| Year |
Citation |
Score |
| 2024 |
Belle R, Saraç H, Salah E, Bhushan B, Szykowska A, Roper G, Tumber A, Kriaucionis S, Burgess-Brown N, Schofield CJ, Brown T, Kawamura A. Focused Screening Identifies Different Sensitivities of Human TET Oxygenases to the Oncometabolite 2-Hydroxyglutarate. Journal of Medicinal Chemistry. PMID 38294854 DOI: 10.1021/acs.jmedchem.3c01820 |
0.524 |
|
| 2024 |
Šimelis K, Saraç H, Salah E, Nishio K, McAllister TE, Corner TP, Tumber A, Belle R, Schofield CJ, Suga H, Kawamura A. Selective targeting of human TET1 by cyclic peptide inhibitors: Insights from biochemical profiling. Bioorganic & Medicinal Chemistry. 99: 117597. PMID 38262305 DOI: 10.1016/j.bmc.2024.117597 |
0.53 |
|
| 2023 |
Coleman OD, Macdonald J, Thomson B, Ward JA, Stubbs CJ, McAllister TE, Clark S, Amin S, Cao Y, Abboud MI, Zhang Y, Sanganee H, Huber KVM, Claridge TDW, Kawamura A. Cyclic peptides target the aromatic cage of a PHD-finger reader domain to modulate epigenetic protein function. Chemical Science. 14: 7136-7146. PMID 37416723 DOI: 10.1039/d2sc05944d |
0.824 |
|
| 2023 |
Miura T, Malla TR, Owen CD, Tumber A, Brewitz L, McDonough MA, Salah E, Terasaka N, Katoh T, Lukacik P, Strain-Damerell C, Mikolajek H, Walsh MA, Kawamura A, Schofield CJ, et al. In vitro selection of macrocyclic peptide inhibitors containing cyclic γ-amino acids targeting the SARS-CoV-2 main protease. Nature Chemistry. PMID 37217786 DOI: 10.1038/s41557-023-01205-1 |
0.603 |
|
| 2023 |
Bonnici J, Oueini R, Salah E, Johansson C, Schofield CJ, Kawamura A. The catalytic domains of all human KDM5 JmjC demethylases catalyse N-methyl arginine demethylation. Febs Letters. PMID 36700827 DOI: 10.1002/1873-3468.14586 |
0.482 |
|
| 2022 |
Belle R, Kamps JJAG, Poater J, Kumar K, Pieters BJGE, Salah E, Claridge TDW, Paton RS, Bickelhaupt FM, Kawamura A, Schofield CJ, Mecinović J. Reading and erasing of the phosphonium analogue of trimethyllysine by epigenetic proteins. Communications Chemistry. 5: 27. PMID 36697896 DOI: 10.1038/s42004-022-00640-4 |
0.727 |
|
| 2022 |
Bulut I, Lee A, Cevatemre B, Ruzic D, Belle R, Kawamura A, Gul S, Nikolic K, Ganesan A, Acilan C. Dual LSD1 and HDAC6 Inhibition Induces Doxorubicin Sensitivity in Acute Myeloid Leukemia Cells. Cancers. 14. PMID 36497494 DOI: 10.3390/cancers14236014 |
0.342 |
|
| 2022 |
Belle R, Kamps JJAG, Poater J, Kumar K, Pieters BJGE, Salah E, Claridge TDW, Paton RS, Matthias Bickelhaupt F, Kawamura A, Schofield CJ, Mecinović J. Reading and erasing of the phosphonium analogue of trimethyllysine by epigenetic proteins. Communications Chemistry. 5. PMID 36071790 DOI: 10.1038/s42004-022-00640-4 |
0.728 |
|
| 2021 |
Nowak RP, Tumber A, Hendrix E, Ansari MSZ, Sabatino M, Antonini L, Andrijes R, Salah E, Mautone N, Pellegrini FR, Simelis K, Kawamura A, Johansson C, Passeri D, Pellicciari R, et al. First-in-Class Inhibitors of the Ribosomal Oxygenase MINA53. Journal of Medicinal Chemistry. 64: 17031-17050. PMID 34843649 DOI: 10.1021/acs.jmedchem.1c00605 |
0.541 |
|
| 2021 |
Paschalis A, Welti J, Neeb AJ, Yuan W, Figueiredo I, Pereira R, Ferreira A, Riisnaes R, Rodrigues DN, Jiménez-Vacas JM, Kim S, Uo T, Micco PD, Tumber A, Islam MS, ... ... Kawamura A, et al. JMJD6 Is a Druggable Oxygenase That Regulates AR-V7 Expression in Prostate Cancer. Cancer Research. 81: 1087-1100. PMID 33822745 DOI: 10.1158/0008-5472.CAN-20-1807 |
0.335 |
|
| 2020 |
Chowdhury R, Abboud MI, McAllister TE, Banerji B, Bhushan B, Sorensen JL, Kawamura A, Schofield CJ. Use of cyclic peptides to induce crystallization: case study with prolyl hydroxylase domain 2. Scientific Reports. 10: 21964. PMID 33319810 DOI: 10.1038/s41598-020-76307-8 |
0.772 |
|
| 2020 |
Reinbold R, John T, Spingardi P, Kawamura A, Schofield CJ, Hopkinson RJ. Metampicillin is a cyclic aminal produced by reaction of ampicillin with formaldehyde. Scientific Reports. 10: 17955. PMID 33087772 DOI: 10.1038/s41598-020-74990-1 |
