2015

Epigenetic regulation by histone demethylases in hypoxia. Hancock RL, Dunne K, Walport LJ, Flashman E, Kawamura A. Epigenomics 2015 Apr 2:1-21. [Epub ahead of print]

2014

Studies on the Catalytic Domains of Multiple JmjC Oxygenases Using Peptide Substrates. Williams S, Walport L, Hopkinson R, Madden S, Chowdhury R, Schofield CJ, Kawamura A. Epigenetics. 2014 9(12): Online
Targeting histone lysine demethylases - Progress, challenges, and the future. Thinnes CC, England KS, Kawamura A, Chowdhury R, Schofield CJ, Hopkinson RJ. Biochim Biophys Acta. 2014 Dec;1839(12):1416-1432. doi: 10.1016/j.bbagrm.2014.05.009. Epub 2014 May 21. Review.
Rhodanine hydrolysis leads to potent thioenolate mediated metallo-β-lactamase inhibition. Brem J, van Berkel SS, Aik W, Rydzik AM, Avison MB, Pettinati I, Umland KD, Kawamura A, Spencer J, Claridge TD, McDonough MA, Schofield CJ. Nat Chem. 2014 Dec;6(12):1084-90. doi: 10.1038/nchem.2110. Epub 2014 Nov 17.
Differences between murine arylamine N-acetyltransferase type 1 and human arylamine N-acetyltransferase type 2 defined by substrate specificity and inhibitor binding. Laurieri N, Kawamura A, Westwood IM, Varney A, Morris E, Russell AJ, Stanley LA, Sim E. BMC Pharmacol Toxicol. 2014 Nov 29;15:68. doi: 10.1186/2050-6511-15-68.
Optimisation of a triazolopyridine based histone demethylase inhibitor yields a potent and selective KDM2A (FBXL11) inhibitor. England KS, Tumber A, Krojer T, Scozzafava G, Ng SS, Daniel M, Szykowska A, Che KH, von Delft F, Burgess-Brown NA, Kawamura A, Schofield CJ, Brennan PE. Med. Chem. Commun. 2014 5:1879-1886.
Modulating carnitine levels by targeting its biosynthesis – selective inhibition of γ-butyrobetaine hydroxylase. Rydzik AM, Chowdhury R, Kochan GT, Williams ST, McDonough MA, Kawamura A, Schofield CJ. Chem. Sci. 2014 5:1765-1771.
Non-enzymatic chemistry enables 2-hydroxyglutarate-mediated activation of 2-oxoglutarate oxygenases. Tarhonskaya H, Rydzik AM, Leung IK, Loik ND, Chan MC, Kawamura A, McCullagh JS, Claridge TD, Flashman E, Schofield CJ. Nat Commun. 2014 Mar 5;5:3423. doi: 10.1038/ncomms4423.
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.
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.

2013

5-Carboxy-8-hydroxyquinoline is a Broad Spectrum 2-Oxoglutarate Oxygenase Inhibitor which Causes Iron Translocation. Hokpkinson RJ, Tumber A, Yapp C, Chowdhury R, Aik W, Che KH, Li XL, Kristensen JBL, King ON, Chan MC, Yeoh KK, Choi H, Walport LJ, Thinnes CC, Bush JT, Lejeune C, Rydzik AM, Rose NR, Bagg EA, Donough MA, Yue WW, Ng SS, Olse L, Brennan P, Oppermann U, Muller-Knapp S, Klose RJ, Ratcliffe PJ, Schofield CJ, Kawamura A. Chem. Sci. 2013 4:3110-3117.
Identification of the KDM2/7 histone lysine demethylase subfamily inhibitor and its antiproliferative activity. Suzuki T, Ozasa H, Itoh Y, Zhan P, Sawada H, Mino K, Walport L, Ohkubo R, Kawamura A, Yonezawa M, Tsukada Y, Tumber A, Nakagawa H, Hasegawa M, Sasaki R, Mizukami T, Schofield CJ, Miyata N. J Med Chem. 2013 Sep 26;56(18):7222-31. doi: 10.1021/jm400624b. Epub 2013 Sep 5.
Is JmjC oxygenase catalysis limited to demethylation? Hopkinson RJ, Walport LJ, Münzel M, Rose NR, Smart TJ, Kawamura A, Claridge TD, Schofield CJ. Angew Chem Int Ed Engl. 2013 Jul 22;52(30):7709-13. doi: 10.1002/anie.201303282. Epub 2013 Jun 20.
Selective small molecule probes for the hypoxia inducible factor (HIF) prolyl hydroxylases. Chowdhury R, Candela-Lena JI, Chan MC, Greenald DJ, Yeoh KK, Tian YM, McDonough MA, Tumber A, Rose NR, Conejo-Garcia A, Demetriades M, Mathavan S, Kawamura A, Lee MK, van Eeden F, Pugh CW, Ratcliffe PJ, Schofield CJ. ACS Chem Biol. 2013 Jul 19;8(7):1488-96. doi: 10.1021/cb400088q. Epub 2013 Jun 12.
Dual-action inhibitors of HIF prolyl hydroxylases that induce binding of a second iron ion. Yeoh KK, Chan MC, Thalhammer A, Demetriades M, Chowdhury R, Tian YM, Stolze I, McNeill LA, Lee MK, Woon EC, Mackeen MM, Kawamura A, Ratcliffe PJ, Mecinović J, Schofield CJ. Org Biomol Chem. 2013 Feb 7;11(5):732-45. doi: 10.1039/c2ob26648b. Epub 2012 Nov 15.
Reporter ligand NMR screening method for 2-oxoglutarate oxygenase inhibitors. Leung IK, Demetriades M, Hardy AP, Lejeune C, Smart TJ, Szöllössi A, Kawamura A, Schofield CJ, Claridge TD. J Med Chem. 2013 Jan 24;56(2):547-55. doi: 10.1021/jm301583m. Epub 2013 Jan 4.

