Biological Activity
tetradecyl phosphonate is a pan-antagonist of lysophosphatidic acid 1 (lpa1), lpa2, and lpa3 receptors. the ic50 value for inhibition of lpa-induced calcium mobilization was 10 μm, 5.5 μm, and 3.1 μm, respectively. at a concentration of 10 μm, tetradecyl phosphonate activates a peroxisome proliferator-activated receptor γ reporter construct 4-fold when compared with the controls and partially inhibits autotaxin with an ic50 value of approximately 3 μm [1].lysophosphatidic acid (lpa), also known as autotaxin (atx), is a lipid signalling molecule formed by the hydrolysis of lysophosphatidyl choline by lysophospholipase d [2]. lpa signals through four different g protein-coupled receptors, named as lpa1/edg-2, lpa2/edg-4, lpa3/edg-7, and lpa4/gpr23 [3]. it has been reported that lpa was involved in activating peroxisome proliferator-activated receptor γ (pparγ) [4].
References
[1]. durgam g g, virag t, walker m d, et al. synthesis, structure activity relationships, and biological evaluation of fatty alcohol phosphates as lysophosphatidic acid receptor ligands, activators of pparγ, and inhibitors of autotaxin[j]. journal of medicinal chemistry, 2005, 48(15): 4919-4930.
[2]. tokumura a, majima e, kariya y, et al. identification of human plasma lysophospholipase d, a lysophosphatidic acid-producing enzyme, as autotaxin, a multifunctional phosphodiesterase[j]. journal of biological chemistry, 2002, 277(42): 39436-39442.
[3]. noguchi k, ishii s, shimizu t. identification of p2y9/gpr23 as a novel g protein-coupled receptor for lysophosphatidic acid, structurally distant from the edg family[j]. journal of biological chemistry, 2003, 278(28): 25600-25606.
[4]. mcintyre t m, pontsler a v, silva a r, et al. identification of an intracellular receptor for lysophosphatidic acid (lpa): lpa is a transcellular pparγ agonist[j]. proceedings of the national academy of sciences, 2003, 100(1): 131-136.