0.322 |
|
| 2020 |
Kawamura A, Ganesan A. Editorial overview: Epigenetics equals chemical biology. Current Opinion in Chemical Biology. PMID 32800628 DOI: 10.1016/J.Cbpa.2020.07.001 |
0.317 |
|
| 2020 |
Hsu KF, Wilkins SE, Hopkinson RJ, Sekirnik R, Flashman E, Kawamura A, McCullagh JSO, Walport LJ, Schofield CJ. Hypoxia and hypoxia mimetics differentially modulate histone post-translational modifications. Epigenetics. 1-14. PMID 32609604 DOI: 10.1080/15592294.2020.1786305 |
0.539 |
|
| 2020 |
Darlot B, Eaton JRO, Geis-Asteggiante L, Yakala GK, Karuppanan K, Davies G, Robinson CV, Kawamura A, Bhattacharya S. Engineered anti-inflammatory peptides inspired by mapping an evasin-chemokine interaction. The Journal of Biological Chemistry. PMID 32471866 DOI: 10.1074/Jbc.Ra120.014103 |
0.329 |
|
| 2019 |
Saraç H, Morova T, Pires E, McCullagh J, Kaplan A, Cingöz A, Bagci-Onder T, Önder T, Kawamura A, Lack NA. Systematic characterization of chromatin modifying enzymes identifies KDM3B as a critical regulator in castration resistant prostate cancer. Oncogene. PMID 31822799 DOI: 10.1038/S41388-019-1116-8 |
0.367 |
|
| 2019 |
Reinbold R, John T, Spingardi P, Kawamura A, Thompson AL, Schofield CJ, Hopkinson RJ. Formaldehyde quantification using ampicillin is not selective. Scientific Reports. 9: 18289. PMID 31797955 DOI: 10.1038/S41598-019-54610-3 |
0.427 |
|
| 2019 |
Roatsch M, Hoffmann I, Abboud MI, Hancock RL, Tarhonskaya H, Hsu KF, Wilkins SE, Yeh TL, Lippl K, Serrer K, Moneke I, Ahrens TD, Robaa D, Wenzler S, Barthes NPF, ... ... Kawamura A, et al. The Clinically Used Iron Chelator Deferasirox is an Inhibitor of Epigenetic JumonjiC Domain-Containing Histone Demethylases. Acs Chemical Biology. PMID 31287655 DOI: 10.1021/Acschembio.9B00289 |
0.616 |
|
| 2019 |
Lee AW, Deruaz M, Lynch C, Davies G, Singh K, Alenazi Y, Eaton JRO, Kawamura A, Shaw J, Proudfoot AEI, Dias JM, Bhattacharya S. A knottin scaffold directs the CXC-chemokine-binding specificity of tick evasins. The Journal of Biological Chemistry. PMID 31167786 DOI: 10.1074/Jbc.Ra119.008817 |
0.358 |
|
| 2018 |
Passioura T, Bhushan B, Tumber A, Kawamura A, Suga H. Corrigendum to "Structure-activity studies of a macrocyclic peptide inhibitor of histone lysine demethylase 4A" [Bioorg. Med. Chem. 26/6 (2018) 1225-1231]. Bioorganic & Medicinal Chemistry. PMID 30594451 DOI: 10.1016/J.Bmc.2018.12.020 |
0.371 |
|
| 2018 |
Vazquez-Rodriguez S, Wright M, Rogers CM, Cribbs A, Velupillai S, Philpott M, Lee H, Dunford JE, Huber KVM, Robers MB, Vasta JD, Thezenas ML, Bonham S, Kessler B, Bennett J, ... ... Kawamura A, et al. Design, Synthesis and Characterization of Covalent KDM5 Inhibitors. Angewandte Chemie (International Ed. in English). PMID 30431220 DOI: 10.1002/Anie.201810179 |
0.476 |
|
| 2018 |
Walport LJ, Hopkinson RJ, Chowdhury R, Zhang Y, Bonnici J, Schiller R, Kawamura A, Schofield CJ. Mechanistic and Structural Studies of KDM-Catalysed Demethylation of Histone 1 Isotype 4 at Lysine 26. Febs Letters. PMID 30156264 DOI: 10.1002/1873-3468.13231 |
0.661 |
|
| 2018 |
Guillade L, Sarno F, Tarhnskaya H, Nebbioso A, Alvarez S, Kawamura A, Schofield C, Altucci L, de Lera AR. Synthesis and biological evaluation of tripartin, a putative KDM4 natural product inhibitor, and 1-dichloromethylinden-1-ol analogues. Chemmedchem. PMID 30047603 DOI: 10.1002/Cmdc.201800377 |
0.567 |
|
| 2018 |
Tarhonskaya H, Tumber A, Kawamura A, Schofield CJ. In Vitro Enzyme Assays for JmjC-Domain-Containing Lysine Histone Demethylases (JmjC-KDMs). Current Protocols in Pharmacology. 80: 3.15.1-3.15.12. PMID 30040204 DOI: 10.1002/Cpph.34 |
0.581 |
|
| 2018 |
