Orphan GPCR target validation.
Nearly half of the identified non-olfactory G protein-coupled receptors (GPCRs) have no identified cognate ligand. These 'orphan' receptors are likely to have important physiological roles that could potentially be exploited therapeutically. However, by definition, such receptors are not immediately open for pharmacological investigation of their function. Here we summarize several strategic approaches to facilitate the discovery of orphan GPCR biology.
Thomsen
William
W
Arena Pharmaceuticals Inc, 6166 Nancy Ridge Drive, San Diego, CA 92121, USA.
Leonard
James
J
Behan
Dominic P
DP
D000818:Animals; D018390:Gene Targeting / Q000379:methods*; D006801:Humans; D016376:Oligonucleotides, Antisense / Q000235:genetics / Q000378:metabolism; D043562:Receptors, G-Protein-Coupled / Q000737:chemistry / Q000235:genetics* / Q000378:metabolism
D016376:Oligonucleotides, Antisense; D043562:Receptors, G-Protein-Coupled