Description
Lysophosphatidic acid (LPA) is a potent lipid mediator that elicits its effect through four distinct receptors -
LPA
1/EDG-
2, LPA
2/EDG-
4, LPA
3/EDG-
7 and LPA
4/GPR23.
1,2 OMPT is a selective agonist of the lysophosphatidic acid 3 (LPA
3) receptor. It exhibits EC
50 values of 68 nM and >6.8 μM for calcium mobilization in LPA
1 and LPA
2-
expressing Sf9 cells, respectively.
3 The (2S)-
OMPT enantiomer is 5-
to 20-
fold more active than (2R)-
OMPT in calcium release assays in both LPA
3-
transfected Sf9 and rat hepatoma Rh7777 cells.
4
References
1. Chun, J., Goetzl, E.J., Hla, T., et al. International union of pharmacology. XXXIV. Lysophospholipid receptor nomenclature Pharmacol. Rev. 54,265-269(2002).
2. Niu, S.L., Mitchell, D.C., and Litman, B.J. Trans fatty acid derived phospholipids show increased membrane cholesterol and reduced receptor activation as compared to their cis analogs Biochemistry 44,4458-4465(2005).
3. Hasegawa, Y., Erickson, J.R., Goddard, G.J., et al. Identification of a phosphothionate analogue of lysophosphatidic acid (LPA) as a selective agonist of the LPA3 receptor J. Biol. Chem. 278(14),11962-11969(2003).
4. Qian, L., Xu, Y., Hasegawa, Y., et al. Enantioselective responses to a phosphorothioate analogue of lysophosphatidic acid with LPA3 receptor-selective agonist activity J. Med. Chem. 46,5575-5578(2003).
