4bvn

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<StructureSection load='4bvn' size='340' side='right'caption='[[4bvn]], [[Resolution|resolution]] 2.10&Aring;' scene=''>
<StructureSection load='4bvn' size='340' side='right'caption='[[4bvn]], [[Resolution|resolution]] 2.10&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[4bvn]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Melga Melga]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4BVN OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4BVN FirstGlance]. <br>
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<table><tr><td colspan='2'>[[4bvn]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Meleagris_gallopavo Meleagris gallopavo]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4BVN OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4BVN FirstGlance]. <br>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=MHA:(CARBAMOYLMETHYL-CARBOXYMETHYL-AMINO)-ACETIC+ACID'>MHA</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</scene>, <scene name='pdbligand=OLC:(2R)-2,3-DIHYDROXYPROPYL+(9Z)-OCTADEC-9-ENOATE'>OLC</scene>, <scene name='pdbligand=P32:4-{[(2S)-3-(TERT-BUTYLAMINO)-2-HYDROXYPROPYL]OXY}-3H-INDOLE-2-CARBONITRILE'>P32</scene></td></tr>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=MHA:(CARBAMOYLMETHYL-CARBOXYMETHYL-AMINO)-ACETIC+ACID'>MHA</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</scene>, <scene name='pdbligand=OLC:(2R)-2,3-DIHYDROXYPROPYL+(9Z)-OCTADEC-9-ENOATE'>OLC</scene>, <scene name='pdbligand=P32:4-{[(2S)-3-(TERT-BUTYLAMINO)-2-HYDROXYPROPYL]OXY}-3H-INDOLE-2-CARBONITRILE'>P32</scene></td></tr>
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<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=4bvn FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4bvn OCA], [http://pdbe.org/4bvn PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4bvn RCSB], [http://www.ebi.ac.uk/pdbsum/4bvn PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=4bvn ProSAT]</span></td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=4bvn FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4bvn OCA], [https://pdbe.org/4bvn PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4bvn RCSB], [https://www.ebi.ac.uk/pdbsum/4bvn PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4bvn ProSAT]</span></td></tr>
</table>
</table>
== Function ==
== Function ==
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[[http://www.uniprot.org/uniprot/ADRB1_MELGA ADRB1_MELGA]] Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. This receptor binds epinephrine and norepinephrine with approximately equal affinity.
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[[https://www.uniprot.org/uniprot/ADRB1_MELGA ADRB1_MELGA]] Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. This receptor binds epinephrine and norepinephrine with approximately equal affinity.
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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The beta1-adrenoceptor (beta1AR) is a G protein-coupled receptor (GPCR) that is activated by the endogenous agonists adrenaline and noradrenaline. We have determined the structure of an ultra-thermostable beta1AR mutant bound to the weak partial agonist cyanopindolol to 2.1 A resolution. High-quality crystals (100 mum plates) were grown in lipidic cubic phase without the assistance of a T4 lysozyme or BRIL fusion in cytoplasmic loop 3, which is commonly employed for GPCR crystallisation. An intramembrane Na+ ion was identified co-ordinated to Asp872.50, Ser1283.39 and 3 water molecules, which is part of a more extensive network of water molecules in a cavity formed between transmembrane helices 1, 2, 3, 6 and 7. Remarkably, this water network and Na+ ion is highly conserved between beta1AR and the adenosine A2A receptor (rmsd of 0.3 A), despite an overall rmsd of 2.4 A for all Calpha atoms and only 23% amino acid identity in the transmembrane regions. The affinity of agonist binding and nanobody Nb80 binding to beta1AR is unaffected by Na+ ions, but the stability of the receptor is decreased by 7.5 degrees C in the absence of Na+. Mutation of amino acid side chains that are involved in the co-ordination of either Na+ or water molecules in the network decreases the stability of beta1AR by 5-10 degrees C. The data suggest that the intramembrane Na+ and associated water network stabilise the ligand-free state of beta1AR, but still permits the receptor to form the activated state which involves the collapse of the Na+ binding pocket on agonist binding.
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The 2.1 A Resolution Structure of Cyanopindolol-Bound beta1-Adrenoceptor Identifies an Intramembrane Na+ Ion that Stabilises the Ligand-Free Receptor.,Miller-Gallacher JL, Nehme R, Warne T, Edwards PC, Schertler GF, Leslie AG, Tate CG PLoS One. 2014 Mar 24;9(3):e92727. doi: 10.1371/journal.pone.0092727. eCollection, 2014. PMID:24663151<ref>PMID:24663151</ref>
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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</div>
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<div class="pdbe-citations 4bvn" style="background-color:#fffaf0;"></div>
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==See Also==
==See Also==
*[[Adrenergic receptor 3D structures|Adrenergic receptor 3D structures]]
*[[Adrenergic receptor 3D structures|Adrenergic receptor 3D structures]]
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== References ==
 
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<references/>
 
__TOC__
__TOC__
</StructureSection>
</StructureSection>
[[Category: Large Structures]]
[[Category: Large Structures]]
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[[Category: Melga]]
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[[Category: Meleagris gallopavo]]
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[[Category: Edwards, P C]]
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[[Category: Edwards PC]]
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[[Category: Leslie, A G.W]]
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[[Category: Leslie AGW]]
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[[Category: Miller, J]]
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[[Category: Miller J]]
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[[Category: Nehme, R]]
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[[Category: Nehme R]]
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[[Category: Schertler, G]]
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[[Category: Schertler G]]
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[[Category: Tate, C G]]
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[[Category: Tate CG]]
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[[Category: Warne, T]]
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[[Category: Warne T]]
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[[Category: Signaling protein]]
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Revision as of 17:11, 7 September 2022

Ultra-thermostable beta1-adrenoceptor with cyanopindolol bound

PDB ID 4bvn

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