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7bvq

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(New page: '''Unreleased structure''' The entry 7bvq is ON HOLD until Paper Publication Authors: Xu, X., Kaindl, J., Clark, M., Hubner, H., Hirata, K., Sunahara, R., Gmeiner, P., Kobilka, B.K., Li...)
Current revision (15:36, 29 November 2023) (edit) (undo)
 
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'''Unreleased structure'''
 
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The entry 7bvq is ON HOLD until Paper Publication
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==Structure of human beta1 adrenergic receptor bound to carazolol==
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<StructureSection load='7bvq' size='340' side='right'caption='[[7bvq]], [[Resolution|resolution]] 2.50&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[7bvq]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Escherichia_virus_T4 Escherichia virus T4] 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=7BVQ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7BVQ FirstGlance]. <br>
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.5&#8491;</td></tr>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=1WV:(2S)-2,3-DIHYDROXYPROPYL+(7Z)-TETRADEC-7-ENOATE'>1WV</scene>, <scene name='pdbligand=CAU:(2S)-1-(9H-CARBAZOL-4-YLOXY)-3-(ISOPROPYLAMINO)PROPAN-2-OL'>CAU</scene>, <scene name='pdbligand=CIT:CITRIC+ACID'>CIT</scene>, <scene name='pdbligand=CLR:CHOLESTEROL'>CLR</scene>, <scene name='pdbligand=GLC:ALPHA-D-GLUCOSE'>GLC</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</scene>, <scene name='pdbligand=PG4:TETRAETHYLENE+GLYCOL'>PG4</scene>, <scene name='pdbligand=PRD_900001:alpha-maltose'>PRD_900001</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></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=7bvq FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7bvq OCA], [https://pdbe.org/7bvq PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7bvq RCSB], [https://www.ebi.ac.uk/pdbsum/7bvq PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7bvq ProSAT]</span></td></tr>
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/D9IEF7_BPT4 D9IEF7_BPT4] [https://www.uniprot.org/uniprot/ADRB1_HUMAN ADRB1_HUMAN] 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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Beta adrenergic receptors (betaARs) mediate physiologic responses to the catecholamines epinephrine and norepinephrine released by the sympathetic nervous system. While the hormone epinephrine binds beta1AR and beta2AR with similar affinity, the smaller neurotransmitter norepinephrine is approximately tenfold selective for the beta1AR. To understand the structural basis for this physiologically important selectivity, we solved the crystal structures of the human beta1AR bound to an antagonist carazolol and different agonists including norepinephrine, epinephrine and BI-167107. Structural comparison revealed that the catecholamine-binding pockets are identical between beta1AR and beta2AR, but the extracellular vestibules have different shapes and electrostatic properties. Metadynamics simulations and mutagenesis studies revealed that these differences influence the path norepinephrine takes to the orthosteric pocket and contribute to the different association rates and thus different affinities.
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Authors: Xu, X., Kaindl, J., Clark, M., Hubner, H., Hirata, K., Sunahara, R., Gmeiner, P., Kobilka, B.K., Liu, X.
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Binding pathway determines norepinephrine selectivity for the human beta1AR over beta2AR.,Xu X, Kaindl J, Clark MJ, Hubner H, Hirata K, Sunahara RK, Gmeiner P, Kobilka BK, Liu X Cell Res. 2020 Oct 22. pii: 10.1038/s41422-020-00424-2. doi:, 10.1038/s41422-020-00424-2. PMID:33093660<ref>PMID:33093660</ref>
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Description: Structure of human beta1 adrenergic receptor bound to carazolol
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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[[Category: Unreleased Structures]]
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</div>
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[[Category: Clark, M]]
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<div class="pdbe-citations 7bvq" style="background-color:#fffaf0;"></div>
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[[Category: Liu, X]]
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[[Category: Hirata, K]]
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==See Also==
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[[Category: Sunahara, R]]
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*[[Adrenergic receptor 3D structures|Adrenergic receptor 3D structures]]
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[[Category: Xu, X]]
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== References ==
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[[Category: Kobilka, B.K]]
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<references/>
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[[Category: Hubner, H]]
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__TOC__
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[[Category: Kaindl, J]]
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</StructureSection>
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[[Category: Gmeiner, P]]
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[[Category: Escherichia virus T4]]
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[[Category: Homo sapiens]]
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[[Category: Large Structures]]
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[[Category: Clark M]]
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[[Category: Gmeiner P]]
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[[Category: Hirata K]]
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[[Category: Hubner H]]
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[[Category: Kaindl J]]
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[[Category: Kobilka BK]]
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[[Category: Liu X]]
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[[Category: Sunahara R]]
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[[Category: Xu X]]

Current revision

Structure of human beta1 adrenergic receptor bound to carazolol

PDB ID 7bvq

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