Lysophosphatidic acid (LPA; 1-acyl-3-phosphoglycerol) exerts its biological activity through both extracellular and intracellular targets. Receptor targets include the cell-surface G-protein-coupled receptors LPA1–4 and the nuclear PPAR-γ (peroxisome-proliferator-activated receptor γ). Enzyme targets include the secreted cancer cell motility factor, autotaxin, and the transmembrane phosphatases, LPP1–3 (where LPP stands for lipid phosphate phosphatase). Ion channel targets include the two pore domain ion channels in the TREK family, TREK-1, TREK-2 and TRAAK. Structural features of these targets and their interactions with LPA are reviewed.

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