Kawamata et al. 2003 J. Biol. Chem. 278: 9435–9440

So far some nuclear receptors for bile acids have been identified. However, no cell surface receptor for bile acids has yet been reported. We found that a novel G protein-coupled receptor, TGR5, is responsive to bile acids as a cell-surface receptor. Bile acids specifically induced receptor internalization, the activation of extracellular signal-regulated kinase mitogen-activated protein kinase, the increase of guanosine 5
-O-3-thiotriphosphate binding in membrane fractions, and intracellular cAMP production in Chinese hamster ovary cells expressing TGR5. Our quantitative analyses for [TGR5 mRNA showed that it was abundantly expressed in monocytes/macrophages in human and rabbit](brain://avtLtJdGU06FUkyhaOD44g…