Molecular mechanisms controlling μ-opioid receptor activation

2020-02-06T04:20:27Z (GMT) by ARISBEL BATISTA GONDIN
This thesis has advanced the field of opioid receptors, which is a critical research area with much public attention due to the current “opioid epidemic” within western societies. This work has shown that synthetic forms of the endogenous opioids cause very distinct receptor regulation and movement within the cell surface, compared to the prototypical analgesic, morphine. Moreover, this work provides evidence that the efficacy of new generation opioid drugs, widely publicised to be biased ligands, is actually due to weak partial agonist activity. This is critical information, as some of these new drugs are currently being approved by the FDA.