Article
Mutation of a conserved serine in TM4 of opioid receptors confers full agonistic properties to classical antagonists.
Proceedings of the National Academy of Sciences of the United States of America - 11 Jun 1996
Claude P A, Wotta D R, Zhang X H, Prather P L, McGinn T M, Erickson L J, Loh H H, Law P Y
Abstract excerpt
The involvement of a conserved serine (Ser196 at the mu-, Ser177 at the delta-, and Ser187 at the kappa-opioid receptor) in receptor activation is demonstrated by site-directed mutagenesis. It was initially observed during our functional screening of a mu/delta-opioid chimeric receptor, mu delta2, that classical opioid antagonists such as naloxone, naltrexone, naltriben, and H-Tyr-Tic[psi,CH2NH]Phe-Phe-OH...
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