(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.
Gille et al., "GPR41/FFAR3 and GPR43/FFAR2 as cosensors for short-chain fatty acids in enteroendocrine cells vs FFAR3 in enteric neurons and FFAR2 in enteric leukocytes," Endocrinology, vol.
Lam et al., "Short-chain fatty acids stimulate glucagon-like peptide-1 secretion via the G-protein-coupled receptor FFAR2," Diabetes, vol.
found that SCFA butyrate suppressed colonic stem cell proliferation , perhaps through receptors encoded by Ffar3, Ffar2
, and Niacr1 .
GPR41 (i.e., FFAR3) and GPR43 (i.e., FFAR2
) are both highly expressed on immune cells such as polymorphonuclear cells and macrophages [ 22].
SCFAs can stimulate glucagon-like peptide 1 (GLP-1) secretion via the G-protein-coupled receptor FFAR2
(free fatty acid receptor 2) in the colonic mucosa (44).
Receptors for SCFAs are two Gprotein coupled receptors (GPCRs): FFAR2 (free fatty acid receptor2, previously known as GPR43) and FFAR3 (or GPR41) [37-40].
Deficiency of FFAR2 results in increasing or maintaining inflammation in models of colitis, arthritis, and asthma, related to increased production of inflammatory mediators and increased immune cell recruitment .
Expression of both FFAR2 and FFAR3 was reported in the colon, with particularly strong expression in GLP-1 producing L-cells [42-44, 64].
The poor responsiveness to SCFAs of the GLP1, secreting cell line GLUTag, has been associated with the very low expression of FFAR2 .