Hopkinson RJ, Langley GW, Belle R, Walport LJ, Dunne K, Münzel M, Salah E, Kawamura A, Claridge TDW, Schofield CJ. Human histone demethylase KDM6B can catalyse sequential oxidations. Chemical Communications (Cambridge, England). PMID 29961803 DOI: 10.1039/C8Cc04057E |
0.538 |
|
| 2018 |
McAllister TE, Yeh TL, Abboud MI, Leung IKH, Hookway ES, King ONF, Bhushan B, Williams ST, Hopkinson RJ, Münzel M, Loik ND, Chowdhury R, Oppermann U, Claridge TDW, Goto Y, ... ... Kawamura A, et al. Non-competitive cyclic peptides for targeting enzyme-substrate complexes. Chemical Science. 9: 4569-4578. PMID 29899950 DOI: 10.1039/C8Sc00286J |
0.741 |
|
| 2018 |
Bhushan B, Erdmann A, Zhang Y, Belle R, Johannson C, Oppermann U, Hopkinson RJ, Schofield CJ, Kawamura A. Investigations on small molecule inhibitors targeting the histone H3K4 tri-methyllysine binding PHD-finger of JmjC histone demethylases. Bioorganic & Medicinal Chemistry. PMID 29764755 DOI: 10.1016/J.Bmc.2018.03.030 |
0.618 |
|
| 2018 |
Bonnici J, Tumber A, Kawamura A, Schofield CJ. Inhibitors of both the -methyl lysyl- and arginyl-demethylase activities of the JmjC oxygenases. Philosophical Transactions of the Royal Society of London. Series B, Biological Sciences. 373. PMID 29685975 DOI: 10.1098/Rstb.2017.0071 |
0.6 |
|
| 2018 |
Alenazi Y, Singh K, Davies G, Eaton JRO, Elders P, Kawamura A, Bhattacharya S. Genetically engineered two-warhead evasins provide a method to achieve precision targeting of disease-relevant chemokine subsets. Scientific Reports. 8: 6333. PMID 29679010 DOI: 10.1038/S41598-018-24568-9 |
0.316 |
|
| 2018 |
Nishio K, Belle R, Katoh T, Kawamura A, Sengoku T, Hanada K, Ohsawa N, Shirouzu M, Yokoyama S, Suga H. Thioether Macrocyclic Peptides Selected against TET1 Compact Catalytic Domain Inhibit TET1 Catalytic Activity. Chembiochem : a European Journal of Chemical Biology. PMID 29665240 DOI: 10.1002/Cbic.201800047 |
0.404 |
|
| 2018 |
Abboud MI, McAllister TE, Leung IKH, Chowdhury R, Jorgensen C, Domene C, Mecinović J, Lippl K, Hancock RL, Hopkinson RJ, Kawamura A, Claridge TDW, Schofield CJ. 2-Oxoglutarate regulates binding of hydroxylated hypoxia-inducible factor to prolyl hydroxylase domain 2. Chemical Communications (Cambridge, England). PMID 29522057 DOI: 10.1039/C8Cc00387D |
0.777 |
|
| 2018 |
Eaton JRO, Alenazi Y, Singh K, Davies G, Geis-Asteggiante L, Kessler B, Robinson CV, Kawamura A, Bhattacharya S. The N-terminal domain of a tick evasin is critical for chemokine binding and neutralization and confers specific binding activity to other evasins. The Journal of Biological Chemistry. PMID 29487134 DOI: 10.1074/Jbc.Ra117.000487 |
0.361 |
|
| 2018 |
Hancock RL, Abboud MI, Smart TJ, Flashman E, Kawamura A, Schofield CJ, Hopkinson R. Lysine-241 has a role in coupling 2OG turnover with substrate oxidation during KDM4-catalysed histone demethylation. Chembiochem : a European Journal of Chemical Biology. PMID 29443450 DOI: 10.1002/Cbic.201800002 |
0.543 |
|
| 2018 |
Passioura T, Bhushan B, Tumber A, Kawamura A, Suga H. Structure-activity studies of a macrocyclic peptide inhibitor of histone lysine demethylase 4A. Bioorganic & Medicinal Chemistry. PMID 29402611 DOI: 10.1016/J.Bmc.2018.01.013 |
0.437 |
|
| 2017 |
Yeh TL, Leissing TM, Abboud MI, Thinnes CC, Atasoylu O, Holt-Martyn JP, Zhang D, Tumber A, Lippl K, Lohans CT, Leung IKH, Morcrette H, Clifton IJ, Claridge TDW, Kawamura A, et al. Molecular and cellular mechanisms of HIF prolyl hydroxylase inhibitors in clinical trials. Chemical Science. 8: 7651-7668. PMID 29435217 DOI: 10.1039/C7Sc02103H |
0.82 |
|
| 2017 |
Belle R, Al Temimi AHK, Kumar K, Pieters BJGE, Tumber A, Dunford JE, Johansson C, Oppermann U, Brown T, Schofield CJ, Hopkinson RJ, Paton RS, Kawamura A, Mecinović J. Investigating d-lysine stereochemistry for epigenetic methylation, demethylation and recognition. Chemical Communications (Cambridge, England). 53: 13264-13267. PMID 29186216 DOI: 10.1039/C7Cc08028J |