2012

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, et al. J Med Chem. 2012 Jul 26;55(14):6639-43. doi: 10.1021/jm300677j. Epub 2012 Jul 11.
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.
Piperidinols that show anti-tubercular activity as inhibitors of arylamine N-acetyltransferase: an essential enzyme for mycobacterial survival inside macrophages. Abuhammad A, Fullam E, Lowe ED, Staunton D, Kawamura A, Westwood IM, Bhakta S, Garner AC, Wilson DL, Seden PT, Davies SG, Russell AJ, Garman EF, Sim E. PLoS One. 2012;7(12):e52790. doi: 10.1371/journal.pone.0052790. Epub 2012 Dec 28.
Discovery of ML324, a JMJD2 demethylase inhibitor with demonstrated antiviral activity. Rai G, Kawamura A, Tumber A, Liang Y, Vogel JL, Arbuckle JH, Rose NR, Dexheimer TS, Foley TL, King ON, Quinn A, Mott BT, Schofield CJ, Oppermann U, Jadhav A, Simeonov A, Kristie TM, Maloney DJ. Probe Reports from the NIH Molecular Libraries Program [Internet]. 2012 Dec 17 [updated 2013 Sep 16]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.

2011

Mutations to metabolic enzymes in cancer herald a need to unify genetics and biochemistry. Kawamura A, Loenarz C, Schofield CJ. Cell Cycle. 2011 Sep 1;10(17):2819-20. Epub 2011 Sep 1.
Inhibition of 2-oxoglutarate dependent oxygenases. Rose NR, McDonough MA, King ON, Kawamura A, Schofield CJ. Chem Soc Rev. 2011 Aug;40(8):4364-97. doi: 10.1039/c0cs00203h. Epub 2011 Mar 10. Review.
A photoreactive small-molecule probe for 2-oxoglutarate oxygenases. Rotili D, Altun M, Kawamura A, Wolf A, Fischer R, Leung IK, Mackeen MM, Tian YM, Ratcliffe PJ, Mai A, Kessler BM, Schofield CJ. Chem Biol. 2011 May 27;18(5):642-54. doi: 10.1016/j.chembiol.2011.03.007.
The oncometabolite 2-hydroxyglutarate inhibits histone lysine demethylases. Chowdhury R, Yeoh KK, Tian YM, Hillringhaus L, Bagg EA, Rose NR, Leung IK, Li XS, Woon EC, Yang M, McDonough MA, King ON, Clifton IJ, Klose RJ, Claridge TD, Ratcliffe PJ, Schofield CJ, Kawamura A. EMBO Rep. 2011 May;12(5):463-9. doi: 10.1038/embor.2011.43. Epub 2011 Apr 1.
Novel small-molecule inhibitors of arylamine N-acetyltransferases: drug discovery by high-throughput screening. Westwood IM, Kawamura A, Russell AJ, Sandy J, Davies SG, Sim E. Comb Chem High Throughput Screen. 2011 Feb;14(2):117-24.

