5o8f
From Proteopedia
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| - | '''Unreleased structure''' | ||
| - | + | ==Structure of a chimaeric beta3-alpha5 GABAA receptor in complex with nanobody Nb25 and pregnanolone== | |
| + | <StructureSection load='5o8f' size='340' side='right' caption='[[5o8f]], [[Resolution|resolution]] 3.20Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[5o8f]] is a 10 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5O8F OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5O8F FirstGlance]. <br> | ||
| + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=BMA:BETA-D-MANNOSE'>BMA</scene>, <scene name='pdbligand=MAN:ALPHA-D-MANNOSE'>MAN</scene>, <scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</scene>, <scene name='pdbligand=P9N:Pregnanolone'>P9N</scene></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=5o8f FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5o8f OCA], [http://pdbe.org/5o8f PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5o8f RCSB], [http://www.ebi.ac.uk/pdbsum/5o8f PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5o8f ProSAT]</span></td></tr> | ||
| + | </table> | ||
| + | == Disease == | ||
| + | [[http://www.uniprot.org/uniprot/GBRB3_HUMAN GBRB3_HUMAN]] Autism;Childhood absence epilepsy. Disease susceptibility is associated with variations affecting the gene represented in this entry. | ||
| + | == Function == | ||
| + | [[http://www.uniprot.org/uniprot/GBRB3_HUMAN GBRB3_HUMAN]] GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel. | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | Type A gamma-aminobutyric acid receptors (GABAARs) are the principal mediators of inhibitory neurotransmission in the human brain. Endogenous neurosteroids interact with GABAARs to regulate acute and chronic anxiety and are potent sedative, analgesic, anticonvulsant and anesthetic agents. Their mode of binding and mechanism of receptor potentiation, however, remain unknown. Here we report crystal structures of a chimeric GABAAR construct in apo and pregnanolone-bound states. The neurosteroid-binding site is mechanically coupled to the helices lining the ion channel pore and modulates the desensitization-gate conformation. We demonstrate that the equivalent site is responsible for physiological, heteromeric GABAAR potentiation and explain the contrasting modulatory properties of 3a versus 3b neurosteroid epimers. These results illustrate how peripheral lipid ligands can regulate the desensitization gate of GABAARs, a process of broad relevance to pentameric ligand-gated ion channels. | ||
| - | + | Structural basis for GABAA receptor potentiation by neurosteroids.,Miller PS, Scott S, Masiulis S, De Colibus L, Pardon E, Steyaert J, Aricescu AR Nat Struct Mol Biol. 2017 Oct 9. doi: 10.1038/nsmb.3484. PMID:28991263<ref>PMID:28991263</ref> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| - | [[Category: | + | </div> |
| + | <div class="pdbe-citations 5o8f" style="background-color:#fffaf0;"></div> | ||
| + | == References == | ||
| + | <references/> | ||
| + | __TOC__ | ||
| + | </StructureSection> | ||
| + | [[Category: Aricescu, A R]] | ||
| + | [[Category: Colibus, L De]] | ||
[[Category: Masiulis, S]] | [[Category: Masiulis, S]] | ||
| - | [[Category: Miller, P | + | [[Category: Miller, P S]] |
| - | + | ||
[[Category: Pardon, E]] | [[Category: Pardon, E]] | ||
| - | [[Category: Aricescu, A.R]] | ||
| - | [[Category: Steyaert, J]] | ||
[[Category: Scott, S]] | [[Category: Scott, S]] | ||
| + | [[Category: Steyaert, J]] | ||
| + | [[Category: Gabaa receptor]] | ||
| + | [[Category: Ion channel]] | ||
| + | [[Category: Membrane protein]] | ||
| + | [[Category: Nanobody complex]] | ||
| + | [[Category: Neurosteroid]] | ||
| + | [[Category: Pregnanolone]] | ||
Revision as of 06:07, 1 November 2017
Structure of a chimaeric beta3-alpha5 GABAA receptor in complex with nanobody Nb25 and pregnanolone
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