0.717 |
|
| 2017 |
Gerken P, Wolstenhulme J, Tumber A, Hatch S, Zhang Y, Müller S, Chandler S, Mair B, Li F, Nijman S, Konietzny R, Szommer T, Yapp C, Fedorov O, Benesch J, ... ... Kawamura A, et al. Discovery of a highly selective cell-active inhibitor of KDM2/7. Angewandte Chemie (International Ed. in English). PMID 28976073 DOI: 10.1002/Anie.201706788 |
0.447 |
|
| 2017 |
Dobrynin G, McAllister TE, Leszczynska KB, Ramachandran S, Krieg AJ, Kawamura A, Hammond EM. KDM4A regulates HIF-1 levels through H3K9me3. Scientific Reports. 7: 11094. PMID 28894274 DOI: 10.1038/S41598-017-11658-3 |
0.779 |
|
| 2017 |
Tarhonskaya H, Nowak RP, Johansson C, Szykowska A, Tumber A, Hancock RL, Lang P, Flashman E, Oppermann U, Schofield CJ, Kawamura A. Studies on the Interaction of the Histone Demethylase KDM5B with Tricarboxylic Acid Cycle Intermediates. Journal of Molecular Biology. PMID 28827149 DOI: 10.1016/J.Jmb.2017.08.007 |
0.563 |
|
| 2017 |
Singh K, Davies G, Alenazi Y, Eaton JRO, Kawamura A, Bhattacharya S. Yeast surface display identifies a family of evasins from ticks with novel polyvalent CC chemokine-binding activities. Scientific Reports. 7: 4267. PMID 28655871 DOI: 10.1038/S41598-017-04378-1 |
0.324 |
|
| 2017 |
Kawamura A, Münzel M, Kojima T, Yapp C, Bhushan B, Goto Y, Tumber A, Katoh T, King ON, Passioura T, Walport LJ, Hatch SB, Madden S, Müller S, Brennan PE, et al. Highly selective inhibition of histone demethylases by de novo macrocyclic peptides. Nature Communications. 8: 14773. PMID 28382930 DOI: 10.1038/Ncomms14773 |
0.779 |
|
| 2017 |
Hatch SB, Yapp C, Montenegro RC, Savitsky P, Gamble V, Tumber A, Ruda GF, Bavetsias V, Fedorov O, Atrash B, Raynaud F, Lanigan R, Carmichael L, Tomlin K, Burke R, ... ... Kawamura A, et al. Assessing histone demethylase inhibitors in cells: lessons learned. Epigenetics & Chromatin. 10: 9. PMID 28265301 DOI: 10.1186/S13072-017-0116-6 |
0.556 |
|
| 2017 |
Tumber A, Nuzzi A, Hookway ES, Hatch SB, Velupillai S, Johansson C, Kawamura A, Savitsky P, Yapp C, Szykowska A, Wu N, Bountra C, Strain-Damerell C, Burgess-Brown NA, Ruda GF, et al. Potent and Selective KDM5 Inhibitor Stops Cellular Demethylation of H3K4me3 at Transcription Start Sites and Proliferation of MM1S Myeloma Cells. Cell Chemical Biology. PMID 28262558 DOI: 10.1016/J.Chembiol.2017.02.006 |
0.582 |
|
| 2017 |
Yeyati PL, Schiller R, Mali G, Kasioulis I, Kawamura A, Adams IR, Playfoot C, Gilbert N, van Heyningen V, Wills J, von Kriegsheim A, Finch A, Sakai J, Schofield CJ, Jackson IJ, et al. KDM3A coordinates actin dynamics with intraflagellar transport to regulate cilia stability. The Journal of Cell Biology. PMID 28246120 DOI: 10.1083/Jcb.201607032 |
0.436 |
|
| 2017 |
Hanauer T, Hopkinson RJ, Patel K, Li Y, Correddu D, Kawamura A, Sarojini V, Leung IK, Gruber T. Selective recognition of the di/trimethylammonium motif by an artificial carboxycalixarene receptor. Organic & Biomolecular Chemistry. PMID 28091667 DOI: 10.1039/C6Ob02616H |
0.395 |
|
| 2017 |
Hancock RL, Masson N, Dunne K, Flashman E, Kawamura A. The activity of JmjC histone lysine demethylase KDM4A is highly sensitive to oxygen concentrations. Acs Chemical Biology. PMID 28051298 DOI: 10.1021/Acschembio.6B00958 |
0.395 |
|
| 2016 |
Walport LJ, Hopkinson RJ, Chowdhury R, Schiller R, Ge W, Kawamura A, Schofield CJ. Arginine demethylation is catalysed by a subset of JmjC histone lysine demethylases. Nature Communications. 7: 11974. PMID 27337104 DOI: 10.1038/Ncomms11974 |
0.684 |
|
| 2016 |
Bavetsias V, Lanigan RM, Ruda GF, Atrash B, McLaughlin MG, Tumber A, Mok NY, Le Bihan YV, Dempster S, Boxall KJ, Jeganathan F, Hatch SB, Savitsky P, Velupillai S, Krojer T, ... ... Kawamura A, et al. 8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors. Journal of Medicinal Chemistry. PMID 26741168 DOI: 10.1021/Acs.Jmedchem.5B01635 |
