Lysophosphatidic acid receptor 2 (LPA2) (LPA2)

Lysophosphatidic acid receptor 2 (LPA2), also known as LPAR2 or EDG4, is a G protein-coupled receptor that belongs to the endothelial differentiation gene (Edg) family. It is primarily activated by the bioactive lipid lysophosphatidic acid (LPA) and signals through Gi, Gq, and G12/13 proteins to regulate diverse cellular processes such as proliferation, survival, migration, and DNA damage repair (UniProt, 2022; IUPHAR, 2026). LPA2 is notably overexpressed in several malignancies, including ovarian, colorectal, and pancreatic cancers, where it promotes tumor progression, metastasis, and chemoresistance (Journal of Cancer, 2020; PMC, 2012). Conversely, its pro-survival and anti-apoptotic roles make it a target for radioprotection and the treatment of secretory diarrhea, where agonists like Rx100 have shown efficacy in mitigating radiation-induced injury and electrolyte loss (ResearchGate, 2018; SBIR, 2019). In inflammatory and fibrotic conditions, such as asthma and spinal cord injury, LPA2 antagonism is being explored to reduce pathological signaling and promote tissue recovery (MDPI, 2022; PMC, 2022). The dual nature of LPA2 as both a driver of cancer and a protector of normal tissue presents a complex therapeutic landscape, requiring highly selective modulators to balance efficacy and safety (Journal of Lipid Research, 2019).

Other names

EDG4EDG-4LPAR2LPA-2Lysophosphatidic acid receptor Edg-4

Agonist, Antagonist