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Items: 1 to 20 of 72

1.

Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases.

Rose NR, Ng SS, Mecinović J, Liénard BM, Bello SH, Sun Z, McDonough MA, Oppermann U, Schofield CJ.

J Med Chem. 2008 Nov 27;51(22):7053-6. doi: 10.1021/jm800936s.

PMID:
18942826
2.

Crystal structures of histone demethylase JMJD2A reveal basis for substrate specificity.

Ng SS, Kavanagh KL, McDonough MA, Butler D, Pilka ES, Lienard BM, Bray JE, Savitsky P, Gileadi O, von Delft F, Rose NR, Offer J, Scheinost JC, Borowski T, Sundstrom M, Schofield CJ, Oppermann U.

Nature. 2007 Jul 5;448(7149):87-91. Epub 2007 Jun 24.

PMID:
17589501
3.

The JMJD2 members of histone demethylase revisited.

Tan H, Wu S, Wang J, Zhao ZK.

Mol Biol Rep. 2008 Dec;35(4):551-6. Epub 2007 Aug 1.

PMID:
17668288
4.

Dynamic regulation of histone lysine methylation by demethylases.

Shi Y, Whetstine JR.

Mol Cell. 2007 Jan 12;25(1):1-14. Review.

5.

Regulation of histone methylation by demethylimination and demethylation.

Klose RJ, Zhang Y.

Nat Rev Mol Cell Biol. 2007 Apr;8(4):307-18. Epub 2007 Mar 7. Review.

PMID:
17342184
6.

Lysine-specific demethylase 1 as a potential therapeutic target.

Stavropoulos P, Hoelz A.

Expert Opin Ther Targets. 2007 Jun;11(6):809-20. Review.

PMID:
17504018
7.

Inhibitor scaffold for the histone lysine demethylase KDM4C (JMJD2C).

Leurs U, Clausen RP, Kristensen JL, Lohse B.

Bioorg Med Chem Lett. 2012 Sep 15;22(18):5811-3. doi: 10.1016/j.bmcl.2012.07.091. Epub 2012 Aug 2.

PMID:
22917519
8.

The emerging functions of histone demethylases.

Agger K, Christensen J, Cloos PA, Helin K.

Curr Opin Genet Dev. 2008 Apr;18(2):159-68. doi: 10.1016/j.gde.2007.12.003. Epub 2008 Feb 20. Review.

PMID:
18281209
9.

Dynamic Histone H1 Isotype 4 Methylation and Demethylation by Histone Lysine Methyltransferase G9a/KMT1C and the Jumonji Domain-containing JMJD2/KDM4 Proteins.

Trojer P, Zhang J, Yonezawa M, Schmidt A, Zheng H, Jenuwein T, Reinberg D.

J Biol Chem. 2009 Mar 27;284(13):8395-405. doi: 10.1074/jbc.M807818200. Epub 2009 Jan 13.

10.

The future therapeutic potential of histone demethylases: A critical analysis.

Natoli G, Testa G, De Santa F.

Curr Opin Drug Discov Devel. 2009 Sep;12(5):607-15. Review.

PMID:
19736620
11.

Dynamic combinatorial mass spectrometry leads to inhibitors of a 2-oxoglutarate-dependent nucleic acid demethylase.

Woon EC, Demetriades M, Bagg EA, Aik W, Krylova SM, Ma JH, Chan M, Walport LJ, Wegman DW, Dack KN, McDonough MA, Krylov SN, Schofield CJ.

J Med Chem. 2012 Mar 8;55(5):2173-84. doi: 10.1021/jm201417e. Epub 2012 Feb 22.

PMID:
22263962
12.

Linking of 2-oxoglutarate and substrate binding sites enables potent and highly selective inhibition of JmjC histone demethylases.

Woon EC, Tumber A, Kawamura A, Hillringhaus L, Ge W, Rose NR, Ma JH, Chan MC, Walport LJ, Che KH, Ng SS, Marsden BD, Oppermann U, McDonough MA, Schofield CJ.

Angew Chem Int Ed Engl. 2012 Feb 13;51(7):1631-4. doi: 10.1002/anie.201107833. Epub 2012 Jan 12. No abstract available.

PMID:
22241642
13.

Crystal structure of the PHF8 Jumonji domain, an Nepsilon-methyl lysine demethylase.

Yue WW, Hozjan V, Ge W, Loenarz C, Cooper CD, Schofield CJ, Kavanagh KL, Oppermann U, McDonough MA.

FEBS Lett. 2010 Feb 19;584(4):825-30. doi: 10.1016/j.febslet.2009.12.055. Epub 2010 Jan 12.

14.

Inhibition of histone demethylases by 4-carboxy-2,2'-bipyridyl compounds.

Chang KH, King ON, Tumber A, Woon EC, Heightman TD, McDonough MA, Schofield CJ, Rose NR.

ChemMedChem. 2011 May 2;6(5):759-64. doi: 10.1002/cmdc.201100026. Epub 2011 Mar 15. No abstract available.

15.

Investigations on the oxygen dependence of a 2-oxoglutarate histone demethylase.

Sánchez-Fernández EM, Tarhonskaya H, Al-Qahtani K, Hopkinson RJ, McCullagh JS, Schofield CJ, Flashman E.

Biochem J. 2013 Jan 15;449(2):491-6. doi: 10.1042/BJ20121155.

16.

The 2-oxoglutarate-dependent oxygenase JMJD6 catalyses oxidation of lysine residues to give 5S-hydroxylysine residues.

Mantri M, Loik ND, Hamed RB, Claridge TD, McCullagh JS, Schofield CJ.

Chembiochem. 2011 Mar 7;12(4):531-4. doi: 10.1002/cbic.201000641. Epub 2011 Jan 18.

PMID:
22238144
17.

Synthesis and activity of N-oxalylglycine and its derivatives as Jumonji C-domain-containing histone lysine demethylase inhibitors.

Hamada S, Kim TD, Suzuki T, Itoh Y, Tsumoto H, Nakagawa H, Janknecht R, Miyata N.

Bioorg Med Chem Lett. 2009 May 15;19(10):2852-5. doi: 10.1016/j.bmcl.2009.03.098. Epub 2009 Mar 26.

PMID:
19359167
18.

A cell-permeable ester derivative of the JmjC histone demethylase inhibitor IOX1.

Schiller R, Scozzafava G, Tumber A, Wickens JR, Bush JT, Rai G, Lejeune C, Choi H, Yeh TL, Chan MC, Mott BT, McCullagh JS, Maloney DJ, Schofield CJ, Kawamura A.

ChemMedChem. 2014 Mar;9(3):566-71. doi: 10.1002/cmdc.201300428. Epub 2014 Feb 6.

19.

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.

20.

Structure and mechanism of lysine-specific demethylase enzymes.

Anand R, Marmorstein R.

J Biol Chem. 2007 Dec 7;282(49):35425-9. Epub 2007 Sep 26. Review.

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