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Structural basis for bifunctional peptide recognition at human ?-opioid receptor.

ABSTRACT: Bifunctional ?- and ?-opioid receptor (OR) ligands are potential therapeutic alternatives, with diminished side effects, to alkaloid opiate analgesics. We solved the structure of human ?-OR bound to the bifunctional ?-OR antagonist and ?-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.

SUBMITTER: Fenalti G 

PROVIDER: S-EPMC4351130 | biostudies-literature | 2015 Mar

REPOSITORIES: biostudies-literature

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Structural basis for bifunctional peptide recognition at human δ-opioid receptor.

Fenalti Gustavo G   Zatsepin Nadia A NA   Betti Cecilia C   Giguere Patrick P   Han Gye Won GW   Ishchenko Andrii A   Liu Wei W   Guillemyn Karel K   Zhang Haitao H   James Daniel D   Wang Dingjie D   Weierstall Uwe U   Spence John C H JC   Boutet Sébastien S   Messerschmidt Marc M   Williams Garth J GJ   Gati Cornelius C   Yefanov Oleksandr M OM   White Thomas A TA   Oberthuer Dominik D   Metz Markus M   Yoon Chun Hong CH   Barty Anton A   Chapman Henry N HN   Basu Shibom S   Coe Jesse J   Conrad Chelsie E CE   Fromme Raimund R   Fromme Petra P   Tourwé Dirk D   Schiller Peter W PW   Roth Bryan L BL   Ballet Steven S   Katritch Vsevolod V   Stevens Raymond C RC   Cherezov Vadim V  

Nature structural & molecular biology 20150216 3

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 opioi  ...[more]

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