A family of fatty acid binding receptors.

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 Biol

journal_title

DNA and cell biology

authors

Brown AJ,Jupe S,Briscoe CP

doi

10.1089/dna.2005.24.54

keywords:

subject

Has Abstract

pub_date

2005-01-01 00:00:00

pages

54-61

issue

1

eissn

1044-5498

issn

1557-7430

journal_volume

24

pub_type

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