A high affinity, mu-opioid receptor-selective enkephalin analogue lacking an N-terminal tyrosine |
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Authors: | HI Mosberg JC Ho K Sobczyk-Kojiro |
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Affiliation: | College of Pharmacy, University of Michigan, Ann Arbor 48109, USA. |
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Abstract: | We report a high affinity, mu opioid receptor selective enkephalin analogue in which the N-terminal tyrosine residue thought to be required for such high affinity is replaced by phenylalanine. The high affinity can be traced to a shift of the ligand's N-terminal residue within the mu receptor binding pocket, which diminishes the importance of the usual hydrogen bond between the tyrosine phenolic moiety and the receptor. |
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