ArticlePloS one2011
Ligand-directed functional selectivity at the mu opioid receptor revealed by label-free integrative pharmacology on-target.
Article in PloS one, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed.
- Label-free, real-time monitoring of membrane binding events at zeptomolar concentrations using frequency-locked optical microresonators.Nature communications · 2024Article
- Label-free, real-time monitoring of membrane binding events at zeptomolar concentrations using frequency-locked optical microresonators.bioRxiv : the preprint server for biology · 2023Article
- Pharmacology of Kappa Opioid Receptors: Novel Assays and Ligands.Frontiers in pharmacology · 2022Article
- A Dynamic Mass Redistribution Assay for the Human Sweet Taste Receptor Uncovers G-Protein Dependent Biased Ligands.Frontiers in pharmacology · 2022Article
- Pharmacological profile of the neuropeptide S receptor: Dynamic mass redistribution studies.Pharmacology research & perspectives · 2018Article
- Article
- Morphine-induced hyperalgesia involves mu opioid receptors and the metabolite morphine-3-glucuronide.Scientific reports · 2017Article
- Impedance-based analysis of mu opioid receptor signaling and underlying mechanisms.Biochemistry and biophysics reports · 2016Article
- B7-H4 downregulation induces mitochondrial dysfunction and enhances doxorubicin sensitivity via the cAMP/CREB/PGC1-α signaling pathway in HeLa cells.Pflugers Archiv : European journal of physiology · 2014Article
- Label-free cell phenotypic profiling decodes the composition and signaling of an endogenous ATP-sensitive potassium channel.Scientific reports · 2014Article
- Divergent label-free cell phenotypic pharmacology of ligands at the overexpressed β₂-adrenergic receptors.Scientific reports · 2014Article
- Label-free drug discovery.Frontiers in pharmacology · 2014Review
- Effect of anchoring 4-anilidopiperidines to opioid peptides.Bioorganic & medicinal chemistry letters · 2013Article
- Label-free integrative pharmacology on-target of opioid ligands at the opioid receptor family.BMC pharmacology & toxicology · 2013Article
- Ligand-directed signalling within the opioid receptor family.British journal of pharmacology · 2012Review
- Ligand-dependent conformations and dynamics of the serotonin 5-HT(2A) receptor determine its activation and membrane-driven oligomerization properties.PLoS computational biology · 2012Article
Corrections and comments
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Authors and funding
5 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Development of new opioid drugs that provide analgesia without producing dependence is important for pain treatment. Opioid agonist drugs exert their analgesia effects primarily by acting at the mu opioid receptor (MOR) sites. High-resolution differentiation of opioid ligands is crucial for the development of new lead drug candidates with better tolerance profiles. Here, we use a label-free integrative pharmacology on-target (iPOT) approach to characterize the functional selectivity of a library of known opioid ligands for the MOR. This approach is based on the ability to detect dynamic mass redistribution (DMR) arising from the activation of the MOR in living cells. DMR assays were performed in HEK-MOR cells with and without preconditioning with probe molecules using label-free resonant waveguide grating biosensors, wherein the probe molecules were used to modify the activity of specific signaling proteins downstream the MOR. DMR signals obtained were then translated into high resolution heat maps using similarity analysis based on a numerical matrix of DMR parameters. Our data indicate that the iPOT approach clearly differentiates functional selectivity for distinct MOR signaling pathways among different opioid ligands, thus opening new avenues to discover and quantify the functional selectivity of currently used and novel opioid receptor drugs.
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