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Items: 1 to 20 of 169

1.

Targeted disruption of the EZH2-EED complex inhibits EZH2-dependent cancer.

Kim W, Bird GH, Neff T, Guo G, Kerenyi MA, Walensky LD, Orkin SH.

Nat Chem Biol. 2013 Oct;9(10):643-50. doi: 10.1038/nchembio.1331.

2.

Astemizole arrests the proliferation of cancer cells by disrupting the EZH2-EED interaction of polycomb repressive complex 2.

Kong X, Chen L, Jiao L, Jiang X, Lian F, Lu J, Zhu K, Du D, Liu J, Ding H, Zhang N, Shen J, Zheng M, Chen K, Liu X, Jiang H, Luo C.

J Med Chem. 2014 Nov 26;57(22):9512-21. doi: 10.1021/jm501230c.

PMID:
25369470
3.

Wedelolactone disrupts the interaction of EZH2-EED complex and inhibits PRC2-dependent cancer.

Chen H, Gao S, Li J, Liu D, Sheng C, Yao C, Jiang W, Wu J, Chen S, Huang W.

Oncotarget. 2015 May 30;6(15):13049-59.

4.

Polycomb repressive complex 2 is required for MLL-AF9 leukemia.

Neff T, Sinha AU, Kluk MJ, Zhu N, Khattab MH, Stein L, Xie H, Orkin SH, Armstrong SA.

Proc Natl Acad Sci U S A. 2012 Mar 27;109(13):5028-33. doi: 10.1073/pnas.1202258109.

5.

Histone deacetylase inhibitors deplete enhancer of zeste 2 and associated polycomb repressive complex 2 proteins in human acute leukemia cells.

Fiskus W, Pranpat M, Balasis M, Herger B, Rao R, Chinnaiyan A, Atadja P, Bhalla K.

Mol Cancer Ther. 2006 Dec;5(12):3096-104.

6.

Epigenetic therapy with 3-deazaneplanocin A, an inhibitor of the histone methyltransferase EZH2, inhibits growth of non-small cell lung cancer cells.

Kikuchi J, Takashina T, Kinoshita I, Kikuchi E, Shimizu Y, Sakakibara-Konishi J, Oizumi S, Marquez VE, Nishimura M, Dosaka-Akita H.

Lung Cancer. 2012 Nov;78(2):138-43. doi: 10.1016/j.lungcan.2012.08.003.

7.

Biological evaluation of tanshindiols as EZH2 histone methyltransferase inhibitors.

Woo J, Kim HY, Byun BJ, Chae CH, Lee JY, Ryu SY, Park WK, Cho H, Choi G.

Bioorg Med Chem Lett. 2014 Jun 1;24(11):2486-92. doi: 10.1016/j.bmcl.2014.04.010.

PMID:
24767850
8.

Identification of EZH2 and EZH1 small molecule inhibitors with selective impact on diffuse large B cell lymphoma cell growth.

Garapaty-Rao S, Nasveschuk C, Gagnon A, Chan EY, Sandy P, Busby J, Balasubramanian S, Campbell R, Zhao F, Bergeron L, Audia JE, Albrecht BK, Harmange JC, Cummings R, Trojer P.

Chem Biol. 2013 Nov 21;20(11):1329-39. doi: 10.1016/j.chembiol.2013.09.013.

9.

Inactivation of Eed impedes MLL-AF9-mediated leukemogenesis through Cdkn2a-dependent and Cdkn2a-independent mechanisms in a murine model.

Danis E, Yamauchi T, Echanique K, Haladyna J, Kalkur R, Riedel S, Zhu N, Xie H, Bernt KM, Orkin SH, Armstrong SA, Neff T.

Exp Hematol. 2015 Nov;43(11):930-935.e6. doi: 10.1016/j.exphem.2015.06.005.

10.

Targeting histone methyltransferase EZH2 as cancer treatment.

Kondo Y.

J Biochem. 2014 Nov;156(5):249-57. doi: 10.1093/jb/mvu054. Review.

PMID:
25179367
11.

Selective inhibition of EZH2 and EZH1 enzymatic activity by a small molecule suppresses MLL-rearranged leukemia.

