Format
Sort by
Items per page

Send to

Choose Destination

Links from PubMed

Items: 1 to 20 of 147

1.

De novo peptide design and experimental validation of histone methyltransferase inhibitors.

Smadbeck J, Peterson MB, Zee BM, Garapaty S, Mago A, Lee C, Giannis A, Trojer P, Garcia BA, Floudas CA.

PLoS One. 2014 Feb 28;9(2):e90095. doi: 10.1371/journal.pone.0090095. eCollection 2014. Erratum in: PLoS One. 2014;9(4):e95535.

2.

De novo peptide design and experimental validation of histone methyltransferase inhibitors.

Smadbeck J, Peterson MB, Zee BM, Garapaty S, Mago A, Lee C, Giannis A, Trojer P, Garcia BA, Floudas CA.

PLoS One. 2014 Apr 16;9(4):e95535. doi: 10.1371/journal.pone.0095535. eCollection 2014.

3.

Mutation of A677 in histone methyltransferase EZH2 in human B-cell lymphoma promotes hypertrimethylation of histone H3 on lysine 27 (H3K27).

McCabe MT, Graves AP, Ganji G, Diaz E, Halsey WS, Jiang Y, Smitheman KN, Ott HM, Pappalardi MB, Allen KE, Chen SB, Della Pietra A 3rd, Dul E, Hughes AM, Gilbert SA, Thrall SH, Tummino PJ, Kruger RG, Brandt M, Schwartz B, Creasy CL.

Proc Natl Acad Sci U S A. 2012 Feb 21;109(8):2989-94. doi: 10.1073/pnas.1116418109. Epub 2012 Feb 8.

4.

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. Epub 2014 Apr 13.

PMID:
24767850
5.

EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations.

McCabe MT, Ott HM, Ganji G, Korenchuk S, Thompson C, Van Aller GS, Liu Y, Graves AP, Della Pietra A 3rd, Diaz E, LaFrance LV, Mellinger M, Duquenne C, Tian X, Kruger RG, McHugh CF, Brandt M, Miller WH, Dhanak D, Verma SK, Tummino PJ, Creasy CL.

Nature. 2012 Dec 6;492(7427):108-12. doi: 10.1038/nature11606. Epub 2012 Oct 10.

PMID:
23051747
6.

Quantification of histone H3 Lys27 trimethylation (H3K27me3) by high-throughput microscopy enables cellular large-scale screening for small-molecule EZH2 inhibitors.

Luense S, Denner P, Fernández-Montalván A, Hartung I, Husemann M, Stresemann C, Prechtl S.

J Biomol Screen. 2015 Feb;20(2):190-201. doi: 10.1177/1087057114559668. Epub 2014 Nov 19.

7.

Targeting of EZH2 to a defined genomic site is sufficient for recruitment of Dnmt3a but not de novo DNA methylation.

Rush M, Appanah R, Lee S, Lam LL, Goyal P, Lorincz MC.

Epigenetics. 2009 Aug 16;4(6):404-14. Epub 2009 Aug 29.

PMID:
19717977
8.

Substrate preferences of the EZH2 histone methyltransferase complex.

Martin C, Cao R, Zhang Y.

J Biol Chem. 2006 Mar 31;281(13):8365-70. Epub 2006 Jan 23.

9.

Development and validation of reagents and assays for EZH2 peptide and nucleosome high-throughput screens.

Diaz E, Machutta CA, Chen S, Jiang Y, Nixon C, Hofmann G, Key D, Sweitzer S, Patel M, Wu Z, Creasy CL, Kruger RG, LaFrance L, Verma SK, Pappalardi MB, Le B, Van Aller GS, McCabe MT, Tummino PJ, Pope AJ, Thrall SH, Schwartz B, Brandt M.

J Biomol Screen. 2012 Dec;17(10):1279-92. doi: 10.1177/1087057112453765. Epub 2012 Aug 17.

PMID:
22904200
10.

