Residues W320 and Y328 within the binding site of the μ-opioid receptor influence opiate ligand bias

@article{Hothersall2017ResiduesWA,
  title={Residues W320 and Y328 within the binding site of the μ-opioid receptor influence opiate ligand bias},
  author={J. Daniel Hothersall and Rubben Torella and Sian Humphreys and Monique Hooley and Alastair Brown and Gordon McMurray and Sarah A. Nickolls},
  journal={Neuropharmacology},
  year={2017},
  volume={118},
  pages={46-58}
}
The development of G protein-biased agonists for the μ-opioid receptor (MOR) offers a clear drug discovery rationale for improved analgesia and reduced side-effects of opiate pharmacotherapy. However, our understanding of the molecular mechanisms governing ligand bias is limited, which hinders our ability to rationally design biased compounds. We have investigated the role of MOR binding site residues W320 and Y328 in controlling bias, by receptor mutagenesis. The pharmacology of a panel of… CONTINUE READING

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The development of G protein - biased agonists for the μ-opioid receptor ( MOR ) offers a clear drug discovery rationale for improved analgesia and reduced side - effects of opiate pharmacotherapy .
OpioidsNo subtypeOpiates
The development of G protein - biased agonists for the μ-opioid receptor ( MOR ) offers a clear drug discovery rationale for improved analgesia and reduced side - effects of opiate pharmacotherapy .
OpioidsNo subtypeOpiates
The development of G protein - biased agonists for the μ-opioid receptor ( MOR ) offers a clear drug discovery rationale for improved analgesia and reduced side - effects of opiate pharmacotherapy .
The development of G protein - biased agonists for the μ-opioid receptor ( MOR ) offers a clear drug discovery rationale for improved analgesia and reduced side - effects of opiate pharmacotherapy .
OpiatesNo subtypeOpioids
The development of G protein - biased agonists for the μ-opioid receptor ( MOR ) offers a clear drug discovery rationale for improved analgesia and reduced side - effects of opiate pharmacotherapy .
The development of G protein - biased agonists for the μ-opioid receptor ( MOR ) offers a clear drug discovery rationale for improved analgesia and reduced side - effects of opiate pharmacotherapy .
OpiatesNo subtypeOpioids
The development of G protein - biased agonists for the μ-opioid receptor ( MOR ) offers a clear drug discovery rationale for improved analgesia and reduced side - effects of opiate pharmacotherapy .
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