Publications

This research was funded (partially or fully) by the Australian Government through the Australian Research Council.

2021

Discovery and Development of 2-Aminobenzimidazoles as Potent Antimalarials
Shane M.Devine, Matthew P.Challis, Jomo K.Kigotho, GhizalSiddiqui, Amanda De Paoli, Christopher A.MacRaild, Vicky M.Avery, Darren J.Creek, Raymond S.Norton, Peter J.Scammells
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Synthesis and evaluation of pyridine-derived bedaquiline analogues containing modifications at the A-ring subunit
Lisa Barbaro, Gayathri Nagalingam, James A. Triccas, Lendl Tan, Nicholas P. West, Jonathan B. Baell and Daniel L. Priebbenow
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Structure-Guided Development of Potent Benzoylurea Inhibitors of BCL-XL and BCL-2
Michael J. Roy, Amelia Vom, Toru Okamoto, Brian J. Smith, Richard W. Birkinshaw, Hong Yang, Houda Abdo, Christine. A. White, David Segal, David C. S. Huang, Jonathan B. Baell, Peter M. Colman, Peter E. Czabotar, and Guillaume Lessene
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Discovery of Potent and Fast-Acting Antimalarial Bis-1,2,4-triazines
Daniel L. Priebbenow, Mitch Mathiew, Da-Hua Shi, Jitendra R. Harjani, Julia G. Beveridge, Marina Chavchich, Michael D. Edstein, Sandra Duffy, Vicky M. Avery, Robert T. Jacobs, Stephen Brand, David M. Shackleford, Wen Wang, Longjin Zhong, Given Lee, Erin Tay, Helena Barker, Elly Crighton, Karen L. White, Susan A. Charman, Amanda De Paoli, Darren J. Creek, and Jonathan B. Baell
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Therapeutic Opportunities of Targeting Allosteric Binding Sites on the Calcium-Sensing Receptor
Jiayin Diao, Aaron DeBono, Tracy M. Josephs, Jane E. Bourke, Ben Capuano, Karen J. Gregory, and Katie Leach
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Lipopolysaccharide influences the plasma and brain pharmacokinetics of subcutaneously-administered HsTX1[R14A], a KV1.3-blocking peptide
Sanjeevini BabuReddiara, LiangJin, Dorothy C.C.Wai, Agota Csotic, Gyorgy Panyic, Raymond S.Norton, Joseph A.Nicolazzo
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BET-Family Bromodomains Can Recognize Diacetylated Sequences from Transcription Factors Using a Conserved Mechanism
Karishma Patel, Paul D. Solomon, James L. Walshe, Daniel J. Ford, Lorna Wilkinson-White, Richard J. Payne, Jason K. K. Low, and Joel P. Mackay
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Liposome engraftment and antigen combination potentiate the immune response towards conserved epitopes of the malaria vaccine candidate MSP2
Sreedam C. Das, Jason D. Price, Katharine Gosling, Nicola MacLennan, Ricardo Ataíde, Jeffrey Seow, Vashti Irani, Ines I. Atmosukarto, Robin F. Anders, Jack S. Richards, Christopher A. MacRaild, Raymond S. Norton
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Nuisance compounds in cellular assays
Jayme L.Dahlin, Douglas S.Auld, Ina Rothenaigner, SteveHaney, Jonathan Z.Sexton, J. Willem M.Nissink, Jarrod Walsh, Jonathan A.Lee, John M.Strelow, Francis S.Willard, LoriFerrins, Jonathan B.Baell, Michael A.Walters, Bruce K.Hua, Kamyar Hadian, Bridget K.Wagner
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Carbonic anhydrase XII inhibition overcomes P-glycoprotein-mediated drug resistance: a potential new combination therapy in cancer
Kathryn F. Tonissen, Sally-Ann Poulsen
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Early career research in medicinal chemistry
Jonathan B Baell
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Genetic Encoding of N6-(((Trimethylsilyl)methoxy)carbonyl)-l-lysine for NMR Studies of Protein–Protein and Protein–Ligand Interactions
Elwy H. Abdelkader, Haocheng Qianzhu, Yi Jiun Tan, Luke A. Adams, Thomas Huber, and Gottfried Otting
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The bromodomains of BET family proteins can recognize diacetylated histone H2A.Z
Karishma Patel, Paul D. Solomon, James L. Walshe, Jason K. K. Low, Joel P. Mackay
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2020

