6wiv: Difference between revisions

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<StructureSection load='6wiv' size='340' side='right'caption='[[6wiv]], [[Resolution|resolution]] 3.30&Aring;' scene=''>
<StructureSection load='6wiv' size='340' side='right'caption='[[6wiv]], [[Resolution|resolution]] 3.30&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
<table><tr><td colspan='2'>[[6wiv]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6WIV OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=6WIV FirstGlance]. <br>
<table><tr><td colspan='2'>Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6WIV OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6WIV FirstGlance]. <br>
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=CLR:CHOLESTEROL'>CLR</scene>, <scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</scene>, <scene name='pdbligand=U3D:[(2R)-3-[(Z)-icos-11-enoyl]oxy-2-[(Z)-octadec-9-enoyl]oxypropyl]+2-(trimethylazaniumyl)ethyl+phosphate'>U3D</scene>, <scene name='pdbligand=U3G:(2R)-3-{[(S)-(2-aminoethoxy)(hydroxy)phosphoryl]oxy}-2-{[(9Z)-octadec-9-enoyl]oxy}propyl+(5Z,8Z,11Z,14Z)-icosa-5,8,11,14-tetraenoate'>U3G</scene></td></tr>
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">Electron Microscopy, [[Resolution|Resolution]] 3.3&#8491;</td></tr>
<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">GABBR1, GPRC3A ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN]), GABBR2, GPR51, GPRC3B ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr>
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=CLR:CHOLESTEROL'>CLR</scene>, <scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</scene>, <scene name='pdbligand=U3D:[(2R)-3-[(Z)-icos-11-enoyl]oxy-2-[(Z)-octadec-9-enoyl]oxypropyl]+2-(trimethylazaniumyl)ethyl+phosphate'>U3D</scene>, <scene name='pdbligand=U3G:(2R)-3-{[(S)-(2-aminoethoxy)(hydroxy)phosphoryl]oxy}-2-{[(9Z)-octadec-9-enoyl]oxy}propyl+(5Z,8Z,11Z,14Z)-icosa-5,8,11,14-tetraenoate'>U3G</scene></td></tr>
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://proteopedia.org/fgij/fg.htm?mol=6wiv FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6wiv OCA], [http://pdbe.org/6wiv PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6wiv RCSB], [http://www.ebi.ac.uk/pdbsum/6wiv PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6wiv ProSAT]</span></td></tr>
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=6wiv FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6wiv OCA], [https://pdbe.org/6wiv PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6wiv RCSB], [https://www.ebi.ac.uk/pdbsum/6wiv PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6wiv ProSAT]</span></td></tr>
</table>
</table>
== Function ==
[[http://www.uniprot.org/uniprot/GABR1_HUMAN GABR1_HUMAN]] 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.<ref>PMID:9844003</ref> <ref>PMID:9872316</ref> <ref>PMID:18165688</ref> <ref>PMID:22660477</ref>  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.<ref>PMID:9844003</ref> <ref>PMID:9872316</ref> <ref>PMID:18165688</ref> <ref>PMID:22660477</ref>  [[http://www.uniprot.org/uniprot/GABR2_HUMAN GABR2_HUMAN]] 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.<ref>PMID:9872316</ref> <ref>PMID:10328880</ref> <ref>PMID:18165688</ref> <ref>PMID:22660477</ref> 
<div style="background-color:#fffaf0;">
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
== Publication Abstract from PubMed ==
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__TOC__
__TOC__
</StructureSection>
</StructureSection>
[[Category: Human]]
[[Category: Large Structures]]
[[Category: Large Structures]]
[[Category: Cao, B]]
[[Category: Cao B]]
[[Category: Chen, S]]
[[Category: Chen S]]
[[Category: Clarke, O B]]
[[Category: Clarke OB]]
[[Category: Eng, E T]]
[[Category: Eng ET]]
[[Category: Fan, Q R]]
[[Category: Fan QR]]
[[Category: Fiehn, O]]
[[Category: Fiehn O]]
[[Category: Frangaj, A]]
[[Category: Frangaj A]]
[[Category: Frank, J]]
[[Category: Frank J]]
[[Category: Fu, Z]]
[[Category: Fu Z]]
[[Category: Geng, Y]]
[[Category: Geng Y]]
[[Category: Grassucci, R]]
[[Category: Grassucci R]]
[[Category: Graziano, J]]
[[Category: Graziano J]]
[[Category: Hendrickson, W A]]
[[Category: Hendrickson WA]]
[[Category: Huang, R K]]
[[Category: Huang RK]]
[[Category: Javitch, J A]]
[[Category: Javitch JA]]
[[Category: Kloss, B]]
[[Category: Kloss B]]
[[Category: Kou, Y]]
[[Category: Kou Y]]
[[Category: Lin, X]]
[[Category: Lin X]]
[[Category: Liu, J]]
[[Category: Liu J]]
[[Category: Liu, Z]]
[[Category: Liu Z]]
[[Category: Mosyak, L]]
[[Category: Mosyak L]]
[[Category: Park, J]]
[[Category: Park J]]
[[Category: Quick, M]]
[[Category: Quick M]]
[[Category: Ray, K M]]
[[Category: Ray KM]]
[[Category: Rice, W J]]
[[Category: Rice WJ]]
[[Category: Shen, T]]
[[Category: Shen T]]
[[Category: Slavkovich, V N]]
[[Category: Slavkovich VN]]
[[Category: Slesinger, P A]]
[[Category: Slesinger PA]]
[[Category: Soni, R K]]
[[Category: Soni RK]]
[[Category: Taura, J]]
[[Category: Taura J]]
[[Category: Williams, J P]]
[[Category: Williams JP]]
[[Category: Yu, H]]
[[Category: Yu H]]
[[Category: Yu, Z]]
[[Category: Yu Z]]
[[Category: Zuo, H]]
[[Category: Zuo H]]
[[Category: Class c gpcr]]
[[Category: Gaba]]
[[Category: Inhibitory neurotransmission]]
[[Category: Membrane protein]]
[[Category: Phospholipid]]

Latest revision as of 09:15, 9 October 2024

Structure of human GABA(B) receptor in an inactive state

6wiv, resolution 3.30Å

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