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Items: 1 to 20 of 104

1.

Discovery of a 2,4-diamino-7-aminoalkoxyquinazoline as a potent and selective inhibitor of histone lysine methyltransferase G9a.

Liu F, Chen X, Allali-Hassani A, Quinn AM, Wasney GA, Dong A, Barsyte D, Kozieradzki I, Senisterra G, Chau I, Siarheyeva A, Kireev DB, Jadhav A, Herold JM, Frye SV, Arrowsmith CH, Brown PJ, Simeonov A, Vedadi M, Jin J.

J Med Chem. 2009 Dec 24;52(24):7950-3. doi: 10.1021/jm901543m.

2.

Protein lysine methyltransferase G9a inhibitors: design, synthesis, and structure activity relationships of 2,4-diamino-7-aminoalkoxy-quinazolines.

Liu F, Chen X, Allali-Hassani A, Quinn AM, Wigle TJ, Wasney GA, Dong A, Senisterra G, Chau I, Siarheyeva A, Norris JL, Kireev DB, Jadhav A, Herold JM, Janzen WP, Arrowsmith CH, Frye SV, Brown PJ, Simeonov A, Vedadi M, Jin J.

J Med Chem. 2010 Aug 12;53(15):5844-57. doi: 10.1021/jm100478y.

4.

Structural basis for G9a-like protein lysine methyltransferase inhibition by BIX-01294.

Chang Y, Zhang X, Horton JR, Upadhyay AK, Spannhoff A, Liu J, Snyder JP, Bedford MT, Cheng X.

Nat Struct Mol Biol. 2009 Mar;16(3):312-7. doi: 10.1038/nsmb.1560. Epub 2009 Feb 15.

5.

Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines.

Liu F, Barsyte-Lovejoy D, Allali-Hassani A, He Y, Herold JM, Chen X, Yates CM, Frye SV, Brown PJ, Huang J, Vedadi M, Arrowsmith CH, Jin J.

J Med Chem. 2011 Sep 8;54(17):6139-50. doi: 10.1021/jm200903z. Epub 2011 Aug 5.

6.

Properly substituted analogues of BIX-01294 lose inhibition of G9a histone methyltransferase and gain selective anti-DNA methyltransferase 3A activity.

Rotili D, Tarantino D, Marrocco B, Gros C, Masson V, Poughon V, Ausseil F, Chang Y, Labella D, Cosconati S, Di Maro S, Novellino E, Schnekenburger M, Grandjenette C, Bouvy C, Diederich M, Cheng X, Arimondo PB, Mai A.

PLoS One. 2014 May 8;9(5):e96941. doi: 10.1371/journal.pone.0096941. eCollection 2014.

7.

Discovery of novel small molecule inhibitors of lysine methyltransferase G9a and their mechanism in leukemia cell lines.

Kondengaden SM, Luo LF, Huang K, Zhu M, Zang L, Bataba E, Wang R, Luo C, Wang B, Li KK, Wang PG.

Eur J Med Chem. 2016 Oct 21;122:382-93. doi: 10.1016/j.ejmech.2016.06.028. Epub 2016 Jun 21.

PMID:
27393948
8.

Epidithiodiketopiperazine as a pharmacophore for protein lysine methyltransferase G9a inhibitors: reducing cytotoxicity by structural simplification.

Fujishiro S, Dodo K, Iwasa E, Teng Y, Sohtome Y, Hamashima Y, Ito A, Yoshida M, Sodeoka M.

Bioorg Med Chem Lett. 2013 Feb 1;23(3):733-6. doi: 10.1016/j.bmcl.2012.11.087. Epub 2012 Dec 5.

PMID:
23266120
9.

Adding a lysine mimic in the design of potent inhibitors of histone lysine methyltransferases.

Chang Y, Ganesh T, Horton JR, Spannhoff A, Liu J, Sun A, Zhang X, Bedford MT, Shinkai Y, Snyder JP, Cheng X.

J Mol Biol. 2010 Jul 2;400(1):1-7. doi: 10.1016/j.jmb.2010.04.048. Epub 2010 Apr 29.

10.

Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferase.

Kubicek S, O'Sullivan RJ, August EM, Hickey ER, Zhang Q, Teodoro ML, Rea S, Mechtler K, Kowalski JA, Homon CA, Kelly TA, Jenuwein T.

Mol Cell. 2007 Feb 9;25(3):473-81.

11.

A chemical tool for in vitro and in vivo precipitation of lysine methyltransferase G9a.

