GABBR1 - Gamma-aminobutyric acid type B receptor subunit 1 - human protein (Function)
 
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GABBR1 »  Gamma-aminobutyric acid type B receptor subunit 1  (Gb1)
 
Gene name:  GABBR1
Entry whose protein(s) existence is based on evidence at protein level
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GENE REF ISO

Function

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Overview 
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.  
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  • CuratedUniProtKB
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.  
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  • CuratedUniProtKB
GO molecular function 
Contributes to G-protein coupled GABA receptor activitydefinition[GO:0004965]  
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  • IDAUniProtKB
Protein bindingdefinition[GO:0005515]  
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  • IPIIntAct
GO biological process 
Adenylate cyclase-inhibiting G-protein coupled receptor signaling pathwaydefinition[GO:0007193]  
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  • IDAUniProtKB
Gamma-aminobutyric acid signaling pathwaydefinition[GO:0007214]  
1
  • IDAUniProtKB
Negative regulation of adenylate cyclase activitydefinition[GO:0007194]  
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  • TASPINC
Pathways 
According to KEGG, this protein belongs to the following pathways:
GABAergic synapse  hsa04727+2550  
Neuroactive ligand-receptor interaction  hsa04080+2550  
According to Reactome, this protein belongs to the following pathways:
Neuronal System  REACT_13685  
Signal Transduction  REACT_111102  
 

Keywords

Molecular function 
G-protein coupled receptor  definition   [KW-0297]
Receptor  definition   [KW-0675]
Transducer  definition   [KW-0807]
Technical term 
Reference proteome  definition   [KW-1185]
 

Further external links

Other
GeneWiki: GABBR1
GenomeRNAi: 2550
PRO: PR:Q9UBS5
Chemistry
GuidetoPHARMACOLOGY: 240