Modulating β-arrestin 2 recruitment at the δ- and μ-opioid receptors using peptidomimetic ligands

作者：Krishna K. Sharma, Robert J. Cassell, Yazan J. Meqbil, Hongyu Su, Arryn T. Blaine, Benjamin Cummins, Kendall L. Mores, David K. Johnson, Richard M. van Rijn, Ryan A. Altman · 发表于：RSC Medicinal Chemistry · 年份：2021 · DOI：10.1039/d1md00025j · 被引用次数：12 · 研究领域：Receptor Mechanisms and Signaling、Neuropeptides and Animal Physiology、Pharmacological Receptor Mechanisms and Effects

Pr) reduced β-arrestin recruitment efficacy through both the δ-opioid and μ-opioid, while retaining affinity and cAMP potency. For this series, computational studies suggest key ligand-receptor interactions that might influence bias. These findings should enable the discovery of a range of tool compounds with previously unexplored biased μ/δ opioid agonist pharmacological profiles.