Konze KD, Pattenden SG, Liu F, Barsyte-Lovejoy D, Li F, Simon JM, Davis IJ, Vedadi M, Jin J.

ChemMedChem. 2014 Mar;9(3):549-53. doi: 10.1002/cmdc.201300450. Epub 2014 Jan 17.

12.

Structure-Based Design of a Covalent Inhibitor of the SET Domain-Containing Protein 8 (SETD8) Lysine Methyltransferase.

Butler KV, Ma A, Yu W, Li F, Tempel W, Babault N, Pittella-Silva F, Shao J, Wang J, Luo M, Vedadi M, Brown PJ, Arrowsmith CH, Jin J.

J Med Chem. 2016 Nov 10;59(21):9881-9889. Epub 2016 Nov 2.

PMID:
27804297
13.

Using 'biased-privileged' scaffolds to identify lysine methyltransferase inhibitors.

Kashyap S, Sandler J, Peters U, Martinez EJ, Kapoor TM.

Bioorg Med Chem. 2014 Apr 1;22(7):2253-60. doi: 10.1016/j.bmc.2014.02.024. Epub 2014 Feb 28.

14.

A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells.

Vedadi M, Barsyte-Lovejoy D, Liu F, Rival-Gervier S, Allali-Hassani A, Labrie V, Wigle TJ, Dimaggio PA, Wasney GA, Siarheyeva A, Dong A, Tempel W, Wang SC, Chen X, Chau I, Mangano TJ, Huang XP, Simpson CD, Pattenden SG, Norris JL, Kireev DB, Tripathy A, Edwards A, Roth BL, Janzen WP, Garcia BA, Petronis A, Ellis J, Brown PJ, Frye SV, Arrowsmith CH, Jin J.

Nat Chem Biol. 2011 Jul 10;7(8):566-74. doi: 10.1038/nchembio.599. Erratum in: Nat Chem Biol. 2011 Sep;7(9):648. Nat Chem Biol. 2011;7(8):following 574.

15.

Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP.

Liu F, Barsyte-Lovejoy D, Li F, Xiong Y, Korboukh V, Huang XP, Allali-Hassani A, Janzen WP, Roth BL, Frye SV, Arrowsmith CH, Brown PJ, Vedadi M, Jin J.

J Med Chem. 2013 Nov 14;56(21):8931-42. doi: 10.1021/jm401480r. Epub 2013 Oct 31.

16.

Discovery of a selective, substrate-competitive inhibitor of the lysine methyltransferase SETD8.

Ma A, Yu W, Li F, Bleich RM, Herold JM, Butler KV, Norris JL, Korboukh V, Tripathy A, Janzen WP, Arrowsmith CH, Frye SV, Vedadi M, Brown PJ, Jin J.

J Med Chem. 2014 Aug 14;57(15):6822-33. doi: 10.1021/jm500871s. Epub 2014 Jul 25.

17.

A small-molecule probe of the histone methyltransferase G9a induces cellular senescence in pancreatic adenocarcinoma.

Yuan Y, Wang Q, Paulk J, Kubicek S, Kemp MM, Adams DJ, Shamji AF, Wagner BK, Schreiber SL.

ACS Chem Biol. 2012 Jul 20;7(7):1152-7. doi: 10.1021/cb300139y. Epub 2012 Apr 30.

18.

G9a/GLP histone lysine dimethyltransferase complex activity in the hippocampus and the entorhinal cortex is required for gene activation and silencing during memory consolidation.

Gupta-Agarwal S, Franklin AV, Deramus T, Wheelock M, Davis RL, McMahon LL, Lubin FD.

J Neurosci. 2012 Apr 18;32(16):5440-53. doi: 10.1523/JNEUROSCI.0147-12.2012.

19.

An analog of BIX-01294 selectively inhibits a family of histone H3 lysine 9 Jumonji demethylases.

Upadhyay AK, Rotili D, Han JW, Hu R, Chang Y, Labella D, Zhang X, Yoon YS, Mai A, Cheng X.

J Mol Biol. 2012 Feb 24;416(3):319-27. doi: 10.1016/j.jmb.2011.12.036. Epub 2011 Dec 29.

20.

A chemiluminescence-based method for identification of histone lysine methyltransferase inhibitors.

Quinn AM, Allali-Hassani A, Vedadi M, Simeonov A.

Mol Biosyst. 2010 May;6(5):782-8. doi: 10.1039/b921912a. Epub 2010 Mar 2.

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