Structural basis for bifunctional peptide recognition at human ?-opioid receptor [electronic resource]

• Ngôn ngữ: eng
• Thông tin xuất bản: Bethesda, Md. : Oak Ridge, Tenn. : National Institutes of Health (U.S.) ; Distributed by the Office of Scientific and Technical Information, U.S. Dept. of Energy, 2015
• Mô tả vật lý: Size: p. 265-268 : , digital, PDF file.
• Bộ sưu tập: Metadata
• ID: 261254
• Chủ đề: 1. 60 applied life sciences; 2. G protein-coupled receptors; 3. Peptides; 4. X-ray crystallography

Tóm tắt

 Bi-functional ?- and ?- opioid receptor (OR) ligands are potential therapeutic alternatives to alkaloid opiate analgesics with diminished side effects. We solved the structure of human ?-OR bound to the bi-functional ?-OR antagonist and ?-OR agonist tetrapeptide H-Dmt-Tic-Phe-Phe-NH<
 sub>
 2<
 /sub>
  (DIPP-NH<
 sub>
 2<
 /sub>
 ) by serial femtosecond crystallography, revealing a cis-peptide bond between H-Dmt and Tic. In summary, the observed receptor-peptide interactions are critical to understand the pharmacological profiles of opioid peptides, and to develop improved analgesics.