GPR116
GPR116 (also known as Adhesion G Protein-Coupled Receptor G1, ADGRG1) is a protein that in humans is encoded by the ADGRG1 gene. This gene is a member of the adhesion GPCR family, which is characterized by an extended extracellular region with a variety of domain structures, followed by a GPCR proteolysis site (GPS), and a seven-transmembrane domain. GPR116 has been implicated in several physiological and pathological processes, including the regulation of pulmonary surfactant homeostasis, which is critical for lung function and respiratory health.
Function
GPR116 is an adhesion G protein-coupled receptor (aGPCR) that plays a significant role in maintaining pulmonary surfactant homeostasis. Pulmonary surfactant is a complex mixture of lipids and proteins that reduces surface tension in the lungs, preventing lung collapse and promoting efficient gas exchange. GPR116 is expressed predominantly in the lung epithelium, particularly in alveolar type II cells, which are responsible for surfactant production. The exact mechanism by which GPR116 regulates surfactant homeostasis is not fully understood, but it is believed to involve the receptor's ability to mediate cell signaling in response to extracellular cues.
Clinical Significance
Alterations in GPR116 function or expression have been associated with various lung diseases, including pulmonary fibrosis, chronic obstructive pulmonary disease (COPD), and asthma. Given its role in surfactant homeostasis, GPR116 is considered a potential therapeutic target for treating these conditions. Research is ongoing to develop drugs that can modulate GPR116 activity to restore normal lung function in affected individuals.
Genetics
The ADGRG1 gene encoding GPR116 is located on human chromosome 6. Variants within or near this gene have been studied in the context of their potential association with lung function and susceptibility to respiratory diseases. Understanding the genetic regulation of GPR116 expression and function may provide insights into the pathogenesis of lung diseases and guide the development of personalized medicine approaches for their treatment.
Research Directions
Future research on GPR116 is likely to focus on elucidating the detailed mechanisms of its action in lung tissue, its interactions with other components of the surfactant system, and its role in lung development and repair. Additionally, studies are needed to explore the therapeutic potential of targeting GPR116 in various lung diseases, including the identification of small molecules or antibodies that can specifically modulate its activity.
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Contributors: Prab R. Tumpati, MD