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Staff Profile
Professor Akane Kawamura
Professor of Chemical Biology
- Address: School of Natural and Environmental Sciences, Chemistry
Bedson Building (Room 3.11)
Kings Road
Newcastle University
Newcastle Upon Tyne
NE1 7RU
Background
Visit: Kawamura group website
Publications
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Articles
- Simelis 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 2024, 99, 117597.
- Smith TS, Bhushan B, Granata D, Kaas CS, Andersen B, Decoene KW, Ren Q, Liu H, Qu X, Yang Y, Pan J, Chen Q, Munzel M, Kawamura A. Identification and engineering of potent cyclic peptides with selective or promiscuous binding through biochemical profiling and bioinformatic data analysis. RSC Chemical Biology 2024, 5(1), 12-18.
- 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 2024, Epub ahead of print.
- 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 2023, 597(7), 933-946.
- 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, Suga H. In vitro selection of macrocyclic peptide inhibitors containing cyclic γ2,4-amino acids targeting the SARS-CoV-2 main protease. Nature Chemistry 2023, 15, 998-1005.
- Salvini CLA, Darlot B, Davison J, Martin MP, Tudhope SJ, Turberville S, Kawamura A, Noble MEM, Wedge SR, Crawford JJ, Waring MJ. Fragment expansion with NUDELs – poised DNA-encoded libraries. Chemical Science 2023, 14(31), 8288-8294.
- 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 2023, 14(26), 7136-7146.
- Pringle TA, Coleman O, Kawamura A, Knight JC. The influence of degree of labelling upon cellular internalisation of antibody-cell penetrating peptide conjugates. RSC Advances 2022, 12(43), 27716-27722.
- Belle R, Kamps JJAG, Poater J, Kumar K, Pieters BJGE, Salah E, Claridge TDW, Paton RS, Bickelhaupt FM, Kawamura A, Schofield CJ, Mecinovic J. Reading and erasing of the phosphonium analogue of trimethyllysine by epigenetic proteins. Communications Chemistry 2022, 5, 27.
- Bhushan B, Granata D, Kaas CS, Kasimova MA, Ren Q, Cramer CN, White MD, Hansen AMK, Fledelius C, Invernizzi G, Deibler K, Coleman OD, Zhao X, Qu X, Liu H, Zurmühl SS, Kodra JT, Kawamura A, Münzel M. An integrated platform approach enables discovery of potent, selective and ligand-competitive cyclic peptides targeting the GIP receptor. Chemical Science 2022, 13(11), 3256-3262.
- McAllister TE, Coleman OC, Roper G, Kawamura A. Structural diversity in de novo cyclic peptide ligands from genetically encoded library technologies. Peptide Science 2021, 113(1), e24204.
- Hsu KF, Wilkins SE, Hopkinson RJ, Sekirnik R, Flashman E, Kawamura A, McCullagh JSO, Walport L, Schofield CJ. Hypoxia and hypoxia mimetics differentially modulate histone post-translational modifications. Epigenetics 2021, 16(1), 14-27.
- 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 2020, 10(1), 21964.
- Sarac H, Morova T, Pires E, McCullagh J, Kaplan A, Cingoz A, Bagci-Onder T, Onder T, Kawamura A, Lack NA. Systematic characterization of chromatin modifying enzymes identifies KDM3B as a critical regulator in castration resistant prostate cancer. Oncogene 2020, 39, 2187–2201.
- 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 2020, 10, 17955.
- Josephson B, Fehl C, Isenegger PG, Nadal S, Wright TH, Poh AWJ, Bower BJ, Giltrap AM, Chen L, Batchelor-McAuley C, Roper G, Arisa O, Sap JBI, Kawamura A, Baldwin AJ, Mohammed S, Compton RG, Gouverneur V, Davis BG. Light-driven post-translational installation of reactive protein side chains. Nature 2020, 585, 530-537.
- 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. Journal of Biological Chemistry 2020, 295(32), 10926-10939.
