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Article Abstract
Agonists targeting the μ-opioid receptor (MOR) are the most effective analgesics, but their clinical use is limited by adverse side effects which are partly induced by β-arrestin signaling. Here, we combined in silico methods and cell-based functional assays to design novel structural scaffold molecules with high affinity that were biased at the G protein signaling of MOR. Furthermore, we explored the molecular mechanism of G protein subtype preference via computational methods. The results of our studies provide an insightful view into the ligand-MOR binding mode, which could serve as an important guide for the design of next-generation MOR ligands with reduced side effects.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC12260933 | PMC |
| http://dx.doi.org/10.1021/acsptsci.5c00055 | DOI Listing |
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