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| Content Provider | World Health Organization (WHO)-Global Index Medicus |
|---|---|
| Author | Byrne, Bernadette Smith, Kathrine J. Hubbard, Julia A. Bertheleme, Nicolas Mossakowska, Danuta Chae, Pil Seok Singh, Shweta Hann, Michael M. Dowell, Simon J. |
| Description | Author Affiliation: Bertheleme N ( Department of Life Sciences, Imperial College London, SW7 2AZ, UK.) |
| Abstract | G-protein coupled receptors (GPCRs) are integral membrane cell surface receptors with key roles in mediating the cellular responses to a wide range of biologically relevant molecules including hormones, neurotransmitters and importantly the majority of currently available drugs. The first high-resolution, X-ray crystallographic structure of a GPCR, that of rhodopsin, was obtained in 2000. It took a further seven years for the next structure, that of the $β_{2}$ adrenergic receptor. Remarkably, at the time of writing, there have been an astonishing 18 further independent high-resolution GPCR structures published in the last five years (overall total of 68 structures in different conformations or bound to different ligands). Of particular note is the recent structure of the $β_{2}$ adrenergic receptor in complex with its cognate heterotrimeric G-protein revealing for the first time molecular details of the interaction between a GPCR and the complete G-protein. Together these structures have provided unprecedented detail into the mechanism of action of these incredibly important proteins. This review describes several key methodological advances that have made such extraordinarily fast progress possible. |
| ISSN | 00063002 |
| Journal | Biochimica et Biophysica Acta (BBA) - Reviews on Cancer |
| Issue Number | 11 |
| Volume Number | 1828 |
| Language | English |
| Publisher | Elsevier |
| Publisher Date | 2013-11-01 |
| Publisher Place | Netherlands |
| Access Restriction | Open |
| Subject Keyword | Receptors, G-Protein-Coupled Metabolism Crystallization Crystallography, X-Ray Immunoglobulin Fragments Models, Molecular Mutagenesis Chemistry Genetics Research Support, Non-U.S. Gov't Biochemistry |
| Content Type | Text |
| Resource Type | Article |
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