Lysophosphatidic acid receptor 3 (LPA3) (LPA3)

The Lysophosphatidic acid receptor 3 (LPA3) is a member of the G protein-coupled receptor (GPCR) superfamily, specifically belonging to the lysophospholipid receptor family [1.3.1, 1.4.1]. It is encoded by the LPAR3 gene and primarily couples with Gαi/o and Gαq/11 proteins to mediate cellular responses to lysophosphatidic acid (LPA), a bioactive lipid [1.1.1, 1.2.4]. LPA3 is uniquely characterized by its preference for 2-acyl LPA with unsaturated fatty acids and its relatively restricted expression in tissues such as the heart, prostate, and reproductive organs [1.1.3, 1.3.5]. Biologically, it plays a critical role in embryo implantation, uterine motility, and cell migration [1.1.3, 1.3.1]. In clinical contexts, LPA3 is highly relevant in oncology, particularly in ovarian cancer, where its overexpression is linked to increased proliferation, metastasis, and poor prognosis [1.2.4, 1.5.2]. It has also been implicated in the progression of breast, lung, and pancreatic cancers [1.2.4, 1.3.1]. Pharmacological targeting of LPA3 involves the development of selective agonists and antagonists, though many current compounds like Ki16425 also target LPA1 [1.5.1, 1.5.2]. Therapeutic challenges include achieving subtype selectivity to avoid adverse effects on reproductive and cardiovascular systems [1.5.1]. Recent research has also explored the interaction of common antidepressants with LPA3, suggesting potential off-target effects or novel therapeutic avenues [1.2.1, 1.2.2].

Other names

EDG7Edg-7LPAR3LP-A3HOFNH30RP4-678I3Lysophosphatidic acid receptor 3

G protein-coupled receptor antagonism and agonism, specifically modulating Gαi/o and Gαq/11 signaling pathways to influence adenylyl cyclase activity and calcium mobilization [1.1.1, 1.2.4, 1.3.1].