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Sphingosine kinase activity is not required for tumor cell viability.
Rex K, Jeffries S, Brown ML, Carlson T, Coxon A, Fajardo F, Frank B, Gustin D, Kamb A, Kassner PD, Li S, Li Y, Morgenstern K, Plant M, Quon K, Ruefli-Brasse A, Schmidt J, Swearingen E, Walker N, Wang Z, Watson JE, Wickramasinghe D, Wong M, Xu G, Wesche H. Rex K, et al. Among authors: xu g. PLoS One. 2013 Jul 5;8(7):e68328. doi: 10.1371/journal.pone.0068328. Print 2013. PLoS One. 2013. PMID: 23861887 Free PMC article.
Structure guided design of a series of sphingosine kinase (SphK) inhibitors.
Gustin DJ, Li Y, Brown ML, Min X, Schmitt MJ, Wanska M, Wang X, Connors R, Johnstone S, Cardozo M, Cheng AC, Jeffries S, Franks B, Li S, Shen S, Wong M, Wesche H, Xu G, Carlson TJ, Plant M, Morgenstern K, Rex K, Schmitt J, Coxon A, Walker N, Kayser F, Wang Z. Gustin DJ, et al. Among authors: xu g. Bioorg Med Chem Lett. 2013 Aug 15;23(16):4608-16. doi: 10.1016/j.bmcl.2013.06.030. Epub 2013 Jun 20. Bioorg Med Chem Lett. 2013. PMID: 23845219
Identification of potent, noncovalent fatty acid amide hydrolase (FAAH) inhibitors.
Gustin DJ, Ma Z, Min X, Li Y, Hedberg C, Guimaraes C, Porter AC, Lindstrom M, Lester-Zeiner D, Xu G, Carlson TJ, Xiao S, Meleza C, Connors R, Wang Z, Kayser F. Gustin DJ, et al. Among authors: xu g. Bioorg Med Chem Lett. 2011 Apr 15;21(8):2492-6. doi: 10.1016/j.bmcl.2011.02.052. Epub 2011 Feb 17. Bioorg Med Chem Lett. 2011. PMID: 21392988
Discovery of amide replacements that improve activity and metabolic stability of a bis-amide smoothened antagonist hit.
Brown ML, Aaron W, Austin RJ, Chong A, Huang T, Jiang B, Kaizerman JA, Lee G, Lucas BS, McMinn DL, Orf J, Rong M, Toteva MM, Xu G, Ye Q, Zhong W, Degraffenreid MR, Wickramasinghe D, Powers JP, Hungate R, Johnson MG. Brown ML, et al. Among authors: xu g. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5206-9. doi: 10.1016/j.bmcl.2011.07.052. Epub 2011 Jul 23. Bioorg Med Chem Lett. 2011. PMID: 21840217
Design of 1-piperazinyl-4-arylphthalazines as potent Smoothened antagonists.
Lucas BS, Aaron W, An S, Austin RJ, Brown M, Chan H, Chong A, Hungate R, Huang T, Jiang B, Johnson MG, Kaizerman JA, Lee G, McMinn DL, Orf J, Powers JP, Rong M, Toteva MM, Uyeda C, Wickramasinghe D, Xu G, Ye Q, Zhong W. Lucas BS, et al. Among authors: xu g. Bioorg Med Chem Lett. 2010 Jun 15;20(12):3618-22. doi: 10.1016/j.bmcl.2010.04.110. Epub 2010 Apr 28. Bioorg Med Chem Lett. 2010. PMID: 20493695
Identification and characterization of a non-retinoid ligand for retinol-binding protein 4 which lowers serum retinol-binding protein 4 levels in vivo.
Motani A, Wang Z, Conn M, Siegler K, Zhang Y, Liu Q, Johnstone S, Xu H, Thibault S, Wang Y, Fan P, Connors R, Le H, Xu G, Walker N, Shan B, Coward P. Motani A, et al. Among authors: xu g, xu h. J Biol Chem. 2009 Mar 20;284(12):7673-80. doi: 10.1074/jbc.M809654200. Epub 2009 Jan 15. J Biol Chem. 2009. PMID: 19147488 Free PMC article.
Addressing PXR liabilities of phthalazine-based hedgehog/smoothened antagonists using novel pyridopyridazines.
Kaizerman JA, Aaron W, An S, Austin R, Brown M, Chong A, Huang T, Hungate R, Jiang B, Johnson MG, Lee G, Lucas BS, Orf J, Rong M, Toteva MM, Wickramasinghe D, Xu G, Ye Q, Zhong W, McMinn DL. Kaizerman JA, et al. Among authors: xu g. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4607-10. doi: 10.1016/j.bmcl.2010.06.006. Epub 2010 Jun 8. Bioorg Med Chem Lett. 2010. PMID: 20594845
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