Topic
Free fatty acid receptor
About: Free fatty acid receptor is a research topic. Over the lifetime, 1513 publications have been published within this topic receiving 88532 citations. The topic is also known as: GPR40-rel_orph & IPR013312.
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TL;DR: The results suggest that PPARs, by their ability to interact with a number of structurally diverse compounds, have acquired unique ligand-binding properties among the superfamily of nuclear receptors that are compatible with their biological activity.
Abstract: Peroxisome proliferator-activated receptors (PPARs) are nuclear hormone receptors controlling the expression of genes involved in lipid homeostasis PPARs activate gene transcription in response to a variety of compounds including hypolipidemic drugs as well as natural fatty acids From the plethora of PPAR activators, Scatchard analysis of receptor-ligand interactions has thus far identified only four ligands These are the chemotactic agent leukotriene B4 and the hypolipidemic drug Wy 14,643 for the alpha-subtype and a prostaglandin J2 metabolite and synthetic antidiabetic thiazolidinediones for the gamma-subtype Based on the hypothesis that ligand binding to PPAR would induce interactions of the receptor with transcriptional coactivators, we have developed a novel ligand sensor assay, termed coactivator-dependent receptor ligand assay (CARLA) With CARLA we have screened several natural and synthetic candidate ligands and have identified naturally occurring fatty acids and metabolites as well as hypolipidemic drugs as bona fide ligands of the three PPAR subtypes from Xenopus laevis Our results suggest that PPARs, by their ability to interact with a number of structurally diverse compounds, have acquired unique ligand-binding properties among the superfamily of nuclear receptors that are compatible with their biological activity
1,196 citations
TL;DR: It is suggested that PPARs are key messengers responsible for the translation of nutritional and pharmacological stimuli into changes in gene expression and differentiation pathways.
1,193 citations
TL;DR: A novel mechanism by which fatty acids modulate signaling pathways and target gene expression is represented by both SFA-induced COX-2 expression and its inhibition by UFAs are mediated through a common signaling pathway derived from Tlr4.
1,189 citations
TL;DR: In this article, the authors classified polyunsaturated fatty acids (PUFAs) in n-3 fatty acids and n-6 fatty acids, and in westernized diet the predominant dietary PUFAs are n- 6 fatty acids.
1,087 citations
TL;DR: expression analysis by quantitative reverse transcription-PCR showed that GPR40 was specifically expressed in brain and Pancreas, with expression in rodent pancreas being localized to insulin-producing β-cells.
1,043 citations