- Roatsch M, Hoffmann I, Abboud MI, Hancock RL, Tarhonskaya H, Hsu K-F, Wilkins SE, Yeh T-L, Lippl K, Serrer K, Moneke I, Ahrens TD, Robaa D, Wenzler S, Barthes NPF, Franz H, Sippl W, Lassmann S, Diederichs S, Schleicher E, Schofield CJ, Kawamura A, Schule R, Jung M. The Clinically Used Iron Chelator Deferasirox Is an Inhibitor of Epigenetic JumonjiC Domain-Containing Histone Demethylases. ACS Chemical Biology 2019, 14(8), 1737-1750.
- Reinbold R, John T, Spingardi P, Kawamura A, Thompson AL, Schofield CJ, Hopkinson RJ. Formaldehyde quantification using ampicillin is not selective. Scientific Reports 2019, 9, 18289.
- Vazquez-Rodriguez S, Wright M, Rogers CM, Cribbs AP, Velupillai S, Philpott M, Lee H, Dunford JE, Huber KVM, Robers MB, Vasta JD, Thezenas M-L, Bonham S, Kessler B, Bennett J, Fedorov O, Raynaud F, Donovan A, Blagg J, Bavetsias V, Oppermann U, Bountra C, Kawamura A, Brennan PE. Design, Synthesis and Characterization of Covalent KDM5 Inhibitors. Angewandte Chemie - International Edition 2019, 58(2), 515-519.
- 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. Journal of Biological Chemistry 2019, 294(29), 11199-11212.
- 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 2018, 19(9), 979-985.
- 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. Journal of Biological Chemistry 2018, 293(16), 6134-6146.
- Guillade L, Sarno F, Tarhonskaya H, Nebbioso A, Alvarez S, Kawamura A, Schofield CJ, Altucci L, de Lera AR. Synthesis and Biological Evaluation of Tripartin, a Putative KDM4 Natural Product Inhibitor, and 1-Dichloromethylinden-1-ol Analogues. ChemMedChem 2018, 13(18), 1949-1956.
- Passioura T, Bhushan B, Tumber A, Kawamura A, Suga H. Structure-activity studies of a macrocyclic peptide inhibitor of histone lysine demethylase 4A. Bioorganic and Medicinal Chemistry 2018, 26(6), 1225-1231.
- McAllister TE, Yeh T-L, Abboud MI, Leung IKH, Hookway ES, King ONF, Bhushan B, Williams ST, Hopkinson RJ, Munzel M, Loik ND, Chowdhury R, Oppermann U, Claridge TDW, Goto Y, Suga H, Schofield CJ, Kawamura A. Non-competitive cyclic peptides for targeting enzyme-substrate complexes. Chemical Science 2018, 9(20), 4569-4578.
- 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 2018, 592(19), 3264-3273.
- Hancock RL, Abboud MI, Smart TJ, Flashman E, Kawamura A, Schofield CJ, Hopkinson RJ. Lysine-241 Has a Role in Coupling 2OG Turnover with Substrate Oxidation During KDM4-Catalysed Histone Demethylation. ChemBioChem 2018, 19(9), 917-921.
- Bonnici J, Tumber A, Kawamura A, Schofield CJ. Inhibitors of both the N-methyl lysyl- and arginyl-demethylase activities of the JmjC oxygenases. Philosophical Transactions of the Royal Society B: Biological Sciences 2018, 373(1748), 20170071.
- 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 2018, 80(1), 3.15.1-3.15.12.
- Hopkinson RJ, Langley GW, Belle R, Walport LJ, Dunne K, Munzel M, Salah E, Kawamura A, Claridge TDW, Schofield CJ. Human histone demethylase KDM6B can catalyse sequential oxidations. Chemical Communications 2018, 54(57), 7975-7978.
- 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 2018, 8, 6333.
- Abboud MI, McAllister TE, Leung IKH, Chowdhury R, Jorgensen C, Domene C, Mecinovic 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 2018, 54(25), 3130-3133.
