Chemotype-selective modes of action of κ-opioid receptor agonists.
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...
DOI: 10.1074/jbc.m113.515668 (opens in new tab)
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Mutagenesis site-specific
Opiate opioid
Pharmacology
Receptor structure-function