4amj: Difference between revisions
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[[ | ==Turkey beta1 adrenergic receptor with stabilising mutations and bound biased agonist carvedilol== | ||
<StructureSection load='4amj' size='340' side='right' caption='[[4amj]], [[Resolution|resolution]] 2.30Å' scene=''> | |||
== Structural highlights == | |||
<table><tr><td colspan='2'>[[4amj]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Common_turkey Common turkey]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4AMJ OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4AMJ FirstGlance]. <br> | |||
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=2CV:HEGA-10'>2CV</scene>, <scene name='pdbligand=CVD:(2S)-1-(8H-CARBAZOL-4-YLOXY)-3-[2-(2-METHOXYPHENOXY)ETHYLAMINO]PROPAN-2-OL'>CVD</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</scene></td></tr> | |||
<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[1dep|1dep]], [[2vt4|2vt4]], [[2y00|2y00]], [[2y01|2y01]], [[2y02|2y02]], [[2y03|2y03]], [[2y04|2y04]], [[2ycw|2ycw]], [[2ycx|2ycx]], [[2ycy|2ycy]], [[2ycz|2ycz]], [[4ami|4ami]]</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=4amj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4amj OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4amj RCSB], [http://www.ebi.ac.uk/pdbsum/4amj PDBsum]</span></td></tr> | |||
</table> | |||
<div style="background-color:#fffaf0;"> | |||
== Publication Abstract from PubMed == | |||
The beta(1)-adrenoceptor (beta(1)AR) is the site of action of beta blockers used in the treatment of cardiac-related illnesses. Two beta blockers, carvedilol and bucindolol, show distinctive activities compared to other beta blockers and have been proposed as treatments tailored to the Arg/Gly389(8.56) polymorphism of the human beta(1)AR. Both carvedilol and bucindolol are classified as biased agonists, because they stimulate G protein-independent signaling, while acting as either inverse or partial agonists of the G protein pathway. We have determined the crystal structures of a thermostabilized avian beta(1)AR mutant bound to bucindolol and to carvedilol at 3.2 and 2.3 A resolution, respectively. In comparison to other beta blockers, bucindolol and carvedilol interact with additional residues, in extracellular loop 2 and transmembrane helix 7, which may promote G protein-independent signaling. The structures also suggest that there may be a structural explanation for the pharmacological differences arising from the Arg/Gly389(8.56) polymorphism. | |||
Crystal Structures of a Stabilized beta(1)-Adrenoceptor Bound to the Biased Agonists Bucindolol and Carvedilol.,Warne T, Edwards PC, Leslie AG, Tate CG Structure. 2012 May 9;20(5):841-9. PMID:22579251<ref>PMID:22579251</ref> | |||
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |||
</div> | |||
==See Also== | |||
*[[Adrenergic receptor|Adrenergic receptor]] | |||
== | == References == | ||
[[ | <references/> | ||
__TOC__ | |||
== | </StructureSection> | ||
< | [[Category: Common turkey]] | ||
[[Category: | [[Category: Edwards, P C]] | ||
[[Category: Edwards, P C | [[Category: Leslie, A G]] | ||
[[Category: Leslie, A G | [[Category: Tate, C G]] | ||
[[Category: Tate, C G | [[Category: Warne, T]] | ||
[[Category: Warne, T | |||
[[Category: 7tmr beta1-adrenoceptor]] | [[Category: 7tmr beta1-adrenoceptor]] | ||
[[Category: Biased agonist]] | [[Category: Biased agonist]] | ||
[[Category: Membrane protein]] | [[Category: Membrane protein]] | ||
[[Category: Stabilising mutation]] | [[Category: Stabilising mutation]] | ||
