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Differential interaction patterns of opioid analgesics with µ opioid receptors correlate with ligand-specific voltage sensitivity

The µ opioid receptor (MOR) is the key target for analgesia, but the application of opioids is accompanied by several issues. There is a wide range of opioid analgesics, differing in their chemical structure and their properties of receptor activation and subsequent effects. A better understanding o...

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Main Authors: Kirchhofer Sina B., Lim, Victor Jun Yu, Ernst, Sebastian, Karsai, Noemi, Julia, Ruland G., Canals, Meritxell, Kolb, Peter, Bünemann, Moritz
Format: Article
Language:English
Published: Philipps-Universität Marburg 2023
Subjects:
neuroscience
human
Biowissenschaften, Biologie
Life sciences
Online Access:PDF Full Text
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Summary:The µ opioid receptor (MOR) is the key target for analgesia, but the application of opioids is accompanied by several issues. There is a wide range of opioid analgesics, differing in their chemical structure and their properties of receptor activation and subsequent effects. A better understanding of ligand-receptor interactions and the resulting effects is important. Here, we calculated the respective binding poses for several opioids and analyzed interaction fingerprints between ligand and receptor. We further corroborated the interactions experimentally by cellular assays. As MOR was observed to display ligand-induced modulation of activity due to changes in membrane potential, we further analyzed the effects of voltage sensitivity on this receptor. Combining in silico and in vitro approaches, we defined discriminating interaction patterns responsible for ligand-specific voltage sensitivity and present new insights into their specific effects on activation of the MOR.
Item Description:Gefördert durch den Open-Access-Publikationsfonds der UB Marburg.
Physical Description:52 Pages
DOI:10.7554/eLife.91291

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