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Drug Discov Today. 2002 Feb 15;7(4):235-46.

Target validation of G-protein coupled receptors.

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Systems Research, GlaxoSmithKline, Medicines Research Centre, Gunnels Wood Road, Stevenage, UK SG1 2NY.


G-protein coupled receptors (GPCRs) represent possibly the most important target class of proteins for drug discovery. Over 30% of clinically marketed drugs are active at this receptor family. These drugs exhibit their activity at <10% of all known GPCRs. A major challenge for the pharmaceutical industry is to associate the many novel GPCRs with disease to identify the drugs of the future. This process consists of a collection of experimental paradigms that together can be loosely labelled 'target validation'.

[Indexed for MEDLINE]

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