Journal
BIOCHEMICAL PHARMACOLOGY
Volume 110, Issue -, Pages 1-15Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bcp.2016.01.021
Keywords
Free-fatty acid receptor-4; GPR120; Polyunsaturated fats; G protein-coupled receptors; Free fatty acids
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Funding
- National Institutes of Health, National Institute of Diabetes and Digestive and Kidney Diseases Grant [DK098730]
- Diabetes Action Research and Educational Foundation
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Over the last decade, a subfamily of G protein-coupled receptors that are agonized by endogenous and dietary free-fatty acids (FFA) has been discovered. These free-fatty acid receptors include FFA2 and FFA3, which are agonized by short-chained FFA, as well as FFA1 and FFA4, which are agonized by medium-to-long chained FFA. Ligands for FFA1 and FFA4 comprise the family of long chain polyunsaturated omega-3 fatty acids including alpha-linolenic acid (ALA), eicosapentaenoic acid (EPA), and docosahexaenoic acid (DHA), suggesting that many of the long-known beneficial effects of these fats may be receptor mediated. In this regard, FFA4 has gathered considerable interest due to its role in ameliorating inflammation, promoting insulin sensitization, and regulating energy metabolism in response to FFA ligands. The goal of this review is to summarize the body of evidence in regard to FFA4 signal transduction, its mechanisms of regulation, and its functional role in a variety of tissues. In addition, recent endeavors toward discovery of small molecules that modulate FFA4 activity are also presented. (C) 2016 Elsevier Inc. All rights reserved.
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