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Article

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

Neuropharmacology - 15 May 2017

Hothersall J Daniel, Torella Rubben, Humphreys Sian, Hooley Monique, Brown Alastair, McMurray Gordon, Nickolls Sarah A

Abstract excerpt

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...

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Identifiers

PMID: 28283391
DOI: 10.1016/j.neuropharm.2017.03.007

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