Gamma-aminobutyric acid receptor subunit pi
Also known as: GABRP
Function
Pi subunit of the heteropentameric ligand-gated chloride channel gated by gamma-aminobutyric acid (GABA). 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. Pi-containing GABAARs are mostly located in peripheral tissues. In the uterus, pi subunits modulate uterus contraction by altering the sensitivity of GABAARs to pregnanolone. In the lungs, pi-containing GABAARs contribute to pulmonary fluid transport via luminal secretion of chloride (By similarity).
Classification
- Family (Pfam)
- PF02931 Neur_chan_LBD, PF02932 Neur_chan_memb
- InterPro
- GABAA/Glycine_rcpt, GABAAp_rcpt, GABAAR_pi_TM, 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
- Immunoglobulin-Domain Cell Adhesion Proteins
Experimental structures · PDB · 2
A predicted model is available from AlphaFold.
Gene Ontology · 9
- GO:0016324 apical plasma membrane
- GO:0034707 chloride channel complex
- GO:1902711 GABA-A receptor complex
- GO:0005886 plasma membrane
- GO:0045202 synapse
- GO:0004890 GABA-A receptor activity
- GO:0022851 GABA-gated chloride ion channel activity
- GO:1902476 chloride transmembrane 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 pi 0.99
- Gamma-aminobutyric acid receptor subunit pi 0.99
- Gamma-aminobutyric acid receptor subunit pi 0.99
- Gamma-aminobutyric acid receptor subunit delta 0.88
- Gamma-aminobutyric acid receptor subunit delta 0.88
- Gamma-aminobutyric acid receptor subunit delta 0.88
- Acetylcholine-gated chloride channel subunit acc-2 0.87
- Glutamate-gated chloride channel alpha 0.87
- Glycine receptor subunit alpha-3 0.86
- Acetylcholine-gated chloride channel subunit acc-1 0.86
- Glycine receptor subunit alpha-3 0.86
- Glycine receptor subunit alpha-1 0.86
Co-cited proteins · studied together in the literature
- Gamma-aminobutyric acid receptor subunit pi 1 shared papers
- Gamma-aminobutyric acid receptor subunit gamma-3 1 shared papers
- Gamma-aminobutyric acid receptor subunit alpha-5 1 shared papers
- Gamma-aminobutyric acid receptor subunit beta-3 1 shared papers
Literature · 5 cited papers
- The consensus coding sequences of human breast and colorectal cancers. Science · 2006
- The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC). Genome Res. · 2004
- Complete sequencing and characterization of 21,243 full-length human cDNAs. Nat. Genet. · 2004
- Incorporation of the pi subunit into functional gamma-aminobutyric Acid(A) receptors. Mol. Pharmacol. · 1999
- A novel class of GABAA receptor subunit in tissues of the reproductive system. J. Biol. Chem. · 1997