Seeking (and Finding) Biased Ligands of the Kappa Opioid Receptor

ACS Med Chem Lett. 2017 Jul 5;8(7):694-700. doi: 10.1021/acsmedchemlett.7b00224. eCollection 2017 Jul 13.


The discovery and characterization of two classes of kappa opioid receptor agonists that are biased for G protein over βarrestin signaling are described.

Keywords: G protein-coupled receptors; biased ligands; functional selectivity; kappa opioid receptor agonists; βArrestin.