Structure of the δ-opioid receptor bound to naltrindole

Nature

Volumn 485, Issue 7398, 2012, Pages 400-404

  Granier, Sébastien ^a,b   Manglik, Aashish ^a   Kruse, Andrew C ^a   Kobilka, Tong Sun ^a   Thian, Foon Sun ^a   Weis, William I ^a   Kobilka, Brian K ^a  

^a STANFORD UNIVERSITY SCHOOL OF MEDICINE   (United States)

^b UNIV MONTPELLIER   (France)

Author keywords

[No Author keywords available]

Indexed keywords

DELTA OPIATE RECEPTOR; G PROTEIN COUPLED RECEPTOR; KAPPA OPIATE RECEPTOR; MU OPIATE RECEPTOR; NALTRINDOLE;

ALKALOID; LIGAND; PEPTIDE; PROTEIN;

ARTICLE; CRYSTAL STRUCTURE; MOUSE; NONHUMAN; PRIORITY JOURNAL;

AMINO ACID SEQUENCE; ANIMALS; BINDING SITES; CONSERVED SEQUENCE; CRYSTALLOGRAPHY, X-RAY; MICE; MODELS, MOLECULAR; MOLECULAR SEQUENCE DATA; NALTREXONE; PROTEIN STRUCTURE, TERTIARY; RECEPTORS, OPIOID, DELTA; REPRODUCIBILITY OF RESULTS; STRUCTURE-ACTIVITY RELATIONSHIP; SUBSTRATE SPECIFICITY;

EID: 84861075468     PISSN: 00280836     EISSN: 14764687     Source Type: Journal    
DOI: 10.1038/nature11111     Document Type: Article

References (26)

1. Pradhan, A. A., Befort, K., Nozaki, C., Gaveriaux-Ruff, C. & Kieffer, B. L. The delta opioid receptor: an evolving target for the treatment of brain disorders. Trends Pharmacol. Sci. 32, 581-590 (2011).
2. Manglik, A. et al. Crystal structure of the m-opioid receptor bound to a morphinan antagonist. Nature http://dx.doi.org/10.1038/nature10954 (this issue).
3. Wu, H. et al. Structure of the human k-opioid receptor in complex with JDTic. Nature http://dx.doi.org/10.1038/10939 (this issue).
4. Chavkin, C. & Goldstein, A. Specific receptor for the opioid peptide dynorphin: structure-activity relationships. Proc. Natl Acad. Sci. USA 78, 6543-6547 (1981).
5. Lipkowski, A. W., Tam, S. W. & Portoghese, P. S. Peptides as receptor selectivity modulators of opiate pharmacophores. J. Med. Chem. 29, 1222-1225 (1986).
6. Satoh, M. & Minami, M. Molecular pharmacology of the opioid receptors. Pharmacol. Ther. 68, 343-364 (1995).
7. Mollereau, C. et al. ORL1, a novel member of the opioid receptor family. Cloning, functional expression and localization. FEBS Lett. 341, 33-38 (1994).
8. Cox, B. M. et al. Opioid Receptors: Introduction http://www.iuphar-db. org/DATABASE/FamilyIntroductionForward?familyId550 (2009).
9. Portoghese, P. S., Sultana, M., Nagase, H. & Takemori, A. E. Application of the message-address concept in the design of highlypotentand selective non-peptide d opioid receptor antagonists. J. Med. Chem. 31, 281-282 (1988).
10. Warne, T. et al. Structure of a b1-adrenergic G-protein-coupled receptor. Nature 454, 486-491 (2008).
11. George, S. R. et al. Oligomerization of m-andd-opioid receptors. Generation of novel functional properties. J. Biol. Chem. 275, 26128-26135 (2000).
12. Portoghese, P. S., Larson, D. L., Sayre, L. M., Fries, D. S. & Takemori, A. E. A novel opioid receptor site directed alkylating agent with irreversible narcotic antagonistic and reversible agonistic activities. J. Med. Chem. 23, 233-234 (1980).
13. Bonner, G., Meng, F. & Akil, H. Selectivity of m-opioid receptor determined by interfacial residues near third extracellular loop. Eur. J. Pharmacol. 403, 37-44 (2000).
14. Meng, F. et al. Creating a functional opioid alkaloid binding site in the orphanin FQ receptor through site-directedmutagenesis.Mol. Pharmacol. 53, 772-777 (1998).
15. Eguchi, M. Recent advances in selective opioid receptor agonists and antagonists. Med. Res. Rev. 24, 182-212 (2004).
16. Haga, K. et al. Structure of the humanM2muscarinic acetylcholine receptor bound to an antagonist. Nature 482, 547-551 (2011).
17. Valant, C. et al. A novel mechanism of G protein-coupled receptor functional selectivity. Muscarinic partial agonist McN-A-343 as a bitopic orthosteric/allosteric ligand. J. Biol. Chem. 283, 29312-29321 (2008).
18. Metzger, T. G., Paterlini, M. G., Ferguson, D. M. & Portoghese, P. S. Investigation of the selectivity of oxymorphone-and naltrexone-derived ligands via site-directed mutagenesis of opioid receptors: exploring the "address" recognition locus. J. Med. Chem. 44, 857-862 (2001).
19. Xue, J. C. et al. Differential binding domains of peptide and non-peptide ligands in the cloned rat k opioid receptor. J. Biol. Chem. 269, 30195-30199 (1994).
20. Pepin, M. C., Yue, S. Y., Roberts, E.,Wahlestedt, C.& Walker, P. Novel "restoration of function" mutagenesis strategy to identify amino acids of the d-opioid receptor involved in ligand binding. J. Biol. Chem. 272, 9260-9267 (1997).
21. Otwinowski, Z. & Minor, W. Processing of X-ray diffraction data collected in oscillation mode. Methods Enzymol. 276, 307-326 (1997).
22. McCoy, A. J. et al. Phaser crystallographic software. J. Appl. Cryst. 40, 658-674 (2007).
23. Emsley, P. & Cowtan, K. Coot: model-building tools for molecular graphics. Acta Crystallogr. D 60, 2126-2132 (2004).
24. Adams, P. D. et al. PHENIX: a comprehensive Python-based system for macromolecular structure solution. Acta Crystallogr. D 66, 213-221 (2010).
25. Chen, V. B. et al. MolProbity: all-atom structure validation for macromolecular crystallography. Acta Crystallogr. D 66, 12-21 (2010).
26. The. PyMOL Molecular Graphics System v. 1.5.0.1 (Schrödinger, LLC, 2012).