Abstract
Medium- and long-chain free fatty acids (FFAs) are energy source for whole body and biological metabolites and components. In these decades, some research groups have reported that the biological functions of medium- to long-chain FFAs are exerted through G-protein coupled receptor designated free fatty acid receptor (FFAR). As the medium- to long-chain FFAs-activated FFARs, FFA1 and FFA4 are reported to be expressed widely in whole body and regulate various physiological processes. FFA1 expressed in pancreatic β-cells has been shown to be involved in insulin secretion. FFA4 expressed in intestine, adipocytes, and macrophages has been shown to be involved in incretin secretion, differentiation, and anti-inflammatory effect, respectively. These physiological functions have been focused on the treatment of metabolic disorders. In addition, these receptors have been also reported to be expressed in several other tissues such as intestine for FFA1, and tongue and stomach for FFA4. The recent functional studies indicated that they also contributed to energy homeostasis. Further, the number of synthetic compounds of FFA1 and FFA4 strongly promoted the physiological characterization of the receptors and their own therapeutic utility. In this article, we will discuss the recent progress regarding the therapeutic potential of these receptors and its ligands.
Highlights
Free fatty acids (FFAs) are known to act as the critical energy source in the whole body
As one of these mechanisms, G-protein-coupled receptors (GPCRs) activated by FFAs designated as free fatty acid receptor (FFAR) family have played important role especially in energy metabolism [3]
A number of studies for FFA1 and FFA4 revealed that these two receptors have been contributed to regulate energy metabolism and metabolic diseases such as type 2 diabetes and obesity
Summary
Free fatty acids (FFAs) are known to act as the critical energy source in the whole body. FFAs act as signal molecules in various physiological reactions [1, 2] As one of these mechanisms, G-protein-coupled receptors (GPCRs) activated by FFAs designated as free fatty acid receptor (FFAR) family have played important role especially in energy metabolism [3]. THERAPEUTIC POTENTIAL OF FFA1 AND FFA4 PHYSIOLOGICAL FUNCTIONS RELATED TO ENERGY METABOLISM Among FFARs, FFA1 and FFA4 are classified as medium- to longchain FFARs. The ligand property of these two receptors was FFA4 Free fatty acid 4 expressed in intestine, adipose tissue, and taste buds is considered as therapeutic target for metabolic disorders. Since the FFA stimulation of these cells activated taste nerve response, fat preferences might be regulated via FFA4 These findings provided us the possibility for the therapeutic utility of FFA1 and FFA4
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