The DOI matches its Crossref record; 6 of the 6 references it cites were found in a registry or an index.
The 2.6 Angstrom Crystal Structure of a Human A 2A Adenosine Receptor Bound to an Antagonist
Open accessAbstract
The adenosine class of heterotrimeric guanine nucleotide–binding protein (G protein)–coupled receptors (GPCRs) mediates the important role of extracellular adenosine in many physiological processes and is antagonized by caffeine. We have determined the crystal structure of the human A 2A adenosine receptor, in complex with a high-affinity subtype-selective antagonist, ZM241385, to 2.6 angstrom resolution. Four disulfide bridges in the extracellular domain, combined with a subtle repacking of the transmembrane helices relative to the adrenergic and rhodopsin receptor structures, define a pocket distinct from that of other structurally determined GPCRs. The arrangement allows for the binding of the antagonist in an extended conformation, perpendicular to the membrane plane. The binding site highlights an integral role for the extracellular loops, together with the helical core, in ligand recognition by this class of GPCRs and suggests a role for ZM241385 in restricting the movement of a tryptophan residue important in the activation mechanism of the class A receptors.
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Cites
Crystal Structure of Rhodopsin: A G Protein-Coupled Receptor
Palczewski, K., Kumasaka, T., Hori, T., Behnke, C. A., Motoshima, H., Fox, B. A., Trong, I. L., Teller, D. C., Okada, T., Stenkamp, R. E., et al. (2000) · Science · doi:10.1126/science.289.5480.739 · Cited by 5,637
Adenosine Receptors as Therapeutic Targets
Jacobson, K. A., & Gao, Z.-G. (2006) · Nature Reviews Drug Discovery · doi:10.1038/nrd1983 · Cited by 1,431
The Retinal Conformation and its Environment in Rhodopsin in Light of a New 2.2 Å Crystal Structure
Okada, T., Sugihara, M., Bondar, A.-N., Elstner, M., Entel, P., & Buss, V. (2004) · Journal of Molecular Biology · doi:10.1016/j.jmb.2004.07.044 · Cited by 1,049
A meta‐analysis of coffee drinking, cigarette smoking, and the risk of Parkinson's disease
Hernán, M. A., Takkouche, B., Caamaño‐Isorna, F., & Gestal‐Otero, J. J. (2002) · Annals of Neurology · doi:10.1002/ana.10277 · Cited by 818
An Update on the Mechanisms of the Psychostimulant Effects of Caffeine
Ferré, S. (2008) · Journal of Neurochemistry · doi:10.1111/j.1471-4159.2007.05196.x · Cited by 440
Adenosine A1-A2A receptor heteromers: New targets for caffeine in the brain
Ferre, S. (2008) · Frontiers in bioscience · doi:10.2741/2852 · Cited by 149
Cited by
The structure and function of G-protein-coupled receptors
Rosenbaum, D. M., Rasmussen, S. G. F., & Kobilka, B. K. (2009) · Nature · doi:10.1038/nature08144 · Cited by 2,534
Agonist-bound adenosine A2A receptor structures reveal common features of GPCR activation
Lebon, G., Warne, T., Edwards, P. C., Bennett, K., Langmead, C. J., Leslie, A. G. W., & Tate, C. G. (2011) · Nature · doi:10.1038/nature10136 · Cited by 873
Structure of the human histamine H1 receptor complex with doxepin
Shimamura, T., Shiroishi, M., Weyand, S., Tsujimoto, H., Winter, G., Katritch, V., Abagyan, R., Cherezov, V., Liu, W., Han, G. W., et al. (2011) · Nature · doi:10.1038/nature10236 · Cited by 804
Self-citationPharmacology of Adenosine Receptors: The State of the Art
Borea, P. A., Gessi, S., Merighi, S., Vincenzi, F., & Varani, K. (2018) · Physiological Reviews · doi:10.1152/physrev.00049.2017 · Cited by 783
Machine learning unifies the modeling of materials and molecules
Bartók, A. P., De, S., Poelking, C., Bernstein, N., Kermode, J. R., Csányi, G., & Ceriotti, M. (2017) · Science Advances · doi:10.1126/sciadv.1701816 · Cited by 764
Metadata
- Authors
- Jaakola, V.-P., Griffith, M. T., Hanson, M. A., Cherezov, V., Chien, E. Y. T., Lane, J. R., IJzerman, A. P., & Stevens, R. C.
- Venue
- Science
- Published
- 2008-11-21
- Volume
- 322
- Issue
- 5905
- Pages
- 1211-1217
- ISSN
- 0036-8075 (ISSN-L)
- 1095-9203
- OpenAlex
- W1975740938
- Cited by
- 1,781
- References
- 6
- FWCI
- 78.91
- Type
- journal article
- Language
- en
- Open access
- green
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- Jaakola, V.-P., Griffith, M. T., Hanson, M. A., Cherezov, V., Chien, E. Y. T., Lane, J. R., IJzerman, A. P., & Stevens, R. C. (2008). The 2.6 Angstrom Crystal Structure of a Human A 2A Adenosine Receptor Bound to an Antagonist. Science. https://doi.org/10.1126/science.1164772
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Bibliographic data: Semantic Scholar, OpenAlex, Crossref.
Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
