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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)

Chimaeric G alpha proteins: their potential use in drug discovery.

Approaches that allow ligand occupancy of a wide range of G protein-coupled receptors to be converted into robust assays amenable to relatively high-throughput analysis are ideal for screening for novel ligands at this class of receptor. Many attempts have been made to design universal ligand-screening systems such that any GPCR can be screened using a common assay end-point. Manipulation of the G protein within the assay system offers the possibility of achieving this. To better understand the domains involved in the interactions between G protein-coupled receptors, G proteins and effector polypeptides and the fine details of these contacts, a wide range of chimaeric G protein alpha subunits have been produced. Graeme Milligan and Stephen Rees discuss the information generated by such studies and the ways in which such chimaeric G proteins can be integrated into assay systems for drug discovery.[1]


  1. Chimaeric G alpha proteins: their potential use in drug discovery. Milligan, G., Rees, S. Trends Pharmacol. Sci. (1999) [Pubmed]
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