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000293073 1001_ $$0P:(DE-HGF)0$$aFenalti, Gustavo$$b0
000293073 245__ $$aStructural basis for bifunctional peptide recognition at human $\delta$-opioid receptor
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000293073 520__ $$aBifunctional μ- and ​δ-opioid receptor (OR) ligands are potential therapeutic alternatives, with diminished side effects, to alkaloid opiate analgesics. We solved the structure of human ​δ-OR bound to the bifunctional ​δ-OR antagonist and ​μ-OR agonist tetrapeptide ​H-Dmt-Tic-Phe-Phe-NH2 (​DIPP-NH2) by serial femtosecond crystallography, revealing a cis-peptide bond between ​H-Dmt and ​Tic. The observed receptor-peptide interactions are critical for understanding of the pharmacological profiles of opioid peptides and for development of improved analgesics.
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000293073 7001_ $$0P:(DE-HGF)0$$aHan, Gye Won$$b4
000293073 7001_ $$0P:(DE-HGF)0$$aIshchenko, Andrii$$b5
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000293073 7001_ $$0P:(DE-HGF)0$$aZhang, Haitao$$b8
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000293073 7001_ $$0P:(DE-HGF)0$$aWang, Dingjie$$b10
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000293073 7001_ $$00000-0002-5544-320X$$aCoe, Jesse$$b25
000293073 7001_ $$0P:(DE-HGF)0$$aConrad, Chelsie E$$b26
000293073 7001_ $$0P:(DE-HGF)0$$aFromme, Raimund$$b27
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000293073 7001_ $$0P:(DE-HGF)0$$aTourwé, Dirk$$b29
000293073 7001_ $$0P:(DE-HGF)0$$aSchiller, Peter W$$b30
000293073 7001_ $$0P:(DE-HGF)0$$aRoth, Bryan L$$b31
000293073 7001_ $$0P:(DE-HGF)0$$aBallet, Steven$$b32
000293073 7001_ $$0P:(DE-HGF)0$$aKatritch, Vsevolod$$b33
000293073 7001_ $$0P:(DE-HGF)0$$aStevens, Raymond C$$b34
000293073 7001_ $$00000-0002-5265-3914$$aCherezov, Vadim$$b35$$eCorresponding author
000293073 773__ $$0PERI:(DE-600)2131437-8$$a10.1038/nsmb.2965$$gVol. 22, no. 3, p. 265 - 268$$n3$$p265 - 268$$tNature structural & molecular biology$$v22$$x1545-9985$$y2015
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