BrP-LPA

BrP-LPA, aka LPA bromophosphonate, acts as both an Autotaxin inhibitor (94% inhibition at 10 μM) and pan LPA receptor antagonist (LPA₁: 1.5 μM, LPA₂: 1.4 μM, LPA₃: 1.2 μM, LPA₄: 0.27 μM). BrP-LPA inhibits the invasiveness of NIH3T3 ras ATX cells by 40% and decreases chemotaxis by 23%. BrP-LPA reduces the size of breast (MDA-MB-231), colon (HCT-116) and melanoma (B16F10) tumors in mouse models. It also attenuates collagen-induced arthritis PPARγ is not activated by BrP-LPA.

Publications

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1) Jiang, G., Y. Xu, et al. (2007). “Alpha-substituted phosphonate analogues of lysophosphatidic acid (LPA) selectively inhibit production and action of LPA.” ChemMedChem 2(5): 679-90.
2) Zhang, H., X. Xu, et al. (2009). “Dual Activity Lysophosphatidic Acid Receptor Pan-Antagonist/Autotaxin Inhibitor Reduces Breast Cancer Cell Migration In vitro and Causes Tumor Regression In vivo.” Cancer Res 69: 5441
3) Schleicher, S. M., D. K. Thotala, et al. (2011). “Autotaxin and LPA Receptors Represent Potential Molecular Targets for the Radiosensitization of Murine Glioma through Effects on Tumor Vasculature.” PLoS ONE 6(7): e22182.
4) Nikitopoulou, I., E. Kaffe, et al. (2013). “A Metabolically-Stabilized Phosphonate Analog of Lysophosphatidic Acid Attenuates Collagen-Induced Arthritis.” PLoS ONE 8(7): e70941