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.
Milligan
G
G
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
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