AH-7614, FFA4/GPR120 antagonist

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The G-protein coupled receptor GPR120 also known as free fatty acid receptor 4 (FFA4) is a receptor with a molecular mass of approximately 42 kDa. It is expressed widely in human adipose tissue intestine and pancreas. This receptor acts as a sensor for long-chain fatty acids especially omega-3. It is integral in responding to dietary fats and influences several downstream signaling mechanisms.

Biological function summary

The GPR120 receptor plays a significant role in metabolic regulation and inflammation control. It is not part of a larger protein complex but functions as a solo receptor. Its activation can lead to anti-inflammatory effects and improved insulin sensitivity contributing to the homeostasis of glucose and lipid metabolism. GPR120 engagement by its ligands initiates a cascade of cellular responses emphasizing its importance in metabolic pathways.

Pathways

Four major ways exist through which GPR120 operates to influence metabolic health. It is involved in the insulin-sensitizing pathway and the anti-inflammatory pathway. When activated GPR120 couples with Gαq/11 proteins to initiate intracellular signaling influencing downstream proteins such as Akt and ERK1/2. This linkage is important for its role in reducing inflammation and improving insulin sensitivity aligning with other receptors like GPR40 which similarly respond to fatty acids.

GPR120 has implications in type 2 diabetes and non-alcoholic fatty liver disease (NAFLD). Dysregulation of GPR120 signaling is associated with reduced insulin response highlighting its connection to diabetes. Similarly in NAFLD improper function or expression of GPR120 leads to fat accumulation in liver cells. It is linked to inflammatory proteins like TNF-alpha where altered GPR120 activity modulates TNF-alpha levels influencing inflammation and metabolic imbalance.