0.583 |
|
| 2016 |
Peacock H, Thinnes CC, Kawamura A, Hamilton AD. Tetracyanoresorcin[4]arene selectively recognises trimethyllysine and inhibits its enzyme-catalysed demethylation Supramolecular Chemistry. 1-7. DOI: 10.1080/10610278.2016.1140898 |
0.476 |
|
| 2015 |
McAllister TE, England KS, Hopkinson RJ, Brennan PE, Kawamura A, Schofield CJ. Recent Progress in Histone Demethylase Inhibitors. Journal of Medicinal Chemistry. PMID 26710088 DOI: 10.1021/Acs.Jmedchem.5B01758 |
0.814 |
|
| 2015 |
Thinnes CC, Tumber A, Yapp C, Scozzafava G, Yeh T, Chan MC, Tran TA, Hsu K, Tarhonskaya H, Walport LJ, Wilkins SE, Martinez ED, Müller S, Pugh CW, Ratcliffe PJ, ... ... Kawamura A, et al. Betti reaction enables efficient synthesis of 8-hydroxyquinoline inhibitors of 2-oxoglutarate oxygenases. Chemical Communications (Cambridge, England). 51: 15458-61. PMID 26345662 DOI: 10.1039/C5Cc06095H |
0.563 |
|
| 2015 |
Chan MC, Atasoylu O, Hodson E, Tumber A, Leung IK, Chowdhury R, Gómez-Pérez V, Demetriades M, Rydzik AM, Holt-Martyn J, Tian YM, Bishop T, Claridge TD, Kawamura A, Pugh CW, et al. Potent and Selective Triazole-Based Inhibitors of the Hypoxia-Inducible Factor Prolyl-Hydroxylases with Activity in the Murine Brain. Plos One. 10: e0132004. PMID 26147748 DOI: 10.1371/Journal.Pone.0132004 |
0.655 |
|
| 2015 |
Hancock RL, Dunne K, Walport LJ, Flashman E, Kawamura A. Epigenetic regulation by histone demethylases in hypoxia. Epigenomics. 1-21. PMID 25832587 DOI: 10.2217/Epi.15.24 |
0.393 |
|
| 2014 |
Rydzik AM, Chowdhury R, Kochan GT, Williams ST, McDonough MA, Kawamura A, Schofield CJ. Modulating carnitine levels by targeting its biosynthesis pathway - selective inhibition of γ-butyrobetaine hydroxylase. Chemical Science (Royal Society of Chemistry : 2010). 5: 1765-1771. PMID 26682037 DOI: 10.1039/C4Sc00020J |
0.749 |
|
| 2014 |
England KS, Tumber A, Krojer T, Scozzafava G, Ng SS, Daniel M, Szykowska A, Che K, von Delft F, Burgess-Brown NA, Kawamura A, Schofield CJ, Brennan PE. Optimisation of a triazolopyridine based histone demethylase inhibitor yields a potent and selective KDM2A (FBXL11) inhibitor. Medchemcomm. 5: 1879-1886. PMID 26682034 DOI: 10.1039/C4Md00291A |
0.581 |
|
| 2014 |
Williams ST, Walport LJ, Hopkinson RJ, Madden SK, Chowdhury R, Schofield CJ, Kawamura A. Studies on the catalytic domains of multiple JmjC oxygenases using peptide substrates. Epigenetics. 9: 1596-603. PMID 25625844 DOI: 10.4161/15592294.2014.983381 |
0.686 |
|
| 2014 |
Laurieri N, Kawamura A, Westwood IM, Varney A, Morris E, Russell AJ, Stanley LA, Sim E. Differences between murine arylamine N-acetyltransferase type 1 and human arylamine N-acetyltransferase type 2 defined by substrate specificity and inhibitor binding. Bmc Pharmacology & Toxicology. 15: 68. PMID 25432241 DOI: 10.1186/2050-6511-15-68 |
0.694 |
|
| 2014 |
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. Rhodanine hydrolysis leads to potent thioenolate mediated metallo-β-lactamase inhibition. Nature Chemistry. 6: 1084-90. PMID 25411887 DOI: 10.1038/Nchem.2110 |
0.647 |
|
| 2014 |
Thinnes CC, England KS, Kawamura A, Chowdhury R, Schofield CJ, Hopkinson RJ. Targeting histone lysine demethylases - progress, challenges, and the future. Biochimica Et Biophysica Acta. 1839: 1416-32. PMID 24859458 DOI: 10.1016/J.Bbagrm.2014.05.009 |
0.69 |
|
| 2014 |
Tarhonskaya H, Rydzik AM, Leung IK, Loik ND, Chan MC, Kawamura A, McCullagh JS, Claridge TD, Flashman E, Schofield CJ. Non-enzymatic chemistry enables 2-hydroxyglutarate-mediated activation of 2-oxoglutarate oxygenases. Nature Communications. 5: 3423. PMID 24594748 DOI: 10.1038/Ncomms4423 |
0.502 |
|
| 2014 |
