Tclin GABBR1 Gamma-aminobutyric acid type B receptor subunit 1

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:10906333, PubMed:10773016, PubMed:10075644, PubMed:9872744, PubMed:24305054). Signaling inhibits adenylate cyclase, stimulates phospholipase A2, activates potassium channels, inactivates voltage-dependent calcium-channels and modulates inositol phospholipid hydrolysis (PubMed:10075644). Calcium is required for high affinity binding to GABA (By similarity). Plays a critical role in the fine-tuning of inhibitory synaptic transmission (PubMed:9844003). 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:9844003, 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). Activated by (-)-baclofen, cgp27492 and blocked by phaclofen (PubMed:9844003, PubMed:9872316, PubMed:24305054). 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. This gene encodes a receptor for gamma-aminobutyric acid (GABA), which is the main inhibitory neurotransmitter in the mammalian central nervous system. This receptor functions as a heterodimer with GABA(B) receptor 2. Defects in this gene may underlie brain disorders such as schizophrenia and epilepsy. Alternative splicing generates multiple transcript variants, but the full-length nature of some of these variants has not been determined. [provided by RefSeq, Jan 2016]

Uniprot Accession IDs

• Q9UBS5
• B0UXY7
• O95375
• O95468
• O95975
• O96022
• Q5STL4
• Q5SUJ8
• Q5SUL3
• Q71SG6
• Q86W60
• Q9UQQ0
• GABA-B receptor 1

Gene Name

• GABBR1

Ensembl ID

• ENST00000355973
• ENSP00000348248
• ENSG00000204681
• ENST00000376977
• ENSP00000366176
• ENST00000377012
• ENSP00000366211
• ENST00000377016
• ENSP00000366215
• ENST00000377034
• ENSP00000366233
• ENST00000383537
• ENSP00000373029
• ENSG00000206466
• ENST00000383541
• ENSP00000373033
• ENST00000383542
• ENSP00000373034
• ENST00000383543
• ENSP00000373035
• ENST00000383636
• ENSP00000373132
• ENSG00000206511
• ENST00000383637
• ENSP00000373133
• ENST00000383638
• ENSP00000373134
• ENST00000383639
• ENSP00000373135
• ENST00000414980
• ENSP00000406499
• ENSG00000232632
• ENST00000417759
• ENSP00000391572
• ENSG00000237112
• ENST00000419674
• ENSP00000399861
• ENSG00000232569
• ENST00000423604
• ENSP00000388035
• ENST00000425097
• ENSP00000411286
• ENST00000434660
• ENSP00000412167
• ENST00000438094
• ENSP00000406285
• ENST00000439457
• ENSP00000406066
• ENST00000443440
• ENSP00000399318
• ENST00000446436
• ENSP00000394528
• ENST00000448754
• ENSP00000405709
• ENSG00000237051
• ENST00000449163
• ENSP00000411263
• ENST00000452300
• ENSP00000408938
• ENST00000458612
• ENSP00000416903
• ENST00000494877
• ENSP00000419061
• ENST00000546913
• ENSP00000448999
• ENST00000547410
• ENSP00000448531
• ENST00000548767
• ENSP00000446983
• ENST00000551140
• ENSP00000448654
• ENST00000551423
• ENSP00000449342
• ENST00000552399
• ENSP00000449449

Symbol

• GPRC3A
• GB1
• GPRC3A
• GABABR1
• GABBR1-3

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
PubMedID	0.92
hub protein	0.85
protein domain	0.85
phenotype	0.69
transcription factor perturbation	0.68

Protein Classes

PANTHER Classes

Protein / Receptor / G-protein Coupled Receptor / Gamma-aminobutyric Acid Type B Receptor Subunit 1

DTO Classes

Protein / G-protein Coupled Receptor / Class C Metabotropic Glutamate/pheromone / Gaba-b Receptor / Gamma-aminobutyric Acid Type B Receptor Subunit 1

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: 1287.58   (req: < 5)

Gene RIFs: 81   (req: <= 3)

Antibodies: 510   (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: 1287.58   (req: >= 5)

Gene RIFs: 81   (req: > 3)

Antibodies: 510   (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 Ligands: 8

Tclin

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

Active Drugs: 3