Chemotype-selective modes of action of κ-opioid receptor agonists.
The Journal of biological chemistry November 29, 2013 Eyal Vardy, Philip D Mosier, Kevin J Frankowski et al.
The crystal structures of opioid receptors provide a novel platform for inquiry into opioid receptor function. The molecular determinants for activation of the κ-opioid receptor (KOR) were studied using a combination of agonist docking, functional assays, and site-directed mutagenesis. Eighteen positions in the putative agonist binding site of KOR were selected and evaluated for their effects...