Home > Publications database > Structural basis for bifunctional peptide recognition at human $\delta$-opioid receptor > print

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100 1 _ |a Fenalti, Gustavo
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245 _ _ |a Structural basis for bifunctional peptide recognition at human $\delta$-opioid receptor
260 _ _ |a London [u.a.]
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|b Nature Publishing Group
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520 _ _ |a Bifunctional μ- and ​δ-opioid receptor (OR) ligands are potential therapeutic alternatives, with diminished side effects, to alkaloid opiate analgesics. We solved the structure of human ​δ-OR bound to the bifunctional ​δ-OR antagonist and ​μ-OR agonist tetrapeptide ​H-Dmt-Tic-Phe-Phe-NH2 (​DIPP-NH2) by serial femtosecond crystallography, revealing a cis-peptide bond between ​H-Dmt and ​Tic. The observed receptor-peptide interactions are critical for understanding of the pharmacological profiles of opioid peptides and for development of improved analgesics.
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773 _ _ |a 10.1038/nsmb.2965
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