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(Crystal structure of the µ-opioid receptor bound to a morphinan antagonist)
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Notice that the inhibitor, shown as space-filling spheres, is nestled relatively deeply within the helical core. Binding at this position effects a change in conformation through a twisting action of the helices. This twisting gets delivered to a second binding site of the receptor. This second binding site is attached to the helical assembly via TM3 and TM6 (not shown here). It is where an associated protein that binds GTP can bind. This protein's binding is what makes this receptor a "G-protein-coupled receptor." Its binding triggers the transmission of the chemical "signal" delivered by the opioid (or, in this case, being prevented from doing that).
Notice that the inhibitor, shown as space-filling spheres, is nestled relatively deeply within the helical core. Binding at this position effects a change in conformation through a twisting action of the helices. This twisting gets delivered to a second binding site of the receptor. This second binding site is attached to the helical assembly via TM3 and TM6 (not shown here). It is where an associated protein that binds GTP can bind. This protein's binding is what makes this receptor a "G-protein-coupled receptor." Its binding triggers the transmission of the chemical "signal" delivered by the opioid (or, in this case, being prevented from doing that).
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Investigate the structure after downloading the <jmol><jmollink><text>figure</text><script>exit;SCRIPT "http://proteopedia.org/wiki/images/2/20/Nature10954Fig1aLeft_4dkl-2.png"</script></jmollink></jmol> by dragging it around using your mouse or clicking the buttons below. SHIFT-drag to zoom.
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Investigate the structure after loading the <jmol><jmollink><text>figure</text><script>exit;SCRIPT "http://proteopedia.org/wiki/images/2/20/Nature10954Fig1aLeft_4dkl-2.png"</script></jmollink></jmol> by dragging it around using your mouse or clicking the buttons below. SHIFT-drag to zoom.
<jmol><jmollink><text>(a) exocellular view</text><script>SCRIPT http://proteopedia.org/wiki/images/0/00/Nature10954_fig1d.spt('top')</script></jmollink></jmol>
<jmol><jmollink><text>(a) exocellular view</text><script>SCRIPT http://proteopedia.org/wiki/images/0/00/Nature10954_fig1d.spt('top')</script></jmollink></jmol>

Revision as of 02:40, 30 January 2018

Crystal structure of the µ-opioid receptor bound to a morphinan antagonist

[https://www.nature.com/articles/nature10954 Nature volume 485, pages 321–326 (17 May 2012) doi:10.1038/nature10954]

Click a green link on the left to load Figure 1

Drag the structure with the mouse to rotate

/wiki/images/8/8b/4dkl-local-contact.png code for the above (space inserted just after the : <jmol><jmollink><text>View Figure 1a: Overall view of the µ-OR structure</text><script>exit;figure=1;SCRIPT "/wiki/images/8/8b/4dkl-local-contact.png"</script></jmollink></jmol>




is a close-up view of a  bound to the µ-opioid receptor. The green circles indicate hydrogen bonds. 
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