Oxoglutarate receptor 1 (OXGR1)

Oxoglutarate receptor 1 (OXGR1) is a G protein-coupled receptor (GPCR) primarily activated by alpha-ketoglutarate, itaconate, and cysteinyl leukotrienes (notably leukotriene E4)[1][3]. It couples to Gq/11 pathways to regulate intracellular calcium and downstream responses. OXGR1 plays roles in diverse physiological processes including immune signaling, mucin secretion in airways, kidney ion homeostasis, energy metabolism, and adrenal-driven muscle hypertrophy[2]. It is expressed in the kidney, placenta, fetal brain, certain immune cells, and various mucosal tissues[1]. Deficiency or mutation of the OXGR1 gene in humans and mice is associated with middle ear inflammation, reduced goblet cell numbers, kidney stone formation, metabolic alterations, and possibly tumor suppression[1][2][3]. Montelukast, a leukotriene receptor antagonist, also blocks OXGR1 activity, supporting its pharmacological relevance, particularly in asthma and allergic disease management[1][3]. OXGR1 has emerging roles in cardiovascular regulation, cancer pathogenesis, and obesity[2].

Other names

2-oxoglutarate receptor 1GPR80GPR99P2Y purinoceptor 15P2Y-like GPCRP2Y-like nucleotide receptoralpha-ketoglutarate receptor 1aKGRCAON2cysteinyl leukotriene receptor E (CysLTE)cysteinyl leukotriene receptor 3 (CysLT3)P2RY15P2Y15

Montelukast antagonizes OXGR1 by blocking ligand binding (including LTE4, LTC4, LTD4, alpha-ketoglutarate, and itaconate), thereby inhibiting receptor-mediated cell signaling[1].