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Structural basis for bifunctional peptide recognition at human δ-opioid receptor.
- Source :
- Nature Structural & Molecular Biology; Mar2015, Vol. 22 Issue 3, p265-268, 4p
- Publication Year :
- 2015
-
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<subscript>2</subscript> (DIPP-NH<subscript>2</subscript>) 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. [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 15459993
- Volume :
- 22
- Issue :
- 3
- Database :
- Complementary Index
- Journal :
- Nature Structural & Molecular Biology
- Publication Type :
- Academic Journal
- Accession number :
- 101361290
- Full Text :
- https://doi.org/10.1038/nsmb.2965