Discovery of Cyclic Peptide Ligands to the SARS-CoV-2 Spike Protein using mRNA Display
Alexander Norman, Charlotte Franck, Mary Christie, Paige Hawkins, Karishma Patel, Anneliese Ashhurst, Anupriya Aggarwal, Jason KK Low, Rezwan Siddiquee, Caroline Ashley, Megan Steain, James A Triccas, Stuart Grant Turville, Joel Mackay, Toby Passioura, Richard J Payne
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Substituted 1-methyl-4-phenylpyrrolidin-2-ones – Fragment-based design of N-methylpyrrolidone-derived bromodomain inhibitors
JP Hilton-Proctor, O Ilyichova, Z Zheng, IG Jennings, RW Johnstone, J Shortt, SJ Mountford, MJ Scanlon, PE Thompson
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Novel approaches for producing purified active recombinant human proteases, and the inability of dipeptidyl peptidase-4 to bind SARS-CoV-2 spike protein
C Xi, A Di Fazio, N Nadvi, M Xiang, H Zhang, C Deshpande, X Wang, Y Chen, B Osborne, M Tabar, X Wang, C Bailey, K Patel, J Mackay, G Mccaughan, B Church, M Gorrell
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Be a Catalyst for Change: Breaking Down Barriers to Maximise Australian Female Talent in Chemistry
Anitha Kopinathan, Lucy Weaver and Katherine Locock
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Merozoite surface protein 2 adsorbed onto acetalated dextran microparticles for malaria vaccination
Rebeca T.Stiepela, Cole J.Batty Christopher A.MacRaild, Raymond S.Norton, EricBacheldera, Kristy M.Ainslieade
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Altered conformational sampling along an evolutionary trajectory changes the catalytic activity of an enzyme
Kaczmarski JA, Mahawaththa MC, Feintuch A, Clifton BE, Adams LA, Goldfarb D, Otting G & Jackson CJ
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Cyclic peptides can engage a single binding pocket through highly divergent modes
Patel K, Walport LJ, Walshe JL, Solomon PD, Low JKK, Tran DH, Mouradian KS, Silva APG, Wilkinson-White L, Norman A, Franck C, Matthews JM, Guss JM, Payne RJ, Passioura T, Suga H, Mackay JP
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Personal Accounts of Australian Drug Discovery at the Public–Private Interface
Baell J
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Investigation of thiazolyl–benzothiophenamides as potential agents for African sleeping sickness
Brown RW, Abdel-Megeed AM, Keller PA, Jones AJ, Sykes ML, Kaiser M, Baell J, Avery VM, Hyland CJT
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A novel purification procedure for active recombinant human DPP4 and the inability of DPP4 to bind SARS-CoV-2
Xi CR, Di Fazio A, Nadvi NA, Patel K, Xiang MSW, Zhang HE, Deshpande C, Low JKK, Wang XT, Chen Y, Osborne B, Vieira de Ribeiro AJ, McCaughan GW, Church WB, Mackay JP, Gorrell MD
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NMR in pharmaceutical discovery and development
Norton RS, Jahnke W
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NMR fragment screening reveals a novel small molecule binding site near the catalytic surface of the disulfide–dithiol oxidoreductase enzyme DsbA from Burkholderia pseudomallei
Nebl S, Alwan WS, Williams ML, Sharma G, Taylor A, Doak BC, Wilde KL, McMahon RM, Halili MA, Martin JL, Capuano B, Fenwick RB, Mohanty B, Scanlon MJ
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The voltage-gated potassium channel KV1.3 as a therapeutic target for venom-derived peptides
Tajti G, Wai DCC, Panyi G, Norton RS
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Improving membrane permeation in the beyond rule-of-five space by using prodrugs to mask hydrogen bond donors
Barlow N, Chalmers DK, Williams-Noonan BJ, Thompson PE, Norton RS
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The novel P2X7 receptor antagonist PKT100 improves cardiac function and survival in pulmonary hypertension by direct targeting of the right ventricle
Hansen T, Karimi Galougahi K, Besnier M, Genetzakis E, Tsang M, Finemore M, O’Brien-Brown J, Di Bartolo BA, Kassiou M, Bubb KJ, Figtree GA
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Rapid elaboration of fragments into leads by X-ray crystallographic screening of parallel chemical libraries (REFiLx)
Bentley MR, Ilyichova OV, Wang G, Williams ML, Sharma G, Alwan WS, Whitehouse RL, Mohanty B, Scammells PJ, Heras B, Martin JL, Totsika M, Capuano B, Doak BC, Scanlon MJ
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A structurally minimized yet fully active insulin based on cone-snail venom insulin principles
Xiong X, Menting JG, Disotuar MM, Smith NA, Delaine CA, Ghabash G, Agrawal R, Wang X, He X, Fisher SJ, MacRaild CA, Norton RS, Gajewiak J, Forbes BE, Smith BJ, Safavi-Hemami H, Olivera B, Lawrence MC, Chou DH
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Hit-to-lead optimization of novel benzimidazole phenylacetamides as broad spectrum trypanosomacides
McNamara N, Rahmani R, Sykes ML, Avery VM, Baell J
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Modulation of lymphocyte potassium channel KV1.3 by membrane-penetrating, joint-targeting immunomodulatory plant defensin
Ong ST, Bajaj S, Tanner MR, Chang SC, Krishnarjuna B, Ng XR, Morales RAV, Chen MW, Luo D, Patel D, Yasmin S, Ng JJH, Zhuang Z, Nguyen HM, El Sahili A, Lescar J, Patil R, Charman SA, Robins EG, Goggi JL, Tan PW, Sadasivam P, Ramasamy B, Hartimath SV, Dhawan V, Bednenko J, Colussi P, Wulff H, Pennington MW, Kuyucak S, Norton RS, Beeton C, Chandy KG
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Structure–activity relationship study reveals the molecular basis for specific sensing of hydrophobic amino acids by the Campylobacter jejuni chemoreceptor Tlp3
Khan MF, Machuca MA, Rahman MM, Koç C, Norton RS, Smith BJ, Roujeinikova A
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Rapid elaboration of fragments into leads applied to Bromodomain-3 extra terminal domain
Adams LA, Wilkinson-White LE, Gunzburg MJ, Headey SJ, Scanlon MJ, Capuano B, Mackay JP, Doak BC
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2019

The fragment-based development of a benzofuran hit as a new class of Escherichia coli DsbA inhibitors
Duncan L, Wang G, Ilyichova OV, Scanlon MJ, Heras BM, Abbott B
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Peppy: A virtual reality environment for exploring the principles of polypeptide structure
Doak DG, Denyer GS, Gerrard JA, Mackay JP, Allison JR
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The stoichiometry and interactome of the Nucleosome Remodeling and Deacetylase (NuRD) complex are conserved across multiple cell lines
Tabar MS, Mackay JP, Low JKK
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