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 …

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 …

Biased agonism at G protein–coupled receptors describes the phenomenon whereby some
drugs can activate some downstream signaling activities to the relative exclusion of others …

The peptidergic system is the most abundant network of ligand-receptor-mediated signaling
in humans. However, the physiological roles remain elusive for numerous peptides and …

Achieving effective pain management is one of the major challenges associated with
modern day medicine. Opioids, such as morphine, have been the reference treatment for …

GPCR functional selectivity opens new opportunities for the design of safer drugs. Ligands
orchestrate GPCR signaling cascades by modulating the receptor conformational …

Opioid drugs are widely used analgesics that activate the G protein-coupled µ-opioid
receptor, whose endogenous neuropeptide agonists, endorphins and enkephalins, are …

Synthetic opioids are increasingly challenging to combat the opioid epidemic and act
primarily at opioid receptors, chiefly the G protein-coupled receptor (GPCR) μ-opioid …

Hydroxycarboxylic acid receptors (HCA) are expressed in various tissues and immune cells.
HCA2 and its agonist are thus important targets for treating inflammatory and metabolic …

Driven by illicit fentanyl, opioid related deaths have reached the highest level in 2020.
Currently, an opioid overdose is resuscitated by the use of naloxone, which competitively …