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Targeting Ffar2 (GPR43) and Ffar3 (GPR441) and down-regulating NF-?B, this patent covers the company's first major drug, SFA001, and provides a way of treating patients afflicted with hepatitis B.
Neyrinck et al., "Inulin-type fructans with prebiotic properties counteract GPR43 over-expression and PPARy-related adipogenesis in the white adipose tissue of high-fat diet-fed mice," Journal of Nutritional Biochemistry, vol.
In the last decades, several G-protein coupled receptors (GPCRs), i.e., GPR40, GPR41, GPR43, GPR84, and GPR120, were deorphaned as free fatty acids (FFAs) receptors [1-5].
It has been elucidated that SCFAs activate GPR41 and GPR43 and thus regulate the secretion of enteroendocrine peptides [61-63].
Noteworthily, as recently reviewed , inconsistent results have been obtained in studies with GPR43 deletion in mice, which precludes a full appreciation of the role of these receptors in chronic inflammatory conditions.
Regulation of inflammatory responses by gut microbiota and chemoattractant receptor GPR43. Nature 2009; 461:1282-6.
Known as two formerly orphan G protein-coupled receptors, GPR41 is found in a wide range of tissues including neutrophils, while GPR43 is shown to be highly expressed in immune cells .
Ng et al., "Regulation of inflammatory responses by gut microbiota and chemoattractant receptor GPR43," Nature, vol.
Two G-protein-coupled receptors identified as receptors for SCFA are free fatty acid receptor 2 (FFA2) and FFA3, also known as GPR43 and GPR41, respectively.
Kimura et al., "Short-chain fatty acids, GPR41 and GPR43 ligands, inhibit TNF-[alpha]-induced MCP-1 expression by modulating p38 and JNK signaling pathways in human renal cortical epithelial cells," Biochemical and Biophysical Research Communications, vol.
Vieira et al., "Metabolite-sensing receptors GPR43 and GPR109A facilitate dietary fibre-induced gut homeostasis through regulation of the inflammasome," Nature Communications, vol.
Inulin-type fructans with prebiotic properties counteract GPR43 overexpression and PPARy-related adipogenesis in the white adipose tissue of high-fat diet-fed mice.
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