Article
Chemotype-selective modes of action of κ-opioid receptor agonists.
The Journal of biological chemistry - 29 Nov 2013
Vardy Eyal, Mosier Philip D, Frankowski Kevin J, Wu Huixian, Katritch Vsevolod, Westkaemper Richard B, Aubé Jeffrey, Stevens Raymond C, Roth Bryan L
Abstract excerpt
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 on receptor binding...
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