Xu B, On DM, Ma A, Parton T, Konze KD, Pattenden SG, Allison DF, Cai L, Rockowitz S, Liu S, Liu Y, Li F, Vedadi M, Frye SV, Garcia BA, Zheng D, Jin J, Wang GG.

Blood. 2015 Jan 8;125(2):346-57. doi: 10.1182/blood-2014-06-581082.

12.

Targeting EZH2 and PRC2 dependence as novel anticancer therapy.

Xu B, Konze KD, Jin J, Wang GG.

Exp Hematol. 2015 Aug;43(8):698-712. doi: 10.1016/j.exphem.2015.05.001. Review.

13.

Selective inhibition of Ezh2 by a small molecule inhibitor blocks tumor cells proliferation.

Qi W, Chan H, Teng L, Li L, Chuai S, Zhang R, Zeng J, Li M, Fan H, Lin Y, Gu J, Ardayfio O, Zhang JH, Yan X, Fang J, Mi Y, Zhang M, Zhou T, Feng G, Chen Z, Li G, Yang T, Zhao K, Liu X, Yu Z, Lu CX, Atadja P, Li E.

Proc Natl Acad Sci U S A. 2012 Dec 26;109(52):21360-5. doi: 10.1073/pnas.1210371110.

14.

Inhibition of histone methyltransferase EZH2 depletes leukemia stem cell of mixed lineage leukemia fusion leukemia through upregulation of p16.

Ueda K, Yoshimi A, Kagoya Y, Nishikawa S, Marquez VE, Nakagawa M, Kurokawa M.

Cancer Sci. 2014 May;105(5):512-9. doi: 10.1111/cas.12386.

15.

Enhancer of zeste homolog 2 promotes the proliferation and invasion of epithelial ovarian cancer cells.

Li H, Cai Q, Godwin AK, Zhang R.

Mol Cancer Res. 2010 Dec;8(12):1610-8. doi: 10.1158/1541-7786.MCR-10-0398.

16.

Discovery, design, and synthesis of indole-based EZH2 inhibitors.

Gehling VS, Vaswani RG, Nasveschuk CG, Duplessis M, Iyer P, Balasubramanian S, Zhao F, Good AC, Campbell R, Lee C, Dakin LA, Cook AS, Gagnon A, Harmange JC, Audia JE, Cummings RT, Normant E, Trojer P, Albrecht BK.

Bioorg Med Chem Lett. 2015 Sep 1;25(17):3644-9. doi: 10.1016/j.bmcl.2015.06.056.

PMID:
26189078
17.

SAH derived potent and selective EZH2 inhibitors.

Kung PP, Huang B, Zehnder L, Tatlock J, Bingham P, Krivacic C, Gajiwala K, Diehl W, Yu X, Maegley KA.

Bioorg Med Chem Lett. 2015 Apr 1;25(7):1532-7. doi: 10.1016/j.bmcl.2015.02.017.

PMID:
25746813
18.

Structure of the catalytic domain of EZH2 reveals conformational plasticity in cofactor and substrate binding sites and explains oncogenic mutations.

Wu H, Zeng H, Dong A, Li F, He H, Senisterra G, Seitova A, Duan S, Brown PJ, Vedadi M, Arrowsmith CH, Schapira M.

PLoS One. 2013 Dec 19;8(12):e83737. doi: 10.1371/journal.pone.0083737.

19.

The trithorax protein partner menin acts in tandem with EZH2 to suppress C/EBPα and differentiation in MLL-AF9 leukemia.

Thiel AT, Feng Z, Pant DK, Chodosh LA, Hua X.

Haematologica. 2013 Jun;98(6):918-27. doi: 10.3324/haematol.2012.074195.

20.

The polycomb group protein enhancer of zeste 2 is a novel therapeutic target for cervical cancer.

Ding M, Zhang H, Li Z, Wang C, Chen J, Shi L, Xu D, Gao Y.

Clin Exp Pharmacol Physiol. 2015 May;42(5):458-64. doi: 10.1111/1440-1681.12382.

PMID:
25739318
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