Structural basis for bifunctional peptide recognition at human δ-opioid receptor
Journal Article
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· Nature Structural & Molecular Biology
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- Scripps Research Inst., La Jolla, FL (United States). Dept. of Integrative Structural and Computational Biology
- Arizona State Univ., Tempe, AZ (United States). Dept. of Physics
- Vrije Univ., Brussels (Belgium). Dept. of Chemistry; Vrije Univ., Brussels (Belgium). Dept. of Bioengineering Sciences
- Univ. of North Carolina Chapel Hill Medical School, Chapel Hill, NC (United States). National Inst. of Mental Health; Univ. of North Carolina Chapel Hill Medical School, Chapel Hill, NC (United States). Dept. of Pharmacology; Univ. of North Carolina Chapel Hill Medical School, Chapel Hill, NC (United States). Division of Chemical Biology and Medicinal Chemistry
- SLAC National Accelerator Lab., Menlo Park, CA (United States). Linac Coherent Light Source (LCLS)
- Deutsches Elektronen-Synchrotron (DESY), Hamburg (Germany). Center for Free-Electron Laser Science
- Deutsches Elektronen-Synchrotron (DESY), Hamburg (Germany). Center for Free-Electron Laser Science; Univ. of Hamburg, Hamburg (Germany). Inst. of Biochemistry and Molecular Biology
- Deutsches Elektronen-Synchrotron (DESY), Hamburg (Germany). Center for Free-Electron Laser Science; Univ. of Hamburg, Hamburg (Germany). Dept. of Physics
- Deutsches Elektronen-Synchrotron (DESY), Hamburg (Germany). Center for Free-Electron Laser Science; European X-ray Free-Electron Laser (XFEL), Hamburg (Germany)
- Arizona State Univ., Tempe, AZ (United States). Dept. of Chemistry and Biochemistry; Arizona State Univ., Tempe, AZ (United States). Center for Applied Structural Discovery at the Biodesign Inst.
- Clinical Research Inst. of Montreal, Montreal, QC (Canada). Lab. of Chemical Biology and Peptide Research
Bi-functional μ- and δ- opioid receptor (OR) ligands are potential therapeutic alternatives to alkaloid opiate analgesics with diminished side effects. We solved the structure of human δ-OR bound to the bi-functional 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. In summary, the observed receptor-peptide interactions are critical to understand the pharmacological profiles of opioid peptides, and to develop improved analgesics.
- Research Organization:
- Argonne National Laboratory (ANL), Argonne, IL (United States). Advanced Photon Source (APS)
- Sponsoring Organization:
- National Institutes of Health (NIH); USDOE Office of Science (SC), Basic Energy Sciences (BES)
- Grant/Contract Number:
- U54 GM094618; R01 GM108635; R01 GM095583; DA-004443; Y1-CO-1020
- OSTI ID:
- 1178834
- Journal Information:
- Nature Structural & Molecular Biology, Vol. 22, Issue 3; ISSN 1545-9993
- Publisher:
- Nature Publishing GroupCopyright Statement
- Country of Publication:
- United States
- Language:
- ENGLISH
Cited by: 130 works
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