Abstract:
:G-protein-coupled receptors (GPCRs), the largest family of membrane proteins, represent ideal therapeutic targets for a number of disorders and diseases. Besides cell-based assays and high throughput screening (HTS), and thanks to the availability of milligram quantities of active purified receptors, protein-based approaches focusing on soluble GPCRs are growingly being used in this drug discovery effort. Along with the exploitation of GPCRs structures, innovative biochemical and biophysical approaches open up new routes for improving the knowledge of structure-activity relationships, for the identification of novel interacting partners and for the determination of receptor behaviour in different model environments. This review summarizes the state-of-the-art methodologies that robustly allow for the production and purification of soluble and active GPCRs, as well as the main outcomes that have been recently gained in GPCR biology using a panel of such protein-based approaches.
journal_name
Curr Opin Pharmacoljournal_title
Current opinion in pharmacologyauthors
Alkhalfioui F,Magnin T,Wagner Rdoi
10.1016/j.coph.2009.04.002subject
Has Abstractpub_date
2009-10-01 00:00:00pages
629-35issue
5eissn
1471-4892issn
1471-4973pii
S1471-4892(09)00044-7journal_volume
9pub_type
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journal_title:Current opinion in pharmacology
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journal_title:Current opinion in pharmacology
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journal_title:Current opinion in pharmacology
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journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
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journal_title:Current opinion in pharmacology
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journal_title:Current opinion in pharmacology
pub_type: 杂志文章,评审
doi:10.1016/j.coph.2008.12.007
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journal_title:Current opinion in pharmacology
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doi:10.1016/j.coph.2013.07.005
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journal_title:Current opinion in pharmacology
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journal_title:Current opinion in pharmacology
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