- 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 2017, 7, 4267.
- 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 2017, 12(4), 1011-1019.
- 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 2017, 429(19), 2895-2906.
- Hanauer T, Hopkinson RJ, Patel K, Li Y, Correddu D, Kawamura A, Sarojini V, Leung IKH, Gruber T. Selective recognition of the di/trimethylammonium motif by an artificial carboxycalixarene receptor. Organic and Biomolecular Chemistry 2017, 15(5), 1100-1105.
- 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, Fedorov O, Munro S, England KS, Nowak RP, Schofield CJ, La Thangue NB, Pawlyn C, Davies F, Morgan G, Athanasou N, Muller S, Oppermann U, Brennan PE. Potent and Selective KDM5 Inhibitor Stops Cellular Demethylation of H3K4me3 at Transcription Start Sites and Proliferation of MM1S Myeloma Cells. Cell Chemical Biology 2017, 24(3), 371-380.
- Yeh T-L, 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, Flashman E, Lu X, Ratcliffe PJ, Chowdhury R, Pugh CW, Schofield CJ. Molecular and cellular mechanisms of HIF prolyl hydroxylase inhibitors in clinical trials. Chemical Science 2017, 8(11), 7651-7668.
- Dobrynin G, McAllister TE, Leszczynska KB, Ramachandran S, Krieg AJ, Kawamura A, Hammond EM. KDM4A regulates HIF-1 levels through H3K9me3. Scientific Reports 2017, 7, 11094.
- 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, Mill P. KDM3A coordinates actin dynamics with intraflagellar transport to regulate cilia stability. Journal of Cell Biology 2017, 216(4), 999-1013.
- 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, Mecinovic J. Investigating d-lysine stereochemistry for epigenetic methylation, demethylation and recognition. Chemical Communications 2017, 53(99), 13264-13267.
- Kawamura A, Munzel M, Kojima T, Yapp C, Bhushan B, Goto Y, Tumber A, Katoh T, King ONF, Passioura T, Walport LJ, Hatch SB, Madden S, Muller S, Brennan PE, Chowdhury R, Hopkinson RJ, Suga H, Schofield CJ. Highly selective inhibition of histone demethylases by de novo macrocyclic peptides. Nature Communications 2017, 8, 14773.
- Gerken PA, Wolstenhulme JR, Tumber A, Hatch SB, Zhang Y, Muller S, Chandler SA, Mair B, Li F, Nijman SMB, Konietzny R, Szommer T, Yapp C, Fedorov O, Benesch JLP, Vedadi M, Kessler BM, Kawamura A, Brennan PE, Smith MD. Discovery of a Highly Selective Cell-Active Inhibitor of the Histone Lysine Demethylases KDM2/7. Angewandte Chemie - International Edition 2017, 56(49), 15555-15559.
- 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, Westaway SM, Brown JA, Prinjha RK, Martinez ED, Oppermann U, Schofield CJ, Bountra C, Kawamura A, Blagg J, Brennan PE, Rossanese O, Muller S. Assessing histone demethylase inhibitors in cells: Lessons learned. Epigenetics and Chromatin 2017, 10, 9.
- Peacock H, Thinnes CC, Kawamura A, Hamilton AD. Tetracyanoresorcin[4]arene selectively recognises trimethyllysine and inhibits its enzyme-catalysed demethylation. Supramolecular Chemistry 2016, 28(5-6), 575-581.
- 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 2016, 7, 11974.
- Bavetsias V, Lanigan RM, Ruda GF, Atrash B, McLaughlin MG, Tumber A, Mok NY, Le Bihan Y-V, Dempster S, Boxall KJ, Jeganathan F, Hatch SB, Savitsky P, Velupillai S, Krojer T, England KS, Sejberg J, Thai C, Donovan A, Pal A, Scozzafava G, Bennett JM, Kawamura A, Johansson C, Szykowska A, Gileadi C, Burgess-Brown NA, Von Delft F, Oppermann U, Walters Z, Shipley J, Raynaud FI, Westaway SM, Prinjha RK, Fedorov O, Burke R, Schofield CJ, Westwood IM, Bountra C, Muller S, Van Montfort RLM, Brennan PE, Blagg J. 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 2016, 59(4), 1388-1409.
