Opioid receptors: Structural and mechanistic insights into pharmacology and signaling

Eur J Pharmacol. 2015 Sep 15;763(Pt B):206-13. doi: 10.1016/j.ejphar.2015.05.012. Epub 2015 May 14.


Opioid receptors are important drug targets for pain management, addiction, and mood disorders. Although substantial research on these important subtypes of G protein-coupled receptors has been conducted over the past two decades to discover ligands with higher specificity and diminished side effects, currently used opioid therapeutics remain suboptimal. Luckily, recent advances in structural biology of opioid receptors provide unprecedented insights into opioid receptor pharmacology and signaling. We review here a few recent studies that have used the crystal structures of opioid receptors as a basis for revealing mechanistic details of signal transduction mediated by these receptors, and for the purpose of drug discovery.

Keywords: Allosteric modulators; Dimerization; Functional selectivity; GPCRs; Molecular dynamics; Opioid binding; Receptor; Virtual screening.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, U.S. Gov't, Non-P.H.S.
  • Review

MeSH terms

  • Animals
  • Drug Design
  • Humans
  • Ligands
  • Pharmacology / methods*
  • Protein Multimerization
  • Receptors, Opioid / chemistry*
  • Receptors, Opioid / metabolism*
  • Signal Transduction / drug effects*


  • Ligands
  • Receptors, Opioid