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Comment
. 2012 May 16;485(7398):314-7.
doi: 10.1038/485314a.

Structural biology: How opioid drugs bind to receptors

Comment

Structural biology: How opioid drugs bind to receptors

Marta Filizola et al. Nature. .

Abstract

The search for safe, non-addictive versions of morphine and other opioid drugs has just received a boost with the solving of the crystal structures of the receptors to which the drugs bind.

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Figures

Figure 1
Figure 1. Binding mode of opioids at their receptors
The structures of the four types of opioid receptor, each in complex with a different opioid antagonist, have been solved. A side view of one of the structures — that of the nociceptin/orphanin FQ peptide (NOP) receptor — is depicted to show features shared by all four receptor types. Only five of the seven transmembrane helices (TM1–7) are shown (grey cylinders). ECL2 is a β-hairpin loop region; the arrows represent β-sheets. The four antagonists used in the studies are depicted as stick representations in the NOP receptor’s binding pocket. The cyan surface indicates the amino-acid residues from TM3, TM6 and TM7 that interact with the ligands’ ‘message’ regions, responsible for a ligand’s efficacy. The magenta surfaces indicate the residues from TM6 and/or TM7 that interact with the ‘address’ region — responsible for opioid selectivity — of classical ligands, which contain the ‘morphinan’ chemical structure. The light-blue surfaces represent residues from TM2 and TM3 that interact with the address region of non-classical opioids.

Comment on

References

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