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Dual activity lysophosphatidic acid receptor pan-antagonist/autotaxin inhibitor reduces breast cancer cell migration in vitro and causes tumor regression in vivo.
Zhang H, Xu X, Gajewiak J, Tsukahara R, Fujiwara Y, Liu J, Fells JI, Perygin D, Parrill AL, Tigyi G, Prestwich GD. Zhang H, et al. Among authors: liu j. Cancer Res. 2009 Jul 1;69(13):5441-9. doi: 10.1158/0008-5472.CAN-09-0302. Epub 2009 Jun 9. Cancer Res. 2009. PMID: 19509223 Free PMC article.
Identification of non-lipid LPA3 antagonists by virtual screening.
Fells JI, Tsukahara R, Fujiwara Y, Liu J, Perygin DH, Osborne DA, Tigyi G, Parrill AL. Fells JI, et al. Among authors: liu j. Bioorg Med Chem. 2008 Jun 1;16(11):6207-17. doi: 10.1016/j.bmc.2008.04.035. Epub 2008 Apr 18. Bioorg Med Chem. 2008. PMID: 18467108 Free PMC article.
Structure-based drug design identifies novel LPA3 antagonists.
Fells JI, Tsukahara R, Liu J, Tigyi G, Parrill AL. Fells JI, et al. Among authors: liu j. Bioorg Med Chem. 2009 Nov 1;17(21):7457-64. doi: 10.1016/j.bmc.2009.09.022. Epub 2009 Sep 18. Bioorg Med Chem. 2009. PMID: 19800804 Free PMC article.
2D binary QSAR modeling of LPA3 receptor antagonism.
Fells JI, Tsukahara R, Liu J, Tigyi G, Parrill AL. Fells JI, et al. Among authors: liu j. J Mol Graph Model. 2010 Jun;28(8):828-33. doi: 10.1016/j.jmgm.2010.03.002. Epub 2010 Mar 7. J Mol Graph Model. 2010. PMID: 20356772 Free PMC article.
Benzyl and naphthalene methylphosphonic acid inhibitors of autotaxin with anti-invasive and anti-metastatic activity.
Gupte R, Patil R, Liu J, Wang Y, Lee SC, Fujiwara Y, Fells J, Bolen AL, Emmons-Thompson K, Yates CR, Siddam A, Panupinthu N, Pham TC, Baker DL, Parrill AL, Mills GB, Tigyi G, Miller DD. Gupte R, et al. Among authors: liu j. ChemMedChem. 2011 May 2;6(5):922-35. doi: 10.1002/cmdc.201000425. Epub 2011 Apr 4. ChemMedChem. 2011. PMID: 21465666 Free PMC article.
Controlling cancer through the autotaxin-lysophosphatidic acid receptor axis.
Gotoh M, Fujiwara Y, Yue J, Liu J, Lee S, Fells J, Uchiyama A, Murakami-Murofushi K, Kennel S, Wall J, Patil R, Gupte R, Balazs L, Miller DD, Tigyi GJ. Gotoh M, et al. Among authors: liu j. Biochem Soc Trans. 2012 Feb;40(1):31-6. doi: 10.1042/BST20110608. Biochem Soc Trans. 2012. PMID: 22260662 Free PMC article. Review.
Autotaxin and LPA1 and LPA5 receptors exert disparate functions in tumor cells versus the host tissue microenvironment in melanoma invasion and metastasis.
Lee SC, Fujiwara Y, Liu J, Yue J, Shimizu Y, Norman DD, Wang Y, Tsukahara R, Szabo E, Patil R, Banerjee S, Miller DD, Balazs L, Ghosh MC, Waters CM, Oravecz T, Tigyi GJ. Lee SC, et al. Among authors: liu j. Mol Cancer Res. 2015 Jan;13(1):174-85. doi: 10.1158/1541-7786.MCR-14-0263. Epub 2014 Aug 26. Mol Cancer Res. 2015. PMID: 25158955 Free PMC article.
(S)-FTY720-vinylphosphonate, an analogue of the immunosuppressive agent FTY720, is a pan-antagonist of sphingosine 1-phosphate GPCR signaling and inhibits autotaxin activity.
Valentine WJ, Kiss GN, Liu J, E S, Gotoh M, Murakami-Murofushi K, Pham TC, Baker DL, Parrill AL, Lu X, Sun C, Bittman R, Pyne NJ, Tigyi G. Valentine WJ, et al. Among authors: liu j. Cell Signal. 2010 Oct;22(10):1543-53. doi: 10.1016/j.cellsig.2010.05.023. Epub 2010 Jun 4. Cell Signal. 2010. PMID: 20566326 Free PMC article.
Hits of a high-throughput screen identify the hydrophobic pocket of autotaxin/lysophospholipase D as an inhibitory surface.
Fells JI, Lee SC, Fujiwara Y, Norman DD, Lim KG, Tsukahara R, Liu J, Patil R, Miller DD, Kirby RJ, Nelson S, Seibel W, Papoian R, Parrill AL, Baker DL, Bittman R, Tigyi G. Fells JI, et al. Among authors: liu j. Mol Pharmacol. 2013 Sep;84(3):415-24. doi: 10.1124/mol.113.087080. Epub 2013 Jun 21. Mol Pharmacol. 2013. PMID: 23793291 Free PMC article.
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