- Chan MC, Atasoylu O, Hodson E, Tumber A, Leung IKH, Chowdhury R, Gomez-Perez V, Demetriades M, Rydzik AM, Holt-Martyn J, Tian Y-M, Bishop T, Claridge TDW, Kawamura A, Pugh CW, Ratcliffe PJ, Schofield CJ. Potent and selective triazole-based inhibitors of the hypoxia-inducible factor prolyl-hydroxylases with activity in the murine brain. PLoS ONE 2015, 10(7), e0132004.
- Thinnes CC, Tumber A, Yapp C, Scozzafava G, Yeh T, Chan MC, Tran TA, Hsu K, Tarhonskaya H, Walport LJ, Wilkins SE, Martinez ED, Muller S, Pugh CW, Ratcliffe PJ, Brennan PE, Kawamura A, Schofield CJ. Betti reaction enables efficient synthesis of 8-hydroxyquinoline inhibitors of 2-oxoglutarate oxygenases. Chemical Communications 2015, 51(84), 15458-15461.
- 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 2014, 9(12), 1596-1603.
- Brem J, Van Berkel SS, Aik W, Rydzik AM, Avison MB, Pettinati I, Umland K-D, Kawamura A, Spencer J, Claridge TDW, McDonough MA, Schofield CJ. Rhodanine hydrolysis leads to potent thioenolate mediated metallo-β-lactamase inhibition. Nature Chemistry 2014, 6(12), 1084-1090.
- 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 ONF, Hopkinson RJ, Kawamura A, Schofield CJ, Mai A. Pan-histone demethylase inhibitors simultaneously targeting Jumonji C and lysine-specific demethylases display high anticancer activities. Journal of Medicinal Chemistry 2014, 57(1), 42-55.
- 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 2014, 5(12), 1879-1886.
- Tarhonskaya H, Rydzik AM, Leung IKH, Loik ND, Chan MC, Kawamura A, McCullagh JSO, Claridge TDW, Flashman E, Schofield CJ. Non-enzymatic chemistry enables 2-hydroxyglutarate-mediated activation of 2-oxoglutarate oxygenases. Nature Communications 2014, 5, 3423.
- 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 2014, 5(5), 1765-1771.
- 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 and Toxicology 2014, 15(1), 68.
- Schiller R, Scozzafava G, Tumber A, Wickens JR, Bush JT, Rai G, Lejeune C, Choi H, Yeh T-L, Chan MC, Mott BT, McCullagh JSO, Maloney DJ, Schofield CJ, Kawamura A. A cell-permeable ester derivative of the JmjC histone demethylase inhibitor IOX1. ChemMedChem 2014, 9(3), 566-571.
- Chowdhury R, Candela-Lena J, Chan M, Greenald D, Yeoh K, Tian Y, McDonough M, Tumber A, Rose NR, Conejo-Garcia A, Demetriades M, Mathavan S, Kawamura A, Lee MK, vanEeden F, Pugh C, Ratcliffe PJ, Schofield CJ. Selective Small Molecule Probes for the Hypoxia Inducible Factor (HIF) Prolyl Hydroxylases. ACS Chemical Biology 2013, 8, 1488-1496.
- Hopkinson RJ, Walport LJ, Münzel M, Rose NR, Smart TJ, Kawamura A, Claridge TDW, Schofield CJ. Is JmjC Oxygenase Catalysis Limited to Demethylation?. Angewandte Chemie International Edition 2013, 55(30), 7709-7713.
- 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. Identification of the KDM2/7 histone lysine demethylase subfamily inhibitor and its antiproliferative activity. Journal of Medicinal Chemistry 2013, 56(18), 7222-7231.
