Lysophosphatidic acid receptor 1 (LPAR1) (LPAR1)

Lysophosphatidic acid receptor 1 (LPAR1), also known as EDG2, is a Class A G protein-coupled receptor that mediates the effects of the bioactive lipid lysophosphatidic acid (LPA) [1, 12]. In mice, Lpar1 is widely expressed and plays critical roles in diverse physiological processes, including neurogenesis, bone development, and the regulation of the actin cytoskeleton [1, 8, 9]. It couples to multiple G proteins, including Gi/o, Gq, and G12/13, to trigger signaling pathways that promote cell proliferation, migration, and survival [1, 15]. Pathologically, LPAR1 is a major driver of fibrotic diseases, such as idiopathic pulmonary fibrosis and systemic sclerosis, by promoting fibroblast recruitment and activation [2, 13, 15]. It is also implicated in cancer progression, where it facilitates tumor cell invasion and metastasis, and in the development of neuropathic pain [4, 7, 18]. Consequently, LPAR1 has become a significant therapeutic target, with several small-molecule antagonists currently in clinical development for fibrotic and inflammatory conditions [4, 14, 17].

Other names

LPA1EDG2VZG1Gpcr26Rec1.3Endothelial differentiation gene 2LPA receptor 1

Antagonist