Journal
BIOLOGICAL & PHARMACEUTICAL BULLETIN
Volume 31, Issue 10, Pages 1847-1851Publisher
PHARMACEUTICAL SOC JAPAN
DOI: 10.1248/bpb.31.1847
Keywords
G protein coupled receptor; free fatty acid; insulin; G protein receptor 40; G protein receptor 120
Categories
Funding
- Ministry of Education, Culture, Sports. Science and Technology of Japan
- Research Foundation for Pharmaceutical Sciences
- Society for Research oil Umami Taste
- Shimadzu Science Foundation
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Utilizing the human genome database, the recently developed G-protein-coupled receptor (GPCR) deorphanizing strategy successfully identified multiple receptors of free fatty, acids (FFAs) and is proposed to play a critical role in a variety of physiologic homeostasis mechanisms. GPR40 and GPR120 are activated by medium- and long-chain FFAs, whereas GPR41 and GPR43 are activated by short-chain FFAs. GPR40, which is preferentially expressed in pancreatic beta-cells, mediates insulin secretion. On the other hand, CPR120, which is abundantly expressed in the intestine, functions as a receptor for unsaturated long-chain FFAs and promotes the secretion of glucagon-like peptide-1 (GLP-1). In this review, we summarize the identification, structure, and pharmacology of the receptors and speculate on the respective physiologic roles that FFA receptor family members may play.
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