- Hopkinson 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. 5-Carboxy-8-hydroxyquinoline is a broad spectrum 2-oxoglutarate oxygenase inhibitor which causes iron translocation. Chemical Science 2013, 4(8), 3110-3117.
- 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, Danie M, Strain-Damerell C, Gileadi C, Kochan G, Leung IK, Dunford J, Yeoh KK, Ratcliffe PJ, Burgess-Brown N, vonDelft F, Muller S, Marsden B, Brennan PE, McDonough MA, Oppermann U, Klose RJ, Schofield CJ, Kawamura A. Plant Growth Regulator Daminozide Is a Selective Inhibitor of Human KDM2/7 Histone Demethylases. Journal of Medicinal Chemistry 2012, 55, 6639-6643.
- 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 2012, 7(12), e52790.
- Woon ECY, Tumber A, Kawamura A, Hillringhaus L, Ge W, Rose NR, Ma JHY, 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 2012, 51, 1631-1634.
- 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, Mecinovic J, Schofield CJ. Dual-action inhibitors of HIF hydroxylases that induce binding of a second iron ion. Org Biomol Chem 2012, 11, 732-745.
- Leung IK, Demetriades M, Hardy AP, Lejeune C, Smart TJ, Szollossi A, Kawamura A, Schofield CJ, Claridge TD. A reporter ligand NMR screening method for 2-oxogluarate inhibitors. Journal of Medicinal Chemistry 2012, 56(2), 547-555.
- Chowdhury R, Yeoh K, Tian Y, Hillringhaus L, Bagg E, Rose NR, Leung IK, Woon EC, Yang M, McDonough MA, King ON, Clifton IJ, Klose RJ, Claridge TD, Ratcliffe PJ, Schofield CJ, Kawamura A. The oncometabolite 2-hydroxyglutarate inhibits histone lysine demethylases. EMBO Reports 2011, 12, 463-469.
- 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 2011, 14(2), 117-24.
- Rotili D, Altun M, Kawamura A, Wolf A, Fischer R, Leung IKH, Mackeen MM, Tian Y, Ratcliffe PJ, Mai A, Kessler BM, Schofield CJ. A Photoreactive Small-Molecule Probe for 2-Oxoglutarate. Cell Chemical Biology 2011, 18, 642-654.
- 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. J Am Chem Soc 2010, 132(10), 3238-9.
- King ON, Li XS, Sakurai M, Kawamura A, Rose NR, Ng SN, Quinn AM, Rai G, Mott BT, Klose RJ, Oppermann U, Heightman T, Maloney DJ, Jadhav A, Schofield CJ, Simeonov A. Quantitative High-Throughput Screening Identifies 8-Hydroxyquinolines as Cell-Active Histone Demethylase Inhibitors. PLOS ONE 2010, 5(11), e15535.
- Westwood I, 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 2010, 1(1), 82-95.
- Kawamura A, Tumber A, Rose NR, King ON, Daniel M, Oppermann U, Heightman TD, Schofield CJ. Development of homogeneous luminescence assays for histone demethylase catalysis and binding. Anal Biochem 2010, 404(1), 86-93.
- 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. Biochem J 2009, 418(2), 369-78.
- 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. Bioorg Med Chem 2009, 17(2), 905-918.
- 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. Biochem Pharm 2009, 75(7), 868-878.
- 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 2009, 28, 281-293.
- Wakefield L, Cornish V, Long H, Kawamura A, Zhang X, Hein DW, Sim E. Mouse arylamine N-acetyltransferase 2 (Nat2) expression in the developing neuroendocrine system. Biomarkers 2007, 13(1), 106-118.
- Fakis G, Boukouvala S, Kawamura A, Kennedy S. Description of a novel polymorphic gene encoding for arylamine N-acetyltransferase in the rhesus macaque (Macaca mulatta), a model animal for endometriosis. Pharmacogenetics and Genomics 2007, 17(3), 181-188.
- Wang H, Vath GM, Kawamura A, Bates CA, Sim E, Hanna PE, Wagner CR. Overexpression, Purification, and Characterization of Recombinant Human Arylamine N-Acetyltransferase 1. The Protein Journal 2005, 24, 65–77.
