probable).
Classification
- Family (Pfam)
- PF02931 Neur_chan_LBD, PF02932 Neur_chan_memb
- InterPro
- GABAA/Glycine_rcpt, GABAAe_rcpt, Neur_chan_lig-bd, Neur_chan_lig-bd_sf, Neur_channel, Neuro-gated_channel_TM_sf, Neuro_actylchol_rec, Neurotrans-gated_channel_TM, Neurotransmitter_ion_chnl_CS
- Functional cluster
- Cytochrome P450 & Heme Enzymes
Gene Ontology · 12
- GO:0034707 chloride channel complex
- GO:0032590 dendrite membrane
- GO:1902711 GABA-A receptor complex
- GO:0098794 postsynapse
- GO:0045211 postsynaptic membrane
- GO:0004890 GABA-A receptor activity
- GO:0022851 GABA-gated chloride ion channel activity
- GO:1902476 chloride transmembrane transport
- GO:0007214 gamma-aminobutyric acid signaling pathway
- GO:1904862 inhibitory synapse assembly
- GO:2001226 negative regulation of chloride transport
- GO:0051932 synaptic transmission, GABAergic
Drugs targeting this protein · 66
- GLUTETHIMIDE positive modulator
- DIAZEPAM positive allosteric modulator
- MIDAZOLAM HYDROCHLORIDE positive allosteric modulator
- QUAZEPAM positive allosteric modulator
- SEVOFLURANE positive allosteric modulator
- CHLORDIAZEPOXIDE HYDROCHLORIDE positive allosteric modulator
- DESFLURANE positive allosteric modulator
- TRICLOFOS SODIUM positive modulator
- METHYPRYLON positive allosteric modulator
- TALBUTAL positive allosteric modulator
- SECOBARBITAL SODIUM positive allosteric modulator
- BUTABARBITAL SODIUM positive allosteric modulator
- THIAMYLAL SODIUM positive allosteric modulator
- ISOFLURANE positive allosteric modulator
- ENFLURANE positive modulator
- FLUNITRAZEPAM positive allosteric modulator
- METHOXYFLURANE positive modulator
- ESZOPICLONE positive allosteric modulator
- GANAXOLONE positive allosteric modulator
- CLOTIAZEPAM positive allosteric modulator
- ACAMPROSATE CALCIUM positive modulator
- BREXANOLONE positive allosteric modulator
- CLORAZEPATE DIPOTASSIUM positive allosteric modulator
- ADIPIPLON partial agonist
- PAGOCLONE positive allosteric modulator
- TETRAZEPAM positive allosteric modulator
- ETIFOXINE antagonist
- METHAQUALONE HYDROCHLORIDE positive allosteric modulator
- RESEQUINIL inverse agonist
- TOPIRAMATE positive modulator
- METHAQUALONE positive allosteric modulator
- ESTAZOLAM positive allosteric modulator
- METHOHEXITAL SODIUM positive allosteric modulator
- CLOMETHIAZOLE positive allosteric modulator
- DARIGABAT agonist
- FLURAZEPAM HYDROCHLORIDE positive allosteric modulator
- CENOBAMATE positive allosteric modulator
- FLUMAZENIL allosteric antagonist
- CIPEPOFOL agonist
- ZURANOLONE positive allosteric modulator
- ABP-700 agonist
- PADSEVONIL partial agonist
- LOREDIPLON positive allosteric modulator
- PENTOBARBITAL positive allosteric modulator
- METHARBITAL positive allosteric modulator
- CHLORDIAZEPOXIDE positive allosteric modulator
- CLONAZEPAM positive allosteric modulator
- BUTALBITAL positive allosteric modulator
- REMIMAZOLAM BESYLATE positive allosteric modulator
- PROPOFOL positive allosteric modulator
- OXAZEPAM positive allosteric modulator
- LORAZEPAM positive allosteric modulator
- ETHCHLORVYNOL positive modulator
- TRIAZOLAM positive allosteric modulator
- MIDAZOLAM positive allosteric modulator
- ALPRAZOLAM positive allosteric modulator
- ETOMIDATE positive modulator
- CLOBAZAM positive allosteric modulator
- THIOPENTAL SODIUM positive allosteric modulator
- PRIMIDONE positive allosteric modulator
- HALOTHANE positive allosteric modulator
- TEMAZEPAM positive allosteric modulator
- PRAZEPAM positive allosteric modulator
- HALAZEPAM positive allosteric modulator
- PENTOBARBITAL SODIUM positive allosteric modulator
- MEPROBAMATE agonist
Related proteins · sequence + function similarity
- Gamma-aminobutyric acid receptor subunit epsilon 0.92
- Gamma-aminobutyric acid receptor subunit gamma-4 0.83
- Acetylcholine receptor subunit delta 0.76
- Acetylcholine receptor subunit delta 0.76
- Neuronal acetylcholine receptor subunit beta-2 0.76
- Neuronal acetylcholine receptor subunit beta-2 0.75
- Neuronal acetylcholine receptor subunit beta-2 0.75
- Acetylcholine receptor subunit beta 0.75
- Neuronal acetylcholine receptor subunit alpha-2 0.75
- Acetylcholine receptor subunit delta 0.75
- Neuronal acetylcholine receptor subunit beta-4 0.75
- Neuronal acetylcholine receptor subunit alpha-2 0.75
Co-cited proteins · studied together in the literature
- Gamma-aminobutyric acid receptor subunit beta-3 1 shared papers
- Gamma-aminobutyric acid receptor subunit theta 1 shared papers
- Gamma-aminobutyric acid receptor subunit alpha-1 1 shared papers
- Gamma-aminobutyric acid receptor subunit alpha-3 1 shared papers
- Gamma-aminobutyric acid receptor subunit beta-1 1 shared papers
- Gamma-aminobutyric acid receptor subunit gamma-2 1 shared papers
Literature · 7 cited papers
- Impact of epsilon and theta subunits on pharmacological properties of alpha3beta1 GABAA receptors expressed in Xenopus oocytes. BMC Pharmacol. · 2006
- The DNA sequence of the human X chromosome. Nature · 2005
- The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC). Genome Res. · 2004
- Spontaneous and gamma-aminobutyric acid (GABA)-activated GABA(A) receptor channels formed by epsilon subunit-containing isoforms. Mol. Pharmacol. · 1999
- A gene in human chromosome band Xq28 (GABRE) defines a putative new subunit class of the GABAA neurotransmitter receptor. Genomics · 1997
- An mRNA encoding a putative GABA-gated chloride channel is expressed in the human cardiac conduction system. J. Neurochem. · 1997
- Insensitivity to anaesthetic agents conferred by a class of GABA(A) receptor subunit. Nature · 1997