|2rh1, resolution 2.40Å ()|
|Ligands:||, , , , , , ,|
|Gene:||ADRB2, ADRB2R, B2AR / E (Enterobacteria phage T4)|
High resolution crystal structure of human B2-adrenergic G protein-coupled receptor.
Heterotrimeric guanine nucleotide-binding protein (G protein)-coupled receptors constitute the largest family of eukaryotic signal transduction proteins that communicate across the membrane. We report the crystal structure of a human beta2-adrenergic receptor-T4 lysozyme fusion protein bound to the partial inverse agonist carazolol at 2.4 angstrom resolution. The structure provides a high-resolution view of a human G protein-coupled receptor bound to a diffusible ligand. Ligand-binding site accessibility is enabled by the second extracellular loop, which is held out of the binding cavity by a pair of closely spaced disulfide bridges and a short helical segment within the loop. Cholesterol, a necessary component for crystallization, mediates an intriguing parallel association of receptor molecules in the crystal lattice. Although the location of carazolol in the beta2-adrenergic receptor is very similar to that of retinal in rhodopsin, structural differences in the ligand-binding site and other regions highlight the challenges in using rhodopsin as a template model for this large receptor family.
High-resolution crystal structure of an engineered human beta2-adrenergic G protein-coupled receptor., Cherezov V, Rosenbaum DM, Hanson MA, Rasmussen SG, Thian FS, Kobilka TS, Choi HJ, Kuhn P, Weis WI, Kobilka BK, Stevens RC, Science. 2007 Nov 23;318(5854):1258-65. Epub 2007 Oct 25. PMID:17962520
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
About this Structure
2rh1 is a 1 chain structure with sequence from Enterobacteria phage t4. The April 2008 RCSB PDB Molecule of the Month feature on Adrenergic Receptors by David S. Goodsell is 10.2210/rcsb_pdb/mom_2008_4. Full crystallographic information is available from OCA.
- Adrenergic receptor
- Beta-2 Adrenergic Receptor
- G protein-coupled receptor
- Nobel Prizes for 3D Molecular Structure
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- Cherezov V, Rosenbaum DM, Hanson MA, Rasmussen SG, Thian FS, Kobilka TS, Choi HJ, Kuhn P, Weis WI, Kobilka BK, Stevens RC. High-resolution crystal structure of an engineered human beta2-adrenergic G protein-coupled receptor. Science. 2007 Nov 23;318(5854):1258-65. Epub 2007 Oct 25. PMID:17962520