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==Crystal structure of an apo chimeric human alpha1GABAA receptor==
==Crystal structure of an apo chimeric human alpha1GABAA receptor==
<StructureSection load='6d1s' size='340' side='right' caption='[[6d1s]], [[Resolution|resolution]] 3.20&Aring;' scene=''>
<StructureSection load='6d1s' size='340' side='right'caption='[[6d1s]], [[Resolution|resolution]] 3.20&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
<table><tr><td colspan='2'>[[6d1s]] is a 10 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=6D1S OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6D1S FirstGlance]. <br>
<table><tr><td colspan='2'>[[6d1s]] is a 10 chain structure with sequence from [https://en.wikipedia.org/wiki/Dickeya_dadantii_3937 Dickeya dadantii 3937] and [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6D1S OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6D1S FirstGlance]. <br>
</td></tr><tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">GABRA1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr>
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 3.2&#8491;</td></tr>
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6d1s FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6d1s OCA], [http://pdbe.org/6d1s PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6d1s RCSB], [http://www.ebi.ac.uk/pdbsum/6d1s PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6d1s 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=6d1s FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6d1s OCA], [https://pdbe.org/6d1s PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6d1s RCSB], [https://www.ebi.ac.uk/pdbsum/6d1s PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6d1s ProSAT]</span></td></tr>
</table>
</table>
<div style="background-color:#fffaf0;">
== Disease ==
== Publication Abstract from PubMed ==
[https://www.uniprot.org/uniprot/GBRA1_HUMAN GBRA1_HUMAN] Juvenile myoclonic epilepsy;Childhood absence epilepsy;Dravet syndrome. Disease susceptibility is associated with variations affecting the gene represented in this entry. Disease susceptibility is associated with variations affecting the gene represented in this entry. Disease susceptibility is associated with variations affecting the gene represented in this entry. The disease is caused by mutations affecting the gene represented in this entry.
A unique aspect of arrestin-3 is its ability to support both receptor-dependent and receptor-independent signaling. Here, we show that inositol hexakisphosphate (IP6) is a non-receptor activator of arrestin-3 and report the structure of IP6-activated arrestin-3 at 2.4-A resolution. IP6-activated arrestin-3 exhibits an inter-domain twist and a displaced C-tail, hallmarks of active arrestin. IP6 binds to the arrestin phosphate sensor, and is stabilized by trimerization. Analysis of the trimerization surface, which is also the receptor-binding surface, suggests a feature called the finger loop as a key region of the activation sensor. We show that finger loop helicity and flexibility may underlie coupling to hundreds of diverse receptors and also promote arrestin-3 activation by IP6. Importantly, we show that effector-binding sites on arrestins have distinct conformations in the basal and activated states, acting as switch regions. These switch regions may work with the inter-domain twist to initiate and direct arrestin-mediated signaling.
== Function ==
[https://www.uniprot.org/uniprot/E0SJQ4_DICD3 E0SJQ4_DICD3] [https://www.uniprot.org/uniprot/GBRA1_HUMAN GBRA1_HUMAN] Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine. Functions as receptor for diazepines and various anesthetics, such as pentobarbital; these are bound at a separate allosteric effector binding site. Functions as ligand-gated chloride channel (By similarity).


Structural basis of arrestin-3 activation and signaling.,Chen Q, Perry NA, Vishnivetskiy SA, Berndt S, Gilbert NC, Zhuo Y, Singh PK, Tholen J, Ohi MD, Gurevich EV, Brautigam CA, Klug CS, Gurevich VV, Iverson TM Nat Commun. 2017 Nov 10;8(1):1427. doi: 10.1038/s41467-017-01218-8. PMID:29127291<ref>PMID:29127291</ref>
==See Also==
 
*[[GABA receptor 3D structures|GABA receptor 3D structures]]
From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
</div>
<div class="pdbe-citations 6d1s" style="background-color:#fffaf0;"></div>
== References ==
<references/>
__TOC__
__TOC__
</StructureSection>
</StructureSection>
[[Category: Human]]
[[Category: Dickeya dadantii 3937]]
[[Category: Arjunan, P]]
[[Category: Homo sapiens]]
[[Category: Chen, Q]]
[[Category: Large Structures]]
[[Category: Cohen, A E]]
[[Category: Arjunan P]]
[[Category: Tang, P]]
[[Category: Chen Q]]
[[Category: Xu, Y]]
[[Category: Cohen AE]]
[[Category: Alphaxalone]]
[[Category: Tang P]]
[[Category: Anesthetic]]
[[Category: Xu Y]]
[[Category: Gabaa receptor]]
[[Category: Neurosteroid]]
[[Category: Protein transport]]

Latest revision as of 17:32, 13 March 2024

Crystal structure of an apo chimeric human alpha1GABAA receptorCrystal structure of an apo chimeric human alpha1GABAA receptor

Structural highlights

6d1s is a 10 chain structure with sequence from Dickeya dadantii 3937 and Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Method:X-ray diffraction, Resolution 3.2Å
Resources:FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Disease

GBRA1_HUMAN Juvenile myoclonic epilepsy;Childhood absence epilepsy;Dravet syndrome. Disease susceptibility is associated with variations affecting the gene represented in this entry. Disease susceptibility is associated with variations affecting the gene represented in this entry. Disease susceptibility is associated with variations affecting the gene represented in this entry. The disease is caused by mutations affecting the gene represented in this entry.

Function

E0SJQ4_DICD3 GBRA1_HUMAN Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine. Functions as receptor for diazepines and various anesthetics, such as pentobarbital; these are bound at a separate allosteric effector binding site. Functions as ligand-gated chloride channel (By similarity).

See Also

6d1s, resolution 3.20Å

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