- Kawamura A, Graham J, Mushtaq A, Vath GM, Hanna PE, Wagner CR, Sim E. Eukaryotic arylamine N-acetyltransferase: Investigation of substrate specificity by high-throughput screening. Biochem Pharm 2005, 69, 347-359.
- 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 2003, 27(1), 75-84.
- 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. J Mol Biol 2002, 318, 1071-1083.
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Book Chapters
- Bhattacharya S, Kawamura A. Using evasins to target the chemokine network in inflammation. In: Advances in Protein Chemistry and Structural Biology – Inflammatory Diseases – Part A. Elsevier, 2020, pp.1-38.
- Wright M, Brennan P, Kawamura A. Inhibitors of JmjC-containing Histone Demethylases: Structural Perspective. In: Antonello Mai, ed. Chemical Epigenetics. Cham: Springer International Publishing, 2020, pp.221-253.
- Serrano L, Roper G, Kawamura A. Cyclic Peptides as Chemical Probes. In: Paul Brennan, Saleta Vazquez Rodriguez, ed. The Discovery and Utility of Chemical Probes in Target Discovery. Cambridge: Royal Society of Chemistry, 2020, pp.100-123.
- Belle R, Kawamura A, Arimondo P. Chemical compounds targeting DNA methylation and hydroxymethylation. In: Antonello Mai, ed. Chemical Epigenetics. Cham: Springer Nature, 2020, pp.255-286.
- Højrup C, Coleman O, Bukowski JP, Clausen RP, Kawamura A. JmjC-domain-Containing Histone Demethylases. In: Wolfgang Sippl & Manfred Jung, ed. Epigenetic Drug Discovery. Weinheim: Wiley-VCH Verlag GmbH & Co. KGaA, 2019, pp.263-296.
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Editorials
- Conway SJ, Kawamura A, Marr TM, Platt F, Russell AJ. Increasing Diversity in Admissions to Postgraduate Study. Journal of Medicinal Chemistry 2022, 65(8), 5867-5869.
- Kawamura A, Ganesan A. Epigenetics equals chemical biology. Current Opinion in Chemical Biology 2020, 57, A1-A4.
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Reviews
- 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 and Medicinal Chemistry 2018, 26(11), 2984-2991.
- McAllister TE, England KS, Hopkinson RJ, Brennan PE, Kawamura A, Schofield CJ. Recent Progress in Histone Demethylase Inhibitors. Journal of Medicinal Chemistry 2016, 59(4), 1308-1329.
- Hancock RL, Dunne K, Walport LJ, Flashman E, Kawamura A. Epigenetic regulation by histone demethylases in hypoxia. Epigenomics 2015, 7(5), 791-811.
- 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 - Gene Regulatory Mechanisms 2014, 1839(12), 1416-1432.
- Kawamura A, Loenarz C, Schofield CJ. Mutations To Metabolic Enzymes In Cancer Herald A Need To Unify Genetics And Biochemistry. Cell Cycle 2011, 10(17).
- Rose NR, McDonough MA, King OF, Kawamura A, Schofield CJ. Inhibition of 2-Oxoglutarate Dependent Oxygenases. Chemical Society Reviews 2011, 40(8), 4364-4369.
- Sim E, Lack N, Wang C, Long H, Westwood I, Fullam E, Kawamura A. Arylamine N-acetyltransferases: Structural and Functional Implications of Polymorphisms. Toxicology 2008, 254, 170-183.
- Westwood IM, Kawamura A, Fullam E, Russell AJ, Davies SG, Sim E. Structure and mechanism of arylamine N- acetyltransferases. Current Topics in Medicinal Chemistry 2006, 6, 1641-1654.
- Pompeo F, Brooke E, Kawamura A, Mustaq A, Sim E. The pharmacogenetics of NAT: structural aspects. Pharmacogenomics 2002, 3(1), 19-30.