Names & Taxonomy
- Uniprot ID:
- Q9UBS5
- Entry Name:
- GABR1_HUMAN
- Status:
- reviewed
- Protein Names:
- Gamma-aminobutyric acid type B receptor subunit 1 (GABA-B receptor 1) (GABA-B-R1) (GABA-BR1) (GABABR1) (Gb1)
- Gene Names:
- GABBR1 GPRC3A
- Gene Names Primary:
- GABBR1
- Organism:
- Homo sapiens (Human)
Structure
- Length:
- 961
- Sequence:
- MLLLLLLAPLFLRPPGAGGAQTPNATSEGCQIIHPPWEGGIRYRGLTRDQVKAINFLPVDYEIEYVCRGEREVVGPKVRKCLANGSWTDMDTPSRCVRICSKSYLTLENGKVFLTGGDLPALDGARVDFRCDPDFHLVGSSRSICSQGQWSTPKPHCQVNRTPHSERRAVYIGALFPMSGGWPGGQACQPAVEMALEDVNSRRDILPDYELKLIHHDSKCDPGQATKYLYELLYNDPIKIILMPGCSSVSTLVAEAARMWNLIVLSYGSSSPALSNRQRFPTFFRTHPSATLHNPTRVKLFEKWGWKKIATIQQTTEVFTSTLDDLEERVKEAGIEITFRQSFFSDPAVPVKNLKRQDARIIVGLFYETEARKVFCEVYKERLFGKKYVWFLIGWYADNWFKIYDPSINCTVDEMTEAVEGHITTEIVMLNPANTRSISNMTSQEFVEKLTKRLKRHPEETGGFQEAPLAYDAIWALALALNKTSGGGGRSGVRLEDFNYNNQTITDQIYRAMNSSSFEGVSGHVVFDASGSRMAWTLIEQLQGGSYKKIGYYDSTKDDLSWSKTDKWIGGSPPADQTLVIKTFRFLSQKLFISVSVLSSLGIVLAVVCLSFNIYNSHVRYIQNSQPNLNNLTAVGCSLALAAVFPLGLDGYHIGRNQFPFVCQARLWLLGLGFSLGYGSMFTKIWWVHTVFTKKEEKKEWRKTLEPWKLYATVGLLVGMDVLTLAIWQIVDPLHRTIETFAKEEPKEDIDVSILPQLEHCSSRKMNTWLGIFYGYKGLLLLLGIFLAYETKSVSTEKINDHRAVGMAIYNVAVLCLITAPVTMILSSQQDAAFAFASLAIVFSSYITLVVLFVPKMRRLITRGEWQSEAQDTMKTGSSTNNNEEEKSRLLEKENRELEKIIAEKEERVSELRHQLQSRQQLRSRRHPPTPPEPSGGLPRGPPEPPDRLSCDGSRVHLLYK
- Proteomes:
- UP000005640
Subcellular location
- Subcellular Location:
- Cell membrane; Multi-pass membrane protein. Cell junction, synapse, postsynaptic cell membrane; Multi-pass membrane protein. Cell projection, dendrite
Function
- Function:
- Component of a heterodimeric G-protein coupled receptor for GABA, formed by GABBR1 and GABBR2. Within the heterodimeric GABA receptor, only GABBR1 seems to bind agonists, while GABBR2 mediates coupling to G proteins. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling inhibits adenylate cyclase, stimulates phospholipase A2, activates potassium channels, inactivates voltage-dependent calcium-channels and modulates inositol phospholipid hydrolysis. Calcium is required for high affinity binding to GABA. Plays a critical role in the fine-tuning of inhibitory synaptic transmission. Pre-synaptic GABA receptor inhibits neurotransmitter release by down-regulating high-voltage activated calcium channels, whereas postsynaptic GABA receptor decreases neuronal excitability by activating a prominent inwardly rectifying potassium (Kir) conductance that underlies the late inhibitory postsynaptic potentials. Not only implicated in synaptic inhibition but also in hippocampal long-term potentiation, slow wave sleep, muscle relaxation and antinociception. Activated by (-)-baclofen, cgp27492 and blocked by phaclofen.; Isoform 1E may regulate the formation of functional GABBR1/GABBR2 heterodimers by competing for GABBR2 binding. This could explain the observation that certain small molecule ligands exhibit differential affinity for central versus peripheral sites.
- Cross Reference Drug Bank:
- DB00181 DB00837 DB01080
- Gene Ontology Go:
- axolemma
cell junction
dendritic shaft
dendritic spine
endoplasmic reticulum membrane
extracellular space
G-protein coupled receptor heterodimeric complex
integral component of plasma membrane
membrane raft
mitochondrial membrane
neuronal cell body
plasma membrane
postsynaptic membrane
presynaptic membrane
synaptic vesicle
G-protein coupled GABA receptor activity
adenylate cyclase-inhibiting G-protein coupled receptor signaling pathway
gamma-aminobutyric acid signaling pathway
negative regulation of adenylate cyclase activity
negative regulation of cell proliferation
negative regulation of dopamine secretion
negative regulation of epinephrine secretion
negative regulation of gamma-aminobutyric acid secretion
negative regulation of synaptic transmission
osteoblast differentiation
positive regulation of glutamate secretion
positive regulation of growth hormone secretion
response to ethanol
response to nicotine
synaptic transmission - Gene Ontology Biological Process:
- adenylate cyclase-inhibiting G-protein coupled receptor signaling pathway
gamma-aminobutyric acid signaling pathway
negative regulation of adenylate cyclase activity
negative regulation of cell proliferation
negative regulation of dopamine secretion
negative regulation of epinephrine secretion
negative regulation of gamma-aminobutyric acid secretion
negative regulation of synaptic transmission
osteoblast differentiation
positive regulation of glutamate secretion
positive regulation of growth hormone secretion
response to ethanol
response to nicotine
synaptic transmission - Gene Ontology Molecular Function:
- G-protein coupled GABA receptor activity
- Gene Ontology Cellular Component:
- axolemma
cell junction
dendritic shaft
dendritic spine
endoplasmic reticulum membrane
extracellular space
G-protein coupled receptor heterodimeric complex
integral component of plasma membrane
membrane raft
mitochondrial membrane
neuronal cell body
plasma membrane
postsynaptic membrane
presynaptic membrane
synaptic vesicle - Keywords:
- 3D-structure
Alternative splicing
Cell junction
Cell membrane
Cell projection
Coiled coil
Complete proteome
Direct protein sequencing
Disulfide bond
G-protein coupled receptor
Glycoprotein
Membrane
Phosphoprotein
Polymorphism
Postsynaptic cell membrane
Receptor
Reference proteome
Repeat
Secreted
Signal
Sushi
Synapse
Transducer
Transmembrane
Transmembrane helix - Interacts With:
- O75899; P61244; P16333; P46459