Abstract
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-NH 2 (DIPP-NH 2) 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.
Original language | English |
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Pages (from-to) | 265-268 |
Number of pages | 4 |
Journal | Nature Structural and Molecular Biology |
Volume | 22 |
Issue number | 3 |
DOIs | |
Publication status | Published - Mar 6 2015 |
ASJC Scopus subject areas
- Structural Biology
- Molecular Biology