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Items: 1 to 20 of 94

1.

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
2.

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.

3.
4.

Plant growth regulator daminozide is a selective inhibitor of human KDM2/7 histone demethylases.

Rose NR, Woon EC, Tumber A, Walport LJ, Chowdhury R, Li XS, King ON, Lejeune C, Ng SS, Krojer T, Chan MC, Rydzik AM, Hopkinson RJ, Che KH, Daniel M, Strain-Damerell C, Gileadi C, Kochan G, Leung IK, Dunford J, Yeoh KK, Ratcliffe PJ, Burgess-Brown N, von Delft F, Muller S, Marsden B, Brennan PE, McDonough MA, Oppermann U, Klose RJ, Schofield CJ, Kawamura A.

J Med Chem. 2012 Jul 26;55(14):6639-43. doi: 10.1021/jm300677j. Epub 2012 Jul 11.

5.

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.

6.

Selective inhibitors of the JMJD2 histone demethylases: combined nondenaturing mass spectrometric screening and crystallographic approaches.

Rose NR, Woon EC, Kingham GL, King ON, Mecinović J, Clifton IJ, Ng SS, Talib-Hardy J, Oppermann U, McDonough MA, Schofield CJ.

J Med Chem. 2010 Feb 25;53(4):1810-8. doi: 10.1021/jm901680b.

7.

A selective inhibitor and probe of the cellular functions of Jumonji C domain-containing histone demethylases.

Luo X, Liu Y, Kubicek S, Myllyharju J, Tumber A, Ng S, Che KH, Podoll J, Heightman TD, Oppermann U, Schreiber SL, Wang X.

J Am Chem Soc. 2011 Jun 22;133(24):9451-6. doi: 10.1021/ja201597b. Epub 2011 May 31.

8.

Structural definitions of Jumonji family demethylase selectivity.

Pilka ES, James T, Lisztwan JH.

Drug Discov Today. 2015 Jun;20(6):743-9. doi: 10.1016/j.drudis.2014.12.013. Epub 2014 Dec 31. Review.

PMID:
25555749
9.

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.

10.

Inhibition of the histone demethylase JMJD2E by 3-substituted pyridine 2,4-dicarboxylates.

Thalhammer A, Mecinović J, Loenarz C, Tumber A, Rose NR, Heightman TD, Schofield CJ.

Org Biomol Chem. 2011 Jan 7;9(1):127-35. doi: 10.1039/c0ob00592d. Epub 2010 Nov 15.

11.

Crystal structure and functional analysis of JMJD5 indicate an alternate specificity and function.

Del Rizzo PA, Krishnan S, Trievel RC.

Mol Cell Biol. 2012 Oct;32(19):4044-52. doi: 10.1128/MCB.00513-12. Epub 2012 Jul 30.

12.

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.

13.

Crystal structure of a novel JmjC-domain-containing protein, TYW5, involved in tRNA modification.

Kato M, Araiso Y, Noma A, Nagao A, Suzuki T, Ishitani R, Nureki O.

Nucleic Acids Res. 2011 Mar;39(4):1576-85. doi: 10.1093/nar/gkq919. Epub 2010 Oct 23.

14.

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
15.

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
16.

Studies on substrate specificity of Jmjd2a-c histone demethylases.

Ponnaluri VK, Vavilala DT, Mukherji M.

Biochem Biophys Res Commun. 2011 Feb 25;405(4):588-92. doi: 10.1016/j.bbrc.2011.01.073. Epub 2011 Jan 23.

PMID:
21266164
17.

Pan-histone demethylase inhibitors simultaneously targeting Jumonji C and lysine-specific demethylases display high anticancer activities.

Rotili D, Tomassi S, Conte M, Benedetti R, Tortorici M, Ciossani G, Valente S, Marrocco B, Labella D, Novellino E, Mattevi A, Altucci L, Tumber A, Yapp C, King ON, Hopkinson RJ, Kawamura A, Schofield CJ, Mai A.

J Med Chem. 2014 Jan 9;57(1):42-55. doi: 10.1021/jm4012802. Epub 2013 Dec 19.

PMID:
24325601
18.

Design, synthesis, enzyme-inhibitory activity, and effect on human cancer cells of a novel series of jumonji domain-containing protein 2 histone demethylase inhibitors.

Hamada S, Suzuki T, Mino K, Koseki K, Oehme F, Flamme I, Ozasa H, Itoh Y, Ogasawara D, Komaarashi H, Kato A, Tsumoto H, Nakagawa H, Hasegawa M, Sasaki R, Mizukami T, Miyata N.

J Med Chem. 2010 Aug 12;53(15):5629-38. doi: 10.1021/jm1003655.

PMID:
20684604
19.

Identification of non-histone substrates for JMJD2A-C histone demethylases.

Ponnaluri VK, Vavilala DT, Putty S, Gutheil WG, Mukherji M.

Biochem Biophys Res Commun. 2009 Dec 11;390(2):280-4. doi: 10.1016/j.bbrc.2009.09.107. Epub 2009 Sep 30.

PMID:
19799855
20.

Enzymatic and structural insights for substrate specificity of a family of jumonji histone lysine demethylases.

Horton JR, Upadhyay AK, Qi HH, Zhang X, Shi Y, Cheng X.

Nat Struct Mol Biol. 2010 Jan;17(1):38-43. doi: 10.1038/nsmb.1753. Epub 2009 Dec 20.

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