GPR81

GPR81 is a gene that encodes the G protein-coupled receptor 81 in humans. This receptor is also known as hydroxycarboxylic acid receptor 1 (HCA1) and is primarily recognized for its role in metabolic regulation and energy homeostasis. GPR81 is a part of the G protein-coupled receptor (GPCR) family, which is a large protein family of receptors that detect molecules outside the cell and activate internal signal transduction pathways and, ultimately, cellular responses.

Function[edit | edit source]

GPR81 is activated by lactate, a byproduct of anaerobic metabolism, suggesting its involvement in the regulation of energy balance and metabolism. Upon activation by lactate, GPR81 inhibits the cyclic AMP (cAMP) production, leading to a decrease in lipolysis in adipose tissue. This suggests that GPR81 plays a significant role in the regulation of lipid metabolism and energy homeostasis. The receptor is predominantly expressed in adipose tissue but can also be found in other tissues, including the brain, where its function is not fully understood.

Clinical Significance[edit | edit source]

The role of GPR81 in metabolic regulation suggests its potential as a therapeutic target for metabolic disorders such as obesity and type 2 diabetes. By modulating GPR81 activity, it may be possible to influence lipid metabolism and improve metabolic health. Research into GPR81 agonists and antagonists is ongoing, with the aim of developing new treatments for metabolic diseases.

Research[edit | edit source]

Research on GPR81 has expanded our understanding of metabolic regulation and the role of lactate in energy homeostasis. Studies have shown that GPR81 activation by lactate can have anti-lipolytic effects, which could be beneficial in the context of metabolic disorders characterized by excessive lipolysis and lipid accumulation. Further research is needed to fully elucidate the physiological and pathological roles of GPR81, including its potential effects in the central nervous system and its role in conditions beyond metabolic disorders.