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
Powered by Bioz See more details on Bioz
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: 54413) 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