Opioid Receptor Structure Findings May Lead to More Selective, Safer Pain Medication

A PPM Brief

University of North Carolina School of Medicine researchers have reported solving the crystal structure of the activated kappa opioid receptor (KOP) bound to a morphine derivative and used it to create a new compound that activates only that receptor, according to a January 10 UNC release. 

Published in Cell, the discovery may widen the sought-after pathway for appropriate opioid use without the adverse effects of nausea, constipation, anxiety, potential dependency, and even death due to respiratory depression.

Wrote the study team in their paper, “Taken together, these findings not only expand our general mechanistic framework of GPCR [G-protein-coupled receptor] activation but also provide molecular insights into KOP structure and function. Given the urgent need to develop safer opioid medications in an effort to battle the growing opioid epidemic, these molecular insights could greatly accelerate the design of novel KOP ligands through structure-enabled technologies and large-scale virtual ligand screening."