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Lysophosphatidic acid (LPA) is a bioactive lipid mediator that signals through five distinct G protein-coupled receptors (LPA1-5).1 Ki16425 is a LPA receptor antagonist with selectivity for LPA1 and LPA3. It exhibits Ki values of 0.34, 6.5, and 0.93 µM for the human LPA1, LPA2, and LPA3 receptors, respectively, as determined by measuring inositol phosphate production in RH7777-transfected cells.2 Ki1642, at 10 µM, significantly blocks the response of a variety of cancer cell lines to LPA-induced cell migration.3
1
Choi, J.W., Lee, C., and Chun, J. Biological roles of lysophospholipid receptors revealed by genetic null mice: An update. Biochim Biophys Acta1781531-539(2008).
2
Ohta, H., Sato, K., Murata, N., et al. Ki16425, a subtype-selective antagonist for EDG-family lysophosphatidic acid receptors. Mol Pharmacol64(4)994-1005(2003).
3
Yamada, T., Sato, K., Komachi, M., et al. Lysophosphatidic acid (LPA) in malignant ascites stimulates motility of human pancreatic cancer cells through LPA. J Biol Chem279(8)6595-6605(2004).
Ohta, H., Sato, K., Murata, N., et al. Ki16425, a subtype-selective antagonist for EDG-family lysophosphatidic acid receptors. Mol Pharmacol64(4)994-1005(2003).
Choi, J.W., Lee, C., and Chun, J. Biological roles of lysophospholipid receptors revealed by genetic null mice: An update. Biochim Biophys Acta1781531-539(2008).
Yamada, T., Sato, K., Komachi, M., et al. Lysophosphatidic acid (LPA) in malignant ascites stimulates motility of human pancreatic cancer cells through LPA. J Biol Chem279(8)6595-6605(2004).
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