Strategies to identify ligands for orphan G-protein-coupled receptors.
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.
Molecular Pharmacology Group, Division of Biochemistry and Molecular Biology, Institute of Biomedical and Life Sciences, Davidson Building, University of Glasgow, Glasgow G12 8QQ, Scotland, UK. g.milligan@bio.gla.ac.uk
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D000818:Animals; D002118:Calcium / Q000378:metabolism; D004345:Drug Industry / Q000379:methods* / Q000639:trends; D019204:GTP-Binding Proteins / Q000235:genetics / Q000378:metabolism*; D008024:Ligands; D021381:Protein Transport; D011956:Receptors, Cell Surface / Q000819:agonists / Q000037:antagonists & inhibitors / Q000235:genetics / Q000378:metabolism*
D008024:Ligands; D011956:Receptors, Cell Surface; D019204:GTP-Binding Proteins; D002118:Calcium