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. A cell-permeable ester derivative of the JmjC histone demethylase inhibitor IOX1. Chemmedchem. 9: 566-71. PMID 24504543 DOI: 10.1002/Cmdc.201300428 |
0.713 |
|
| 2014 |
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, ... ... Kawamura A, et al. Pan-histone demethylase inhibitors simultaneously targeting Jumonji C and lysine-specific demethylases display high anticancer activities. Journal of Medicinal Chemistry. 57: 42-55. PMID 24325601 DOI: 10.1021/Jm4012802 |
0.678 |
|
| 2014 |
Hancock R, Flashman E, Kawamura A. P58Towards understanding the effect of ischaemia on epigenetic regulation by the histone demethylases Cardiovascular Research. 103: S9.2-S9. DOI: 10.1093/Cvr/Cvu082.2 |
0.426 |
|
| 2014 |
Rydzik AM, Chowdhury R, Kochan GT, Williams ST, McDonough MA, Kawamura A, Schofield CJ. Modulating carnitine levels by targeting its biosynthesis-selective inhibition of γ-butyrobetaine hydroxylase Chemical Science. 5: 1765-1771. DOI: 10.1039/c4sc00020j |
0.685 |
|
| 2014 |
England KS, Tumber A, Krojer T, Scozzafava G, Ng SS, Daniel M, Szykowska A, Che K, Von Delft F, Burgess-Brown NA, Kawamura A, Schofield CJ, Brennan PE. Optimisation of a triazolopyridine based histone demethylase inhibitor yields a potent and selective KDM2A (FBXL11) inhibitor Medchemcomm. 5: 1879-1886. DOI: 10.1039/c4md00291a |
0.496 |
|
| 2013 |
Hopkinson RJ, Tumber A, Yapp C, Chowdhury R, Aik W, Che KH, Li XS, Kristensen JB, King ON, Chan MC, Yeoh KK, Choi H, Walport LJ, Thinnes CC, Bush JT, ... ... Kawamura A, et al. 5-Carboxy-8-hydroxyquinoline is a Broad Spectrum 2-Oxoglutarate Oxygenase Inhibitor which Causes Iron Translocation. Chemical Science (Royal Society of Chemistry : 2010). 4: 3110-3117. PMID 26682036 DOI: 10.1039/C3Sc51122G |
0.812 |
|
| 2013 |
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, et al. Identification of the KDM2/7 histone lysine demethylase subfamily inhibitor and its antiproliferative activity. Journal of Medicinal Chemistry. 56: 7222-31. PMID 23964788 DOI: 10.1021/Jm400624B |
0.594 |
|
| 2013 |
Hopkinson RJ, Walport LJ, Münzel M, Rose NR, Smart TJ, Kawamura A, Claridge TD, Schofield CJ. Is JmjC oxygenase catalysis limited to demethylation? Angewandte Chemie (International Ed. in English). 52: 7709-13. PMID 23788451 DOI: 10.1002/Anie.201303282 |
0.683 |
|
| 2013 |
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, et al. Selective small molecule probes for the hypoxia inducible factor (HIF) prolyl hydroxylases. Acs Chemical Biology. 8: 1488-96. PMID 23683440 DOI: 10.1021/Cb400088Q |
0.772 |
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| 2013 |
Leung IK, Demetriades M, Hardy AP, Lejeune C, Smart TJ, Szöllössi A, Kawamura A, Schofield CJ, Claridge TD. Reporter ligand NMR screening method for 2-oxoglutarate oxygenase inhibitors. Journal of Medicinal Chemistry. 56: 547-55. PMID 23234607 DOI: 10.1021/Jm301583M |
0.754 |
|
| 2013 |
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. Dual-action inhibitors of HIF prolyl hydroxylases that induce binding of a second iron ion. Organic & Biomolecular Chemistry. 11: 732-45. PMID 23151668 DOI: 10.1039/C2Ob26648B |
0.797 |
|
| 2013 |
Hopkinson RJ, Tumber A, Yapp C, Chowdhury R, Aik W, Che KH, Li XS, Kristensen JBL, King ONF, Chan MC, Yeoh KK, Choi H, Walport LJ, Thinnes CC, Bush JT, ... ... Kawamura A, et al. 8-Hydroxyquinoline-5-Carboxylic Acid is a Broad Spectrum 2-Oxoglutarate Oxygenase Inhibitor which Causes Iron Translocation Chemical Reviews. 4: 3110. DOI: 10.2210/Pdb4Bio/Pdb |
0.706 |
|
| 2013 |
Hopkinson RJ, Tumber A, Yapp C, Chowdhury R, Aik W, Che KH, Li XS, Kristensen JBL, King ONF, Chan MC, Yeoh KK, Choi H, Walport LJ, Thinnes CC, Bush JT, ... ... Kawamura A, et al. 5-Carboxy-8-hydroxyquinoline is a broad spectrum 2-oxoglutarate oxygenase inhibitor which causes iron translocation Chemical Science. 4: 3110-3117. DOI: 10.1039/c3sc51122g |
