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 View here

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 View here

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 View here

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 View here

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 View research paper here

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 View research paper here

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 View research paper here

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 View research paper here

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 View paper here

Carbonic anhydrase XII inhibition overcomes P-glycoprotein-mediated drug resistance: a potential new combination therapy in cancer Kathryn F. Tonissen, Sally-Ann Poulsen View research paper here

Early career research in medicinal chemistry Jonathan B Baell View paper here

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 View research paper here

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 View research paper here

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 View research paper here

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 View research paper here

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 View research paper here

Be a Catalyst for Change: Breaking Down Barriers to Maximise Australian Female Talent in Chemistry Anitha Kopinathan, Lucy Weaver and Katherine Locock View paper here

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 View research paper here

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 View research paper here

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 View research paper here

Personal Accounts of Australian Drug Discovery at the Public–Private Interface Baell J View paper here

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 View research paper here

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 View research paper here

NMR in pharmaceutical discovery and development Norton RS, Jahnke W View research paper here

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 View research paper here

The voltage-gated potassium channel KV1.3 as a therapeutic target for venom-derived peptides Tajti G, Wai DCC, Panyi G, Norton RS View research paper here

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 View research paper here

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 View research paper here

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 View research paper here

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 View research paper here

Hit-to-lead optimization of novel benzimidazole phenylacetamides as broad spectrum trypanosomacides McNamara N, Rahmani R, Sykes ML, Avery VM, Baell J View research paper here

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 View research paper here

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 View research paper here

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 View research paper here | Read blog post here

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 View research paper here

Peppy: A virtual reality environment for exploring the principles of polypeptide structure Doak DG, Denyer GS, Gerrard JA, Mackay JP, Allison JR View research paper here

The stoichiometry and interactome of the Nucleosome Remodeling and Deacetylase (NuRD) complex are conserved across multiple cell lines Tabar MS, Mackay JP, Low JKK View research paper here