Tyrosine 7.43 is important for mu-opioid receptor downstream signaling pathways activated by fentanyl.

ABSTRACT: G protein-coupled receptors can signal through both G proteins and ß-arrestin2. For the µ-opioid receptor (MOR), early experimental evidence from a single study suggested that G protein signaling mediates analgesia and sedation, whereas ß-arrestin signaling mediates respiratory depression and constipation. Then, receptor mutations were used to clarify which residues interact with ligands to selectively regulate signals in a ligand-specific manner. However, there is no systematic study on how to determine these residues and clarify the molecular mechanism of their influence on signal pathways. We have therefore used molecular docking to predict the amino acid sites that affect the binding of ligands and MOR. Then, the corresponding sites were mutated to determine the ef

SUBMITTER: Tian X 

PROVIDER: S-EPMC9478952 | biostudies-literature | 2022

REPOSITORIES: biostudies-literature