Convergent evolution of chromatin modification by structurally distinct enzymes: comparative enzymology of histone H3 Lys²⁷ methylation by human polycomb repressive complex 2 and vSET.

Swalm BM, Hallenbeck KK, Majer CR, Jin L, Scott MP, Moyer MP, Copeland RA, Wigle TJ.

Biochem J. 2013 Jul 15;453(2):241-7. doi: 10.1042/BJ20130439.

PMID:
23679895
11.

Structural insights into binding of small molecule inhibitors to Enhancer of Zeste Homolog 2.

Kalinić M, Zloh M, Erić S.

J Comput Aided Mol Des. 2014 Nov;28(11):1109-28. doi: 10.1007/s10822-014-9788-1. Epub 2014 Aug 20.

PMID:
25139678
12.

Epigenetic regulation of cell adhesion and communication by enhancer of zeste homolog 2 in human endothelial cells.

Dreger H, Ludwig A, Weller A, Stangl V, Baumann G, Meiners S, Stangl K.

Hypertension. 2012 Nov;60(5):1176-83. doi: 10.1161/HYPERTENSIONAHA.112.191098. Epub 2012 Sep 10.

13.

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.

14.

Different EZH2-containing complexes target methylation of histone H1 or nucleosomal histone H3.

Kuzmichev A, Jenuwein T, Tempst P, Reinberg D.

Mol Cell. 2004 Apr 23;14(2):183-93.

15.

A central role for G9a and EZH2 in the epigenetic silencing of cyclooxygenase-2 in idiopathic pulmonary fibrosis.

Coward WR, Feghali-Bostwick CA, Jenkins G, Knox AJ, Pang L.

FASEB J. 2014 Jul;28(7):3183-96. doi: 10.1096/fj.13-241760. Epub 2014 Mar 20.

16.

An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1.

Konze KD, Ma A, Li F, Barsyte-Lovejoy D, Parton T, Macnevin CJ, Liu F, Gao C, Huang XP, Kuznetsova E, Rougie M, Jiang A, Pattenden SG, Norris JL, James LI, Roth BL, Brown PJ, Frye SV, Arrowsmith CH, Hahn KM, Wang GG, Vedadi M, Jin J.

ACS Chem Biol. 2013;8(6):1324-34. doi: 10.1021/cb400133j. Epub 2013 Apr 24.

17.

Long residence time inhibition of EZH2 in activated polycomb repressive complex 2.

Van Aller GS, Pappalardi MB, Ott HM, Diaz E, Brandt M, Schwartz BJ, Miller WH, Dhanak D, McCabe MT, Verma SK, Creasy CL, Tummino PJ, Kruger RG.

ACS Chem Biol. 2014 Mar 21;9(3):622-9. doi: 10.1021/cb4008748. Epub 2013 Dec 31.

PMID:
24304166
18.
19.

Somatic mutations at EZH2 Y641 act dominantly through a mechanism of selectively altered PRC2 catalytic activity, to increase H3K27 trimethylation.

Yap DB, Chu J, Berg T, Schapira M, Cheng SW, Moradian A, Morin RD, Mungall AJ, Meissner B, Boyle M, Marquez VE, Marra MA, Gascoyne RD, Humphries RK, Arrowsmith CH, Morin GB, Aparicio SA.

Blood. 2011 Feb 24;117(8):2451-9. doi: 10.1182/blood-2010-11-321208. Epub 2010 Dec 29.

20.

A687V EZH2 is a driver of histone H3 lysine 27 (H3K27) hypertrimethylation.

Ott HM, Graves AP, Pappalardi MB, Huddleston M, Halsey WS, Hughes AM, Groy A, Dul E, Jiang Y, Bai Y, Annan R, Verma SK, Knight SD, Kruger RG, Dhanak D, Schwartz B, Tummino PJ, Creasy CL, McCabe MT.

Mol Cancer Ther. 2014 Dec;13(12):3062-73. doi: 10.1158/1535-7163.MCT-13-0876. Epub 2014 Sep 24.

Supplemental Content

Support Center