General Information of This Target
Target ID
BTDT00235
Target Name
Gamma-aminobutyric acid type B receptor subunit 1 (Gabbr1);Gamma-aminobutyric acid type B receptor subunit 2 (Gabbr2)
Target Bioclass
Transporter and channel
Uniprot ID
Q9Z0U4 ; O88871
3D Structure
Download
2D Sequence
3D Structure
Source
Predict by Alphafold2
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Alphafold Parameters: msa_mode: mmseqs2_uniref_env model_type: auto num_recycles: auto
Gene Name
Gabbr1;Gabbr2
Gene ID
81657 ; 83633
Synonym 2
G-protein coupled receptor 51
Sequence 1
MLLLLLVPLFLRPLGAGGAQTPNATSEGCQIIHPPWEGGIRYRGLTRDQVKAINFLPVDY
EIEYVCRGEREVVGPKVRKCLANGSWTDMDTPSRCVRICSKSYLTLENGKVFLTGGDLPA
LDGARVEFRCDPDFHLVGSSRSVCSQGQWSTPKPHCQVNRTPHSERRAVYIGALFPMSGG
WPGGQACQPAVEMALEDVNSRRDILPDYELKLIHHDSKCDPGQATKYLYELLYNDPIKII
LMPGCSSVSTLVAEAARMWNLIVLSYGSSSPALSNRQRFPTFFRTHPSATLHNPTRVKLF
EKWGWKKIATIQQTTEVFTSTLDDLEERVKEAGIEITFRQSFFSDPAVPVKNLKRQDARI
IVGLFYETEARKVFCEVYKERLFGKKYVWFLIGWYADNWFKTYDPSINCTVEEMTEAVEG
HITTEIVMLNPANTRSISNMTSQEFVEKLTKRLKRHPEETGGFQEAPLAYDAIWALALAL
NKTSGGGGRSGVRLEDFNYNNQTITDQIYRAMNSSSFEGVSGHVVFDASGSRMAWTLIEQ
LQGGSYKKIGYYDSTKDDLSWSKTDKWIGGSPPADQTLVIKTFRFLSQKLFISVSVLSSL
GIVLAVVCLSFNIYNSHVRYIQNSQPNLNNLTAVGCSLALAAVFPLGLDGYHIGRSQFPF
VCQARLWLLGLGFSLGYGSMFTKIWWVHTVFTKKEEKKEWRKTLEPWKLYATVGLLVGMD
VLTLAIWQIVDPLHRTIETFAKEEPKEDIDVSILPQLEHCSSKKMNTWLGELWSFAVSSD
VQRRATVGGDSPICVWPAPESIFYGYKGLLLLLGIFLAYETKSVSTEKINDHRAVGMAIY
NVAVLCLITAPVTMILSSQQDAAFAFASLAIVFSSYITLVVLFVPKMRRLITRGEWQSET
QDTMKTGSSTNNNEEEKSRLLEKENRELEKIIAEKEERVSELRHQLQSRQQLRSRRHPPT
PPDPSGGLPRGPSEPPDRLSCDGSRVHLLYK

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Sequence 2
MASPPSSGQPRPPPPPPPPARLLLPLLLSLLLWLAPGAWGWTRGAPRPPPSSPPLSIMGL
MPLTKEVAKGSIGRGVLPAVELAIEQIRNESLLRPYFLDLRLYDTECDNAKGLKAFYDAI
KYGPNHLMVFGGVCPSVTSIIAESLQGWNLVQLSFAATTPVLADKKKYPYFFRTVPSDNA
VNPAILKLLKHFRWRRVGTLTQDVQRFSEVRNDLTGVLYGEDIEISDTESFSNDPCTSVK
KLKGNDVRIILGQFDQNMAAKVFCCAFEESMFGSKYQWIIPGWYEPAWWEQVHVEANSSR
CLRRSLLAAMEGYIGVDFEPLSSKQIKTISGKTPQQFEREYNSKRSGVGPSKFHGYAYDG
IWVIAKTLQRAMETLHASSRHQRIQDFNYTDHTLGKIILNAMNETNFFGVTGQVVFRNGE
RMGTIKFTQFQDSREVKVGEYNAVADTLEIINDTIRFQGSEPPKDKTIILEQLRKISLPL
YSILSALTILGMIMASAFLFFNIKNRNQKLIKMSSPYMNNLIILGGMLSYASIFLFGLDG
SFVSEKTFETLCTVRTWILTVGYTTAFGAMFAKTWRVHAIFKNVKMKKKIIKDQKLLVIV
GGMLLIDLCILICWQAVDPLRRTVERYSMEPDPAGRDISIRPLLEHCENTHMTIWLGIVY
AYKGLLMLFGCFLAWETRNVSIPALNDSKYIGMSVYNVGIMCIIGAAVSFLTRDQPNVQF
CIVALVIIFCSTITLCLVFVPKLITLRTNPDAATQNRRFQFTQNQKKEDSKTSTSVTSVN
QASTSRLEGLQSENHRLRMKITELDKDLEEVTMQLQDTPEKTTYIKQNHYQELNDILSLG
NFTESTDGGKAILKNHLDQNPQLQWNTTEPSRTCKDPIEDINSPEHIQRRLSLQLPILHH
AYLPSIGGVDASCVSPCVSPTASPRHRHVPPSFRVMVSGL

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Family1
the G-protein coupled receptor 3 family.
Family2
the G-protein coupled receptor 3 family
Function 1
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 .

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Function 2
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. 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 .

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Taxonomy ID
10116
TCDB ID
. ; .
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Kingdom: Metazoa
Phylum: Chordata
Class: Mammalia
Order: Rodentia
Family: Muridae
Genus: Rattus
Species: Rattus norvegicus
Toxin Information Related to This Target
                           Toxin Name Activity Data Type Activity Data Reference
 Toxin Info    Alpha-conotoxin-like Kn1.2 Inhibition rate
13 %
[1], [2]
References
Ref 1 Evolution of Conus peptide genes: duplication and positive selection in the A-superfamily. J Mol Evol. 2010 Feb;70(2):190-202. doi: 10.1007/s00239-010-9321-7. Epub 2010 Feb 9.
Ref 2 Structure-Activity Studies of Cysteine-Rich -Conotoxins that Inhibit High-Voltage-Activated Calcium Channels via GABA(B) Receptor Activation Reveal a Minimal Functional Motif. Angew Chem Int Ed Engl. 2016 Apr 4;55(15):4692-6. doi: 10.1002/anie.201600297. Epub 2016 Mar 7.
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