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

2021

Prodromal neuroinflammatory, cholinergic and metabolite dysfunction detected by PET and MRS in the TgF344-AD transgenic rat model of AD: A collaborative multi-modal study Chaney, A.M., Lopez-Picon, F.R., Serrière, S., Wang, R., Bochicchio, D., Webb, S.D., Vandesquille, M., Harte, M.K., Georgiadou, C., Lawrence, C., Busson, J., Vercouillie, J., Tauber, C., Buron, F., Routier, S., Reekie, T., Snellman, A., Kassiou, M., Rokka, J., Davies, K.E., Rinne, J.O., Salih, D.A., Edwards, F.A., Orton, L.D., Williams, S.R., Chalon, S., Boutin, H. View here

Guiding the immune response to a conserved epitope in msp2, an intrinsically disordered malaria vaccine candidate Seow, J., Das, S.C., Morales, R.A.V., Ataide, R., Krishnarjuna, B., Silk, M., Chalmers, D.K., Richards, J., Anders, R.F., Macraild, C.A., Norton, R.S. View here

Tentacle morphological variation coincides with differential expression of toxins in sea anemones Ashwood, L.M., Mitchell, M.L., Madio, B., Hurwood, D.A., King, G.F., Undheim, E.A.B., Norton, R.S., Prentis, P.J. View here

Enantioenriched positive allosteric modulators display distinct pharmacology at the dopamine d1 receptor Fyfe, T.J., Scammells, P.J., Lane, J.R., Capuano, B. View here

The Glitazone Class of Drugs as Carbonic Anhydrase Inhibitors-A Spin-Off Discovery from Fragment Screening Mueller SL, Chrysanthopoulos PK, Halili MA, Hepburn C, Nebl T, Supuran CT, Nocentini A, Peat TS, Poulsen SA View here

Senolytics: A Novel Strategy for Neuroprotection in ALS? Maximova, A., Werry, E.L., Kassiou, M. View here

Dyrk1a negatively regulates cdk5-sox2 pathway and self-renewal of glioblastoma stem cells Chen, B., McCuaig-Walton, D., Tan, S., Montgomery, A.P., Day, B.W., Kassiou, M., Munoz, L., Recasens, A. View here

Identification, synthesis, conformation and activity of an insulin‐like peptide from a sea anemone Mitchell, M.L., Hossain, M.A., Lin, F., Pinheiro‐junior, E.L., Peigneur, S., Wai, D.C.C., Delaine, C., Blyth, A.J., Forbes, B.E., Tytgat, J., Wade, J.D., Norton, R.S. View here

The Nature of Diamino Linker and Halogen Bonding Define Selectivity of Pyrrolopyrimidine-Based LIMK1 Inhibitors Ariawan, D., Au, C., Paric, E., Fath, T., Ke, Y.D., Kassiou, M., van Eersel, J., Ittner, L.M. View here

The novel bis-1,2,4-Triazine MIPS-0004373 demonstrates rapid and potent activity against all blood stages of the malaria parasite Ellis, K.M., Lucantoni, L., Chavchich, M., Abraham, M., De Paoli, A., Luth, M.R., Zeeman, A.-M., Delves, M.J., Terán, F.S.-R., Straschil, U., Baum, J., Kocken, C.H.M., Ralph, S.A., Winzeler, E.A., Avery, V.M., Edstein, M.D., Baell, J.B., Creek, D.J. View here

Drug repurposing: Misconceptions, challenges, and opportunities for academic researchers Begley, C.G., Ashton, M., Baell, J., Bettess, M., Brown, M.P., Carter, B., Charman, W.N., Davis, C., Fisher, S., Frazer, I., Gautam, A., Jennings, M.P., Kearney, P., Keeffe, E., Kelly, D., Lopez, A.F., McGuckin, M., Parker, M.W., Rayner, C., Roberts, B., Rush, J.S., Sullivan, M. View here

Unique protein interaction networks define the chromatin remodelling module of the NuRD complex Sharifi Tabar, M., Giardina, C., Feng, Y., Francis, H., Moghaddas Sani, H., Low, J.K.K., Mackay, J.P., Bailey, C.G., Rasko, J.E.J. View here

Identification and characterization of two drug-like fragments that bind to the same cryptic binding pocket of Burkholderia pseudomallei DsbA Petit GA, Mohanty B, McMahon RM, Nebl S, Hilko DH, Wilde KL, Scanlon MJ, Martin JL, Halili MA View here

Cannabis and Cannabinoids Duggan, P.J., Kassiou, M. View here

Adventures in Translocation: Studies of the Translocator Protein (TSPO) 18 kDa Danon, J.J., Tregeagle, D.F.L., Kassiou, M. View here

Late-stage modification of peptides and proteins at cysteine with diaryliodonium salts Byrne, S.A., Bedding, M.J., Corcilius, L., Ford, D.J., Zhong, Y., Franck, C., Larance, M., Mackay, J.P., Payne, R.J. View here

Synthesis and antitumour evaluation of indole-2-carboxamides against paediatric brain cancer cells Alsayed, S.S.R., Suri, A., Bailey, A.W., Lane, S., Werry, E.L., Huang, C.-C., Yu, L.-F., Kassiou, M., Sredni, S.T., Gunosewoyo, H. View here

The characterization of protein interactions-what, how and how much? Walport, L.J., Low, J.K.K., Matthews, J.M., Mackay, J.P. View here

Stimulus-cleavable chemistry in the field of controlled drug delivery Xue, Y., Bai, H., Peng, B., Fang, B., Baell, J., Li, L., Huang, W., Voelcker, N.H. View here

A binge high sucrose diet provokes systemic and cerebral inflammation in rats without inducing obesity Patkar, O.L., Mohamed, A.Z., Narayanan, A., Mardon, K., Cowin, G., Bhalla, R., Stimson, D.H.R., Kassiou, M