Oxoglutarate receptor 1 (OXGR1) (OXGR1)

Oxoglutarate receptor 1 (OXGR1), also known as GPR99, is a G protein-coupled receptor that serves as a high-affinity receptor for the inflammatory mediator leukotriene E4 (LTE4) and a lower-affinity receptor for the citric acid cycle intermediate alpha-ketoglutarate (AKG). It is primarily expressed in the kidney, respiratory epithelium, adrenal glands, and heart, where it mediates diverse physiological processes including acid-base homeostasis, mucociliary clearance, and exercise-induced muscle hypertrophy. In the kidney, OXGR1 activation by AKG regulates bicarbonate secretion and salt reabsorption, while in the adrenal glands, it triggers adrenaline release in response to exercise-induced AKG. OXGR1 is implicated in various diseases, acting as a mediator of allergic inflammation in asthma and rhinitis, a potential tumor suppressor in hepatocellular carcinoma, and a modulator of cardiac hypertrophy in heart failure. Therapeutic interest in OXGR1 focuses on its role in inflammatory airway diseases and metabolic regulation, with drugs like montelukast potentially interacting with its leukotriene-mediated signaling.

Other names

GPR99GPR80P2RY15Alpha-ketoglutarate receptor 12-oxoglutarate receptor 1CysLT3CysLTE2-oxoglutarate

Activation of Gq-mediated signaling pathways, leading to intracellular calcium release and downstream signaling; antagonism of leukotriene-mediated signaling to treat inflammatory disorders.