0.773 |
|
| 2012 |
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. Piperidinols that show anti-tubercular activity as inhibitors of arylamine N-acetyltransferase: an essential enzyme for mycobacterial survival inside macrophages. Plos One. 7: e52790. PMID 23285185 DOI: 10.1371/Journal.Pone.0052790 |
0.676 |
|
| 2012 |
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, ... ... Kawamura A, et al. Plant growth regulator daminozide is a selective inhibitor of human KDM2/7 histone demethylases. Journal of Medicinal Chemistry. 55: 6639-43. PMID 22724510 DOI: 10.1021/Jm300677J |
0.805 |
|
| 2012 |
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. Linking of 2-oxoglutarate and substrate binding sites enables potent and highly selective inhibition of JmjC histone demethylases. Angewandte Chemie (International Ed. in English). 51: 1631-4. PMID 22241642 DOI: 10.1002/Anie.201107833 |
0.796 |
|
| 2011 |
Kawamura A, Loenarz C, Schofield CJ. Mutations to metabolic enzymes in cancer herald a need to unify genetics and biochemistry. Cell Cycle (Georgetown, Tex.). 10: 2819-20. PMID 21857150 DOI: 10.4161/Cc.10.17.16745 |
0.697 |
|
| 2011 |
Rotili D, Altun M, Kawamura A, Wolf A, Fischer R, Leung IK, Mackeen MM, Tian YM, Ratcliffe PJ, Mai A, Kessler BM, Schofield CJ. A photoreactive small-molecule probe for 2-oxoglutarate oxygenases. Chemistry & Biology. 18: 642-54. PMID 21609845 DOI: 10.1016/J.Chembiol.2011.03.007 |
0.776 |
|
| 2011 |
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, ... ... Kawamura A, et al. The oncometabolite 2-hydroxyglutarate inhibits histone lysine demethylases. Embo Reports. 12: 463-9. PMID 21460794 DOI: 10.1038/Embor.2011.43 |
0.762 |
|
| 2011 |
Rose NR, McDonough MA, King ON, Kawamura A, Schofield CJ. Inhibition of 2-oxoglutarate dependent oxygenases. Chemical Society Reviews. 40: 4364-97. PMID 21390379 DOI: 10.1039/C0Cs00203H |
0.781 |
|
| 2011 |
Westwood IM, Kawamura A, Russell AJ, Sandy J, Davies SG, Sim E. Novel small-molecule inhibitors of arylamine N-acetyltransferases: drug discovery by high-throughput screening. Combinatorial Chemistry & High Throughput Screening. 14: 117-24. PMID 21118080 DOI: 10.2174/138620711794474051 |
0.668 |
|
| 2010 |
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. Identification of arylamine N-acetyltransferase inhibitors as an approach towards novel anti-tuberculars. Protein & Cell. 1: 82-95. PMID 21204000 DOI: 10.1007/S13238-010-0006-1 |
0.657 |
|
| 2010 |
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, et al. Quantitative high-throughput screening identifies 8-hydroxyquinolines as cell-active histone demethylase inhibitors. Plos One. 5: e15535. PMID 21124847 DOI: 10.1371/Journal.Pone.0015535 |
0.787 |
|
| 2010 |
Kawamura A, Tumber A, Rose NR, King ON, Daniel M, Oppermann U, Heightman TD, Schofield C. Development of homogeneous luminescence assays for histone demethylase catalysis and binding. Analytical Biochemistry. 404: 86-93. PMID 20435012 DOI: 10.1016/J.Ab.2010.04.030 |
0.773 |
|
| 2010 |
Laurieri N, Crawford MH, Kawamura A, Westwood IM, Robinson J, Fletcher AM, Davies SG, Sim E, Russell AJ. Small molecule colorimetric probes for specific detection of human arylamine N-acetyltransferase 1, a potential breast cancer biomarker. Journal of the American Chemical Society. 132: 3238-9. PMID 20170182 DOI: 10.1021/Ja909165U |
0.657 |
|
| 2009 |
Fullam E, Kawamura A, Wilkinson H, Abuhammad A, Westwood I, Sim E. Comparison of the Arylamine N-acetyltransferase from Mycobacterium marinum and Mycobacterium tuberculosis. The Protein Journal. 28: 281-93. PMID 19636684 DOI: 10.1007/S10930-009-9193-0 |
0.65 |
|
| 2009 |
