Determinants of ligand selectivity at the kappa-receptor based on the structure of the orphanin FQ receptor.

Abstract excerpt

It is unclear how opioid selectivity and activation are regulated within the receptor core. In previous studies, the OFQ receptor was converted into a functional opioid receptor by mutating five amino acids at three sites to the corresponding residues conserved across the mu-, kappa-, and delta-opioid receptors, suggesting that these sites comprise an opioid binding pocket. To examine this hypothesis, the present...

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