Abstract:
:The family of G protein-coupled receptors (GPCRs) serves as the target for almost a third of currently marketed drugs, and provides the predominant mechanism through which extracellular factors transmit signals to the cell. The discovery of GPCRs with no known ligand has initiated a frenzy of research, with the aim of elucidating the physiological ligands for these "orphan" receptors and revealing new drug targets. The GPR40 family of receptors, tandemly located on chromosome 19q13.1, exhibit 30-40% homology to one another and diverse tissue distribution, yet all are activated by fatty acids. Since agonists of GPR40 are medium to longchain fatty acids and those for GPR41 and 43 are short-chain fatty acids, the family clearly provides an intriguing example of how the ligand specificity, patterns of expression, and function of GPCRs can diverge through evolution. Here we summarize the identification, structure, and pharmacology of the receptors and speculate on the respective physiological roles that the GPR40 family members may play.
journal_name
DNA Cell Bioljournal_title
DNA and cell biologyauthors
Brown AJ,Jupe S,Briscoe CPdoi
10.1089/dna.2005.24.54keywords:
subject
Has Abstractpub_date
2005-01-01 00:00:00pages
54-61issue
1eissn
1044-5498issn
1557-7430journal_volume
24pub_type
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