Russell AJ, Westwood IM, Crawford MH, Robinson J, Kawamura A, Redfield C, Laurieri N, Lowe ED, Davies SG, Sim E. Selective small molecule inhibitors of the potential breast cancer marker, human arylamine N-acetyltransferase 1, and its murine homologue, mouse arylamine N-acetyltransferase 2. Bioorganic & Medicinal Chemistry. 17: 905-18. PMID 19059786 DOI: 10.1016/J.Bmc.2008.11.032 |
0.707 |
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| 2009 |
Lack NA, Kawamura A, Fullam E, Laurieri N, Beard S, Russell AJ, Evangelopoulos D, Westwood I, Sim E. Temperature stability of proteins essential for the intracellular survival of Mycobacterium tuberculosis. The Biochemical Journal. 418: 369-78. PMID 19014350 DOI: 10.1042/Bj20082011 |
0.633 |
|
| 2008 |
Sim E, Lack N, Wang CJ, Long H, Westwood I, Fullam E, Kawamura A. Arylamine N-acetyltransferases: structural and functional implications of polymorphisms. Toxicology. 254: 170-83. PMID 18852012 DOI: 10.1016/J.Tox.2008.08.022 |
0.667 |
|
| 2008 |
Kawamura A, Westwood I, Wakefield L, Long H, Zhang N, Walters K, Redfield C, Sim E. Mouse N-acetyltransferase type 2, the homologue of human N-acetyltransferase type 1. Biochemical Pharmacology. 75: 1550-60. PMID 18280460 DOI: 10.1016/J.Bcp.2007.12.012 |
0.683 |
|
| 2008 |
Norton JT, Witschi MA, Luong L, Kawamura A, Ghosh S, Stack MS, Sim E, Avram MJ, Appella DH, Huang S. Synthesis and anticancer activities of 6-amino amonafide derivatives. Anti-Cancer Drugs. 19: 23-36. PMID 18043127 DOI: 10.1097/Cad.0B013E3282F00E17 |
0.664 |
|
| 2008 |
Wakefield L, Cornish V, Long H, Kawamura A, Zhang X, Hein DW, Sim E. Mouse arylamine N-acetyltransferase 2 (Nat2) expression during embryogenesis: a potential marker for the developing neuroendocrine system. Biomarkers : Biochemical Indicators of Exposure, Response, and Susceptibility to Chemicals. 13: 106-18. PMID 17896208 DOI: 10.1080/13547500701673529 |
0.616 |
|
| 2006 |
Westwood IM, Kawamura A, Fullam E, Russell AJ, Davies SG, Sim E. Structure and mechanism of arylamine N-acetyltransferases. Current Topics in Medicinal Chemistry. 6: 1641-54. PMID 16918475 DOI: 10.2174/156802606778108979 |
0.396 |
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| 2005 |
Wang H, Vath GM, Kawamura A, Bates CA, Sim E, Hanna PE, Wagner CR. Over-expression, purification, and characterization of recombinant human arylamine N-acetyltransferase 1. The Protein Journal. 24: 65-77. PMID 16003948 DOI: 10.1007/S10930-004-1513-9 |
0.659 |
|
| 2005 |
Kawamura A, Graham J, Mushtaq A, Tsiftsoglou SA, Vath GM, Hanna PE, Wagner CR, Sim E. Eukaryotic arylamine N-acetyltransferase. Investigation of substrate specificity by high-throughput screening. Biochemical Pharmacology. 69: 347-59. PMID 15627487 DOI: 10.1016/J.Bcp.2004.09.014 |
0.689 |
|
| 2003 |
Kawamura A, Sandy J, Upton A, Noble M, Sim E. Structural investigation of mutant Mycobacterium smegmatis arylamine N-acetyltransferase: a model for a naturally occurring functional polymorphism in Mycobacterium tuberculosis arylamine N-acetyltransferase. Protein Expression and Purification. 27: 75-84. PMID 12509987 DOI: 10.1016/S1046-5928(02)00592-2 |
0.634 |
|
| 2002 |
Sandy J, Mushtaq A, Kawamura A, Sinclair J, Sim E, Noble M. The structure of arylamine N-acetyltransferase from Mycobacterium smegmatis--an enzyme which inactivates the anti-tubercular drug, isoniazid. Journal of Molecular Biology. 318: 1071-83. PMID 12054803 DOI: 10.1016/S0022-2836(02)00141-9 |
0.64 |
|
| 2002 |
Pompeo F, Brooke E, Kawamura A, Mushtaq A, Sim E. The pharmacogenetics of NAT: structural aspects. Pharmacogenomics. 3: 19-30. PMID 11966400 DOI: 10.1517/14622416.3.1.19 |
0.639 |
|
| 2000 |
Sandy J, Noble M, Sinclair J, Payton M, Upton A, Kawamura A, Mushtaq A, Delgoda R, Sim E. Structure of arylamrae-N-acetyl transferases Biochemical Society Transactions. 28: A74-A74. DOI: 10.1042/Bst028A074 |
0.311 |
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