Tclin GABBR2 Gamma-aminobutyric acid type B receptor subunit 2

Protein Summary

Description

Component of a heterodimeric G-protein coupled receptor for GABA, formed by GABBR1 and GABBR2 (PubMed:9872316, PubMed:9872744, PubMed:15617512, PubMed:18165688, PubMed:22660477, PubMed:24305054). Within the heterodimeric GABA receptor, only GABBR1 seems to bind agonists, while GABBR2 mediates coupling to G proteins (PubMed:18165688). 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 (PubMed:10075644, PubMed:10773016, PubMed:24305054). Signaling inhibits adenylate cyclase, stimulates phospholipase A2, activates potassium channels, inactivates voltage-dependent calcium-channels and modulates inositol phospholipid hydrolysis (PubMed:10075644, PubMed:9872744, PubMed:10906333, PubMed:10773016). Plays a critical role in the fine-tuning of inhibitory synaptic transmission (PubMed:9872744, PubMed:22660477). 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 (PubMed:9872316, PubMed:10075644, PubMed:9872744, PubMed:22660477). Not only implicated in synaptic inhibition but also in hippocampal long-term potentiation, slow wave sleep, muscle relaxation and antinociception (Probable). The multi-pass membrane protein encoded by this gene belongs to the G-protein coupled receptor 3 family and GABA-B receptor subfamily. The GABA-B receptors inhibit neuronal activity through G protein-coupled second-messenger systems, which regulate the release of neurotransmitters, and the activity of ion channels and adenylyl cyclase. This receptor subunit forms an active heterodimeric complex with GABA-B receptor subunit 1, neither of which is effective on its own. Allelic variants of this gene have been associated with nicotine dependence.[provided by RefSeq, Jan 2010]

Uniprot Accession IDs

• O75899
• O75974
• O75975
• Q5VXZ2
• Q8WX04
• Q9P1R2
• Q9UNR1
• Q9UNS9
• GABA-B receptor 2

Gene Name

• GABBR2

Ensembl ID

• ENST00000259455
• ENSP00000259455
• ENSG00000136928

Symbol

• GPR51
• GPRC3B
• HG20
• GPR51
• EIEE59
• GPRC3B
• NDPLHS
• GABABR2
• HRIHFB2099

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
trait	0.93
protein domain	0.92
small molecule perturbation	0.71
PubMedID	0.69
phenotype	0.67

Protein Classes

DTO Classes

Protein / G-protein Coupled Receptor / Class C Metabotropic Glutamate/pheromone / Gaba-b Receptor / Gamma-aminobutyric Acid Type B Receptor Subunit 2

IDG Development Level Summary

Tdark

These are targets about which virtually nothing is known. They do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 92.27   (req: < 5)

Gene RIFs: 36   (req: <= 3)

Antibodies: 515   (req: <= 50)

Tbio

These targets do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 92.27   (req: >= 5)

Gene RIFs: 36   (req: > 3)

Antibodies: 515   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 6

Tchem

Target has at least one ChEMBL compound with an activity cutoff of < 30 nM - AND - satisfies the preceding conditions

Active Ligand: 1

Tclin

Target has at least one approved drug - AND - satisfies the preceding conditions

Active Drugs: 3