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

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-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