Modulating β-arrestin 2 recruitment at the δ- and μ-opioid receptors using peptidomimetic ligands
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
Abstract
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.
Topics & Concepts
PeptidomimeticOpioidReceptorNeuroscienceChemistryOpioid receptorPharmacologyPsychologyMedicineBiochemistryPeptideReceptor Mechanisms and SignalingNeuropeptides and Animal PhysiologyPharmacological Receptor Mechanisms and Effects