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• W2048930008 abstract "G-protein coupled receptors (GPCRs) are targets of approximately 30% of currently marketed drugs. Over the last few years, a number of GPCRs expressed in pancreatic beta-cells and activated by lipids have been discovered. GPR40 was shown to be activated by medium- to long-chain fatty acids (FAs). It has since been shown that GPR40 contributes to FA amplification of glucose-induced insulin secretion. Although some controversy still exists as to whether GPR40 agonists or antagonists should be designed as novel type 2 diabetes drugs, data obtained in our laboratory and others strongly suggest that GPR40 agonism might represent a valuable therapeutic approach. GPR119 is expressed in pancreatic beta-cells and enteroendocrine L-cells, and augments circulating insulin levels both through its direct insulinotropic action on beta-cells and through FA stimulation of glucagon-like peptide 1 (GLP-1) secretion. GPR120 is expressed in L-cells and was also shown to mediate FA-stimulated GLP-1 release. Finally, GPR41 and GPR43 are receptors for short-chain FAs and may indirectly regulate beta-cell function via adipokine secretion. Although the discovery of these various lipid receptors opens new and exciting avenues of research for drug development, a number of questions regarding their mechanisms of action and physiological roles remain to be answered." @default.
• W2048930008 created "2016-06-24" @default.
• W2048930008 creator A5011642018 @default.
• W2048930008 creator A5014614398 @default.
• W2048930008 creator A5053617026 @default.
• W2048930008 creator A5084955564 @default.
• W2048930008 date "2009-10-07" @default.
• W2048930008 modified "2023-10-15" @default.
• W2048930008 title "Lipid receptors and islet function: therapeutic implications?" @default.
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• W2048930008 doi "https://doi.org/10.1111/j.1463-1326.2009.01114.x" @default.
• W2048930008 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/2889915" @default.
• W2048930008 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/19817784" @default.
• W2048930008 hasPublicationYear "2009" @default.
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