G-protein-coupled receptors are the most tractable class of protein targets for small molecule drug design. Sequencing of the human genome allied to bio-informatic analysis has identified a large number of putative receptors for which the natural ligands remain undefined. A range of currently employed and developing strategies to identify ligands that interact with these orphan receptors and to validate them as drug targets are described and discussed.
Conference Article| August 01 2002
Strategies to identify ligands for orphan G-protein-coupled receptors
G. Milligan 1
1Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, Davidson Building, University of Glasgow, Glasgow G12 8QQ, Scotland, U.K.
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G. Milligan; Strategies to identify ligands for orphan G-protein-coupled receptors. Biochem Soc Trans 1 August 2002; 30 (4): 789–793. doi: https://doi.org/10.1042/bst0300789
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