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

Abstract

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.

Authors:
 [1];  [2];  [3];  [4];  [1];  [1];  [1];  [3];  [1];  [2];  [2];  [2];  [2];  [5];  [5];  [5];  [6];  [6];  [6];  [7] more »;  [8];  [9];  [6];  [8];  [10]; ORCiD logo [10];  [10];  [10];  [10];  [3];  [11];  [4];  [3];  [1];  [1]; ORCiD logo [1] « less
+ Show Author Affiliations
  1. Scripps Research Inst., La Jolla, FL (United States). Dept. of Integrative Structural and Computational Biology
  2. Arizona State Univ., Tempe, AZ (United States). Dept. of Physics
  3. Vrije Univ., Brussels (Belgium). Dept. of Chemistry; Vrije Univ., Brussels (Belgium). Dept. of Bioengineering Sciences
  4. 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
  5. SLAC National Accelerator Lab., Menlo Park, CA (United States). Linac Coherent Light Source (LCLS)
  6. Deutsches Elektronen-Synchrotron (DESY), Hamburg (Germany). Center for Free-Electron Laser Science
  7. Deutsches Elektronen-Synchrotron (DESY), Hamburg (Germany). Center for Free-Electron Laser Science; Univ. of Hamburg, Hamburg (Germany). Inst. of Biochemistry and Molecular Biology
  8. Deutsches Elektronen-Synchrotron (DESY), Hamburg (Germany). Center for Free-Electron Laser Science; Univ. of Hamburg, Hamburg (Germany). Dept. of Physics
  9. Deutsches Elektronen-Synchrotron (DESY), Hamburg (Germany). Center for Free-Electron Laser Science; European X-ray Free-Electron Laser (XFEL), Hamburg (Germany)
  10. 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.
  11. Clinical Research Inst. of Montreal, Montreal, QC (Canada). Lab. of Chemical Biology and Peptide Research
Publication Date:
Research Org.:
Argonne National Laboratory (ANL), Argonne, IL (United States). Advanced Photon Source (APS)
Sponsoring Org.:
National Institutes of Health (NIH); USDOE Office of Science (SC), Basic Energy Sciences (BES)
OSTI Identifier:
1178834
Grant/Contract Number:  
U54 GM094618; R01 GM108635; R01 GM095583; DA-004443; Y1-CO-1020
Resource Type:
Accepted Manuscript
Journal Name:
Nature Structural & Molecular Biology
Additional Journal Information:
Journal Volume: 22; Journal Issue: 3; Journal ID: ISSN 1545-9993
Publisher:
Nature Publishing Group
Country of Publication:
United States
Language:
ENGLISH
Subject:
60 APPLIED LIFE SCIENCES; G protein-coupled receptors; Peptides; X-ray crystallography

