One of the overactive genes that helps trigger the inflammation response -- a gene called FFAR3
-- also encodes a receptor for a dietary supplement called butyrate.
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.
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.
Merold et al., "Effects of short chain fatty acid producing bacteria on epigenetic regulation of FFAR3
in type 2 diabetes and obesity," Gene, vol.
Our microarray data revealed that PMNs express a number of cell surface receptors for the recognition of iRBCs, including protein G receptors (P2RY4, GPR88, MRGPRG, FFAR3
, HCAR1, and MRGPRF), adhesion receptors (VIT, CD69), sialic acid (SIGLEC12), Fc receptors (FCGR1a, FCRL1), FLNA, and IL-15RA.
found that SCFA butyrate suppressed colonic stem cell proliferation , perhaps through receptors encoded by Ffar3
, Ffar2, and Niacr1 .
(2014) Effects of short chain fatty acid producing bacteria on epigenetic regulation of FFAR3
in type 2 diabetes and obesity.
Receptors for SCFAs are two Gprotein coupled receptors (GPCRs): FFAR2 (free fatty acid receptor2, previously known as GPR43) and FFAR3 (or GPR41) [37-40].
In particular the promoter region of FFAR3 showed a significantly higher methylation in the lean control group compared to type 2 diabetics and to obese subjects.
GPR41 (i.e., FFAR3
) and GPR43 (i.e., FFAR2) are both highly expressed on immune cells such as polymorphonuclear cells and macrophages [ 22].