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Novel oligoamine analogues inhibit lysine-specific demethylase 1 and induce reexpression of epigenetically silenced genes.

Huang Y, Stewart TM, Wu Y, Baylin SB, Marton LJ, Perkins B, Jones RJ, Woster PM, Casero RA Jr.

Clin Cancer Res. 2009 Dec 1;15(23):7217-28. doi: 10.1158/1078-0432.CCR-09-1293. Epub 2009 Nov 24.


Oligoamine analogues in combination with 2-difluoromethylornithine synergistically induce re-expression of aberrantly silenced tumour-suppressor genes.

Wu Y, Steinbergs N, Murray-Stewart T, Marton LJ, Casero RA.

Biochem J. 2012 Mar 15;442(3):693-701. doi: 10.1042/BJ20111271.


Inhibition of lysine-specific demethylase 1 by polyamine analogues results in reexpression of aberrantly silenced genes.

Huang Y, Greene E, Murray Stewart T, Goodwin AC, Baylin SB, Woster PM, Casero RA Jr.

Proc Natl Acad Sci U S A. 2007 May 8;104(19):8023-8. Epub 2007 Apr 26.


The re-expression of the epigenetically silenced e-cadherin gene by a polyamine analogue lysine-specific demethylase-1 (LSD1) inhibitor in human acute myeloid leukemia cell lines.

Murray-Stewart T, Woster PM, Casero RA Jr.

Amino Acids. 2014 Mar;46(3):585-94. doi: 10.1007/s00726-013-1485-1. Epub 2013 Mar 19.


Synergistic re-activation of epigenetically silenced genes by combinatorial inhibition of DNMTs and LSD1 in cancer cells.

Han H, Yang X, Pandiyan K, Liang G.

PLoS One. 2013 Sep 6;8(9):e75136. doi: 10.1371/journal.pone.0075136. eCollection 2013.


Phosphorylation of histone H3T6 by PKCbeta(I) controls demethylation at histone H3K4.

Metzger E, Imhof A, Patel D, Kahl P, Hoffmeyer K, Friedrichs N, Müller JM, Greschik H, Kirfel J, Ji S, Kunowska N, Beisenherz-Huss C, Günther T, Buettner R, Schüle R.

Nature. 2010 Apr 1;464(7289):792-6. doi: 10.1038/nature08839. Epub 2010 Mar 14.


Polyamine analogues targeting epigenetic gene regulation.

Huang Y, Marton LJ, Woster PM, Casero RA.

Essays Biochem. 2009 Nov 4;46:95-110. doi: 10.1042/bse0460007. Review.


Low molecular weight amidoximes that act as potent inhibitors of lysine-specific demethylase 1.

Hazeldine S, Pachaiyappan B, Steinbergs N, Nowotarski S, Hanson AS, Casero RA Jr, Woster PM.

J Med Chem. 2012 Sep 13;55(17):7378-91. doi: 10.1021/jm3002845. Epub 2012 Sep 4.


(Bis)urea and (bis)thiourea inhibitors of lysine-specific demethylase 1 as epigenetic modulators.

Sharma SK, Wu Y, Steinbergs N, Crowley ML, Hanson AS, Casero RA, Woster PM.

J Med Chem. 2010 Jul 22;53(14):5197-212. doi: 10.1021/jm100217a.


Inhibition of histone demethylase, LSD2 (KDM1B), attenuates DNA methylation and increases sensitivity to DNMT inhibitor-induced apoptosis in breast cancer cells.

Katz TA, Vasilatos SN, Harrington E, Oesterreich S, Davidson NE, Huang Y.

Breast Cancer Res Treat. 2014 Jul;146(1):99-108. doi: 10.1007/s10549-014-3012-9. Epub 2014 Jun 13.


Polyamine analogs modulate gene expression by inhibiting lysine-specific demethylase 1 (LSD1) and altering chromatin structure in human breast cancer cells.

Zhu Q, Huang Y, Marton LJ, Woster PM, Davidson NE, Casero RA Jr.

Amino Acids. 2012 Feb;42(2-3):887-98. doi: 10.1007/s00726-011-1004-1. Epub 2011 Jul 30.


The epigenetic promotion of osteogenic differentiation of human adipose-derived stem cells by the genetic and chemical blockade of histone demethylase LSD1.

Ge W, Liu Y, Chen T, Zhang X, Lv L, Jin C, Jiang Y, Shi L, Zhou Y.

Biomaterials. 2014 Jul;35(23):6015-25. doi: 10.1016/j.biomaterials.2014.04.055. Epub 2014 May 1.


Structure-activity study for (bis)ureidopropyl- and (bis)thioureidopropyldiamine LSD1 inhibitors with 3-5-3 and 3-6-3 carbon backbone architectures.

Nowotarski SL, Pachaiyappan B, Holshouser SL, Kutz CJ, Li Y, Huang Y, Sharma SK, Casero RA Jr, Woster PM.

Bioorg Med Chem. 2015 Apr 1;23(7):1601-12. doi: 10.1016/j.bmc.2015.01.049. Epub 2015 Feb 7.


Inhibitors of histone demethylation and histone deacetylation cooperate in regulating gene expression and inhibiting growth in human breast cancer cells.

Huang Y, Vasilatos SN, Boric L, Shaw PG, Davidson NE.

Breast Cancer Res Treat. 2012 Feb;131(3):777-89. doi: 10.1007/s10549-011-1480-8. Epub 2011 Mar 31.


DNA methylation and histone modifications cause silencing of Wnt antagonist gene in human renal cell carcinoma cell lines.

Kawamoto K, Hirata H, Kikuno N, Tanaka Y, Nakagawa M, Dahiya R.

Int J Cancer. 2008 Aug 1;123(3):535-42. doi: 10.1002/ijc.23514.


A novel selective LSD1/KDM1A inhibitor epigenetically blocks herpes simplex virus lytic replication and reactivation from latency.

Liang Y, Quenelle D, Vogel JL, Mascaro C, Ortega A, Kristie TM.

MBio. 2013 Feb 5;4(1):e00558-12. doi: 10.1128/mBio.00558-12.


Gene silencing of EREG mediated by DNA methylation and histone modification in human gastric cancers.

Yun J, Song SH, Park J, Kim HP, Yoon YK, Lee KH, Han SW, Oh DY, Im SA, Bang YJ, Kim TY.

Lab Invest. 2012 Jul;92(7):1033-44. doi: 10.1038/labinvest.2012.61. Epub 2012 Apr 16. Erratum in: Lab Invest. 2013 Oct;93(10):1165.


Impairment of prostate cancer cell growth by a selective and reversible lysine-specific demethylase 1 inhibitor.

Willmann D, Lim S, Wetzel S, Metzger E, Jandausch A, Wilk W, Jung M, Forne I, Imhof A, Janzer A, Kirfel J, Waldmann H, Schüle R, Buettner R.

Int J Cancer. 2012 Dec 1;131(11):2704-9. doi: 10.1002/ijc.27555. Epub 2012 Jun 28.


Crosstalk between lysine-specific demethylase 1 (LSD1) and histone deacetylases mediates antineoplastic efficacy of HDAC inhibitors in human breast cancer cells.

Vasilatos SN, Katz TA, Oesterreich S, Wan Y, Davidson NE, Huang Y.

Carcinogenesis. 2013 Jun;34(6):1196-207. doi: 10.1093/carcin/bgt033. Epub 2013 Jan 25.

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