The DOI matches its Crossref record; 63 of the 63 references it cites were found in a registry or an index.
Structural insights into µ-opioid receptor activation
Open accessAbstract
Activation of the μ-opioid receptor (μOR) is responsible for the efficacy of the most effective analgesics. To shed light on the structural basis for μOR activation, here we report a 2.1 Å X-ray crystal structure of the murine μOR bound to the morphinan agonist BU72 and a G protein mimetic camelid antibody fragment. The BU72-stabilized changes in the μOR binding pocket are subtle and differ from those observed for agonist-bound structures of the β2-adrenergic receptor (β2AR) and the M2 muscarinic receptor. Comparison with active β2AR reveals a common rearrangement in the packing of three conserved amino acids in the core of the μOR, and molecular dynamics simulations illustrate how the ligand-binding pocket is conformationally linked to this conserved triad. Additionally, an extensive polar network between the ligand-binding pocket and the cytoplasmic domains appears to play a similar role in signal propagation for all three G-protein-coupled receptors.
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Cites
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Cited by
Molecular Dynamics Simulation for All
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Self-citationStructure of the µ-opioid receptor–Gi protein complex
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Metadata
- Authors
- Huang, W., Manglik, A., Venkatakrishnan, A. J., Laeremans, T., Feinberg, E. N., Sanborn, A. L., Kato, H. E., Livingston, K. E., Thorsen, T. S., Kling, R. C., Granier, S., Gmeiner, P., Husbands, S. M., Traynor, J. R., Weis, W. I., Steyaert, J., Dror, R. O., & Kobilka, B. K.
- Venue
- Nature
- Published
- 2015-08
- Volume
- 524
- Issue
- 7565
- Pages
- 315-321
- ISSN
- 0028-0836 (ISSN-L)
- 1476-4687
- OpenAlex
- W1918796765
- Cited by
- 885
- References
- 63
- FWCI
- 35.38
- Type
- journal article
- Language
- en
- Open access
- bronze
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- Huang, W., Manglik, A., Venkatakrishnan, A. J., Laeremans, T., Feinberg, E. N., Sanborn, A. L., Kato, H. E., Livingston, K. E., Thorsen, T. S., Kling, R. C., Granier, S., Gmeiner, P., Husbands, S. M., Traynor, J. R., Weis, W. I., Steyaert, J., Dror, R. O., & Kobilka, B. K. (2015). Structural insights into µ-opioid receptor activation. Nature. https://doi.org/10.1038/nature14886
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