Biased agonism is having a major impact on modern drug discovery, and describes the
ability of distinct G protein–coupled receptor (GPCR) ligands to activate different cell …

Biased agonism describes the ability of distinct G protein-coupled receptor (GPCR) ligands
to stabilise distinct receptor conformations leading to the activation of different cell signalling …

The field of biased agonism has grown substantially in recent years and the μ-opioid
receptor has been one of the most intensively studied receptor targets for developing biased …

G protein-biased agonists of the μ-opioid receptor (MOPr) have been proposed as an
improved class of opioid analgesics. Recent studies have been unable to reproduce the …

Highlights•Biased MOR ligands discovered using empirical, rational and natural product
approaches.•Biased MOR ligands produce analgesia with fewer side effects in mice and …

The opioid crisis represents a major worldwide public health crisis that has accelerated the
search for safer and more effective opioids. Over the past few years, the identification of …

Prescription opioids are a mainstay in the treatment of acute moderate to severe pain.
However, chronic use leads to a host of adverse consequences including tolerance and …

Evidence from several novel opioid agonists and knockout animals suggests that improved
opioid therapeutic window, notably for analgesia versus respiratory depression, is a result of …

Opioids, such as morphine, are the most clinically useful class of analgesic drugs for the
treatment of acute and chronic pain. However, the use of opioids is greatly limited by the …

In ligand bias different agonist drugs are thought to produce distinct signaling outputs when
activating the same receptor. If these signaling outputs mediate therapeutic versus adverse …