2010

Quantitative high-throughput screening identifies 8-hydroxyquinolines as cell-active histone demethylase inhibitors. King ON, Li XS, Sakurai M, Kawamura A, Rose NR, Ng SS, Quinn AM, Rai G, Mott BT, Beswick P, Klose RJ, Oppermann U, Jadhav A, Heightman TD, Maloney DJ, Schofield CJ, Simeonov A. PLoS One. 2010 Nov 23;5(11):e15535. doi: 10.1371/journal.pone.0015535.
Development of homogeneous luminescence assays for histone demethylase catalysis and binding. Kawamura A, Tumber A, Rose NR, King ON, Daniel M, Oppermann U, Heightman TD, Schofield C. Anal Biochem. 2010 Sep 1;404(1):86-93. doi: 10.1016/j.ab.2010.04.030. Epub 2010 May 21.
Small molecule colorimetric probes for specific detection of human arylamine N-acetyltransferase 1, a potential breast cancer biomarker. Laurieri N, Crawford MH, Kawamura A, Westwood IM, Robinson J, Fletcher AM, Davies SG, Sim E, Russell AJ. J Am Chem Soc. 2010 Mar 17;132(10):3238-9. doi: 10.1021/ja909165u.
Identification of arylamine N-acetyltransferase inhibitors as an approach towards novel anti-tuberculars. Westwood IM, Bhakta S, Russell AJ, Fullam E, Anderton MC, Kawamura A, Mulvaney AW, Vickers RJ, Bhowruth V, Besra GS, Lalvani A, Davies SG, Sim E. Protein Cell. 2010 Jan;1(1):82-95. doi: 10.1007/s13238-010-0006-1. Epub 2010 Mar 18.

2009

Comparison of the Arylamine N-acetyltransferase from Mycobacterium marinum and Mycobacterium tuberculosis. Fullam E, Kawamura A, Wilkinson H, Abuhammad A, Westwood I, Sim E. Protein J. 2009 Aug;28(6):281-93. doi: 10.1007/s10930-009-9193-0.
Temperature stability of proteins essential for the intracellular survival of Mycobacterium tuberculosis. Lack NA, Kawamura A, Fullam E, Laurieri N, Beard S, Russell AJ, Evangelopoulos D, Westwood I, Sim E. Biochem J. 2009 Mar 1;418(2):369-78. doi: 10.1042/BJ20082011.
Selective small molecule inhibitors of the potential breast cancer marker, human arylamine N-acetyltransferase 1, and its murine homologue, mouse arylamine N-acetyltransferase 2. Russell AJ, Westwood IM, Crawford MH, Robinson J, Kawamura A, Redfield C, Laurieri N, Lowe ED, Davies SG, Sim E. Bioorg Med Chem. 2009 Jan 15;17(2):905-18. doi: 10.1016/j.bmc.2008.11.032. Epub 2008 Nov 19.
Arylamine N-acetyltransferases: structural and functional implications of polymorphisms. Sim E, Lack N, Wang CJ, Long H, Westwood I, Fullam E, Kawamura A. Toxicology. 2008 Dec 30;254(3):170-83. doi: 10.1016/j.tox.2008.08.022. Epub 2008 Sep 12. Review.

2008

Mouse N-acetyltransferase type 2, the homologue of human N-acetyltransferase type 1. Kawamura A, Westwood I, Wakefield L, Long H, Zhang N, Walters K, Redfield C, Sim E. Biochem Pharmacol. 2008 Apr 1;75(7):1550-60. doi: 10.1016/j.bcp.2007.12.012. Epub 2008 Jan 5.
Mouse arylamine N-acetyltransferase 2 (Nat2) expression during embryogenesis: a potential marker for the developing neuroendocrine system. Wakefield L, Cornish V, Long H, Kawamura A, Zhang X, Hein DW, Sim E. Biomarkers. 2008 Feb;13(1):106-18.
Synthesis and anticancer activities of 6-amino amonafide derivatives. Norton JT, Witschi MA, Luong L, Kawamura A, Ghosh S, Stack MS, Sim E, Avram MJ, Appella DH, Huang S. Anticancer Drugs. 2008 Jan;19(1):23-36.

2007

2006

Structure and mechanism of arylamine N-acetyltransferases. Westwood IM, Kawamura A, Fullam E, Russell AJ, Davies SG, Sim E. Curr Top Med Chem. 2006;6(15):1641-54. Review.

2005

Over-expression, purification, and characterization of recombinant human arylamine N-acetyltransferase 1. Wang H, Vath GM, Kawamura A, Bates CA, Sim E, Hanna PE, Wagner CR. Protein J. 2005 Feb;24(2):65-77.
Eukaryotic arylamine N-acetyltransferase. Investigation of substrate specificity by high-throughput screening. Kawamura A, Graham J, Mushtaq A, Tsiftsoglou SA, Vath GM, Hanna PE, Wagner CR, Sim E. Biochem Pharmacol. 2005 Jan 15;69(2):347-59. Epub 2004 Nov 24.

2003

2002

The structure of arylamine N-acetyltransferase from Mycobacterium smegmatis--an enzyme which inactivates the anti-tubercular drug, isoniazid. Sandy J, Mushtaq A, Kawamura A, Sinclair J, Sim E, Noble M. J Mol Biol. 2002 May 10;318(4):1071-83.
The pharmacogenetics of NAT: structural aspects. Pompeo F, Brooke E, Kawamura A, Mushtaq A, Sim E. Pharmacogenomics. 2002 Jan;3(1):19-30. Review.