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Free fatty acid receptors as therapeutic targets for the treatment of diabetes.

Ichimura A, Hasegawa S, Kasubuchi M, Kimura I - Front Pharmacol (2014)

Bottom Line: Fatty acids are an essential energy source and signaling molecules that regulate various cellular processes and physiological functions.Recently, several orphan G protein-coupled receptors were identified as free fatty acid receptors (FFARs).GPR40/FFAR1 and GPR120/FFAR4 are activated by medium- and/or long-chain fatty acids, whereas GPR41/FFAR3 and GPR43/FFAR2 are activated by short-chain fatty acids.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmacogenomics, Kyoto University Graduate School of Pharmaceutical Science , Kyoto, Japan ; Department of Molecular Medicine and Therapy, Tohoku University Graduate School of Medicine , Sendai, Miyagi, Japan.

ABSTRACT
Nutrition regulates energy balance; however, dysfunction of energy balance can cause metabolic disorders, such as obesity and diabetes. Fatty acids are an essential energy source and signaling molecules that regulate various cellular processes and physiological functions. Recently, several orphan G protein-coupled receptors were identified as free fatty acid receptors (FFARs). GPR40/FFAR1 and GPR120/FFAR4 are activated by medium- and/or long-chain fatty acids, whereas GPR41/FFAR3 and GPR43/FFAR2 are activated by short-chain fatty acids. FFARs are regarded as targets for novel drugs to treat metabolic disorders, such as obesity and type 2 diabetes, because recent studies have showed that these receptors are involved in the energy metabolism in various tissues, including adipose, intestinal, and immune tissue. In this review, we summarize physiological roles of the FFARs, provide a comprehensive overview of energy regulation by FFARs, and discuss new prospects for treatment of metabolic disorders.

No MeSH data available.


Related in: MedlinePlus

Physiological functions of free fatty acid receptors (FFARs). Medium- and long-chain fatty acids derived from dietary fat act as ligands for FFAR1 or FFAR4 (I). Short-chain fatty acids produced by gut microbes from indigestible dietary fiber act as ligands for FFAR3 or FFAR2 (II).
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Figure 2: Physiological functions of free fatty acid receptors (FFARs). Medium- and long-chain fatty acids derived from dietary fat act as ligands for FFAR1 or FFAR4 (I). Short-chain fatty acids produced by gut microbes from indigestible dietary fiber act as ligands for FFAR3 or FFAR2 (II).

Mentions: In recent years, many metabolic and immune response pathways have been reported in relation to nutrient sensing systems. Several studies have provided evidence that FFARs are dietary sensors expressed in both metabolic tissues and immune cells that regulate both energy metabolism and inflammatory responses. These investigations will lead to new insights in nutritional science and drug discovery science, due to the importance of FFA signaling in diverse metabolic process (Figure 2). Since the inflammatory response is also related to the development of obesity and type 2 diabetes, the FFAR family is expected to be a potential therapeutic target for the treatment of these diseases. Although the detailed signaling mechanism and physiological functions of FFARs in tissues are unclear, a further understanding of the regulation of energy metabolism and inflammatory responses by the FFAR family represents an important avenue of research in drug development for the treatment of obesity and type 2 diabetes.


Free fatty acid receptors as therapeutic targets for the treatment of diabetes.

Ichimura A, Hasegawa S, Kasubuchi M, Kimura I - Front Pharmacol (2014)

Physiological functions of free fatty acid receptors (FFARs). Medium- and long-chain fatty acids derived from dietary fat act as ligands for FFAR1 or FFAR4 (I). Short-chain fatty acids produced by gut microbes from indigestible dietary fiber act as ligands for FFAR3 or FFAR2 (II).
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4222138&req=5

Figure 2: Physiological functions of free fatty acid receptors (FFARs). Medium- and long-chain fatty acids derived from dietary fat act as ligands for FFAR1 or FFAR4 (I). Short-chain fatty acids produced by gut microbes from indigestible dietary fiber act as ligands for FFAR3 or FFAR2 (II).
Mentions: In recent years, many metabolic and immune response pathways have been reported in relation to nutrient sensing systems. Several studies have provided evidence that FFARs are dietary sensors expressed in both metabolic tissues and immune cells that regulate both energy metabolism and inflammatory responses. These investigations will lead to new insights in nutritional science and drug discovery science, due to the importance of FFA signaling in diverse metabolic process (Figure 2). Since the inflammatory response is also related to the development of obesity and type 2 diabetes, the FFAR family is expected to be a potential therapeutic target for the treatment of these diseases. Although the detailed signaling mechanism and physiological functions of FFARs in tissues are unclear, a further understanding of the regulation of energy metabolism and inflammatory responses by the FFAR family represents an important avenue of research in drug development for the treatment of obesity and type 2 diabetes.

Bottom Line: Fatty acids are an essential energy source and signaling molecules that regulate various cellular processes and physiological functions.Recently, several orphan G protein-coupled receptors were identified as free fatty acid receptors (FFARs).GPR40/FFAR1 and GPR120/FFAR4 are activated by medium- and/or long-chain fatty acids, whereas GPR41/FFAR3 and GPR43/FFAR2 are activated by short-chain fatty acids.

View Article: PubMed Central - PubMed

Affiliation: Department of Pharmacogenomics, Kyoto University Graduate School of Pharmaceutical Science , Kyoto, Japan ; Department of Molecular Medicine and Therapy, Tohoku University Graduate School of Medicine , Sendai, Miyagi, Japan.

ABSTRACT
Nutrition regulates energy balance; however, dysfunction of energy balance can cause metabolic disorders, such as obesity and diabetes. Fatty acids are an essential energy source and signaling molecules that regulate various cellular processes and physiological functions. Recently, several orphan G protein-coupled receptors were identified as free fatty acid receptors (FFARs). GPR40/FFAR1 and GPR120/FFAR4 are activated by medium- and/or long-chain fatty acids, whereas GPR41/FFAR3 and GPR43/FFAR2 are activated by short-chain fatty acids. FFARs are regarded as targets for novel drugs to treat metabolic disorders, such as obesity and type 2 diabetes, because recent studies have showed that these receptors are involved in the energy metabolism in various tissues, including adipose, intestinal, and immune tissue. In this review, we summarize physiological roles of the FFARs, provide a comprehensive overview of energy regulation by FFARs, and discuss new prospects for treatment of metabolic disorders.

No MeSH data available.


Related in: MedlinePlus