Citation Formats

Fenalti, Gustavo, Zatsepin, Nadia A., Betti, Cecilia, Giguere, Patrick, Han, Gye Won, Ishchenko, Andrii, Liu, Wei, Guillemyn, Karel, Zhang, Haitao, James, Daniel, Wang, Dingjie, Weierstall, Uwe, Spence, John C. H., Boutet, Sébastien, Messerschmidt, Marc, Williams, Garth J., Gati, Cornelius, Yefanov, Oleksandr M., White, Thomas A., Oberthuer, Dominik, Metz, Markus, Yoon, Chun Hong, Barty, Anton, Chapman, Henry N., Basu, Shibom, Coe, Jesse, Conrad, Chelsie E., Fromme, Raimund, Fromme, Petra, Tourwé, Dirk, Schiller, Peter W., Roth, Bryan L., Ballet, Steven, Katritch, Vsevolod, Stevens, Raymond C., and Cherezov, Vadim. Structural basis for bifunctional peptide recognition at human δ-opioid receptor. United States: N. p., 2015. Web. doi:10.1038/nsmb.2965.
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Fenalti, Gustavo, Zatsepin, Nadia A., Betti, Cecilia, Giguere, Patrick, Han, Gye Won, Ishchenko, Andrii, Liu, Wei, Guillemyn, Karel, Zhang, Haitao, James, Daniel, Wang, Dingjie, Weierstall, Uwe, Spence, John C. H., Boutet, Sébastien, Messerschmidt, Marc, Williams, Garth J., Gati, Cornelius, Yefanov, Oleksandr M., White, Thomas A., Oberthuer, Dominik, Metz, Markus, Yoon, Chun Hong, Barty, Anton, Chapman, Henry N., Basu, Shibom, Coe, Jesse, Conrad, Chelsie E., Fromme, Raimund, Fromme, Petra, Tourwé, Dirk, Schiller, Peter W., Roth, Bryan L., Ballet, Steven, Katritch, Vsevolod, Stevens, Raymond C., & Cherezov, Vadim. Structural basis for bifunctional peptide recognition at human δ-opioid receptor. United States. https://doi.org/10.1038/nsmb.2965
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Fenalti, Gustavo, Zatsepin, Nadia A., Betti, Cecilia, Giguere, Patrick, Han, Gye Won, Ishchenko, Andrii, Liu, Wei, Guillemyn, Karel, Zhang, Haitao, James, Daniel, Wang, Dingjie, Weierstall, Uwe, Spence, John C. H., Boutet, Sébastien, Messerschmidt, Marc, Williams, Garth J., Gati, Cornelius, Yefanov, Oleksandr M., White, Thomas A., Oberthuer, Dominik, Metz, Markus, Yoon, Chun Hong, Barty, Anton, Chapman, Henry N., Basu, Shibom, Coe, Jesse, Conrad, Chelsie E., Fromme, Raimund, Fromme, Petra, Tourwé, Dirk, Schiller, Peter W., Roth, Bryan L., Ballet, Steven, Katritch, Vsevolod, Stevens, Raymond C., and Cherezov, Vadim. Mon . "Structural basis for bifunctional peptide recognition at human δ-opioid receptor". United States. https://doi.org/10.1038/nsmb.2965. https://www.osti.gov/servlets/purl/1178834.
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@article{osti_1178834,
title = {Structural basis for bifunctional peptide recognition at human δ-opioid receptor},
author = {Fenalti, Gustavo and Zatsepin, Nadia A. and Betti, Cecilia and Giguere, Patrick and Han, Gye Won and Ishchenko, Andrii and Liu, Wei and Guillemyn, Karel and Zhang, Haitao and James, Daniel and Wang, Dingjie and Weierstall, Uwe and Spence, John C. H. and Boutet, Sébastien and Messerschmidt, Marc and Williams, Garth J. and Gati, Cornelius and Yefanov, Oleksandr M. and White, Thomas A. and Oberthuer, Dominik and Metz, Markus and Yoon, Chun Hong and Barty, Anton and Chapman, Henry N. and Basu, Shibom and Coe, Jesse and Conrad, Chelsie E. and Fromme, Raimund and Fromme, Petra and Tourwé, Dirk and Schiller, Peter W. and Roth, Bryan L. and Ballet, Steven and Katritch, Vsevolod and Stevens, Raymond C. and Cherezov, Vadim},
abstractNote = {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.},
doi = {10.1038/nsmb.2965},
journal = {Nature Structural & Molecular Biology},
number = 3,
volume = 22,
place = {United States},
year = {Mon Feb 16 00:00:00 EST 2015},
month = {Mon Feb 16 00:00:00 EST 2015}
}
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https://doi.org/10.1038/nsmb.2965
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Cited by: 130 works
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Figures / Tables:

Figure 1 Figure 1: Structure of the BRIL$Δ$36$δ$-OR–DIPP-NH2 complex a, Overall view of $δ$-OR (purple cartoon, red ECL2) in complex with DIPP-NH2 (orange sticks and transparent spheres); residues lining the binding pocket are shown as light blue sticks, hydrogen bonds as black dotted lines, and water molecules as red spheres. b,more » Chemical structures of DIPP-NH2, endomorphin-1 and endomorphin-2 showing the structural similarities between the peptide analogue DIPP-NH2 and endogenous OR peptides. c, Close-up view of the DIPP-NH2 binding site; residues forming the DIPP-NH2 pocket are shown as light blue sticks. d, Sliced surface representation of the peptide binding pocket. The omit $Fo$-$Fc$ electron density around the peptide DIPP-NH2 is contoured at 3$σ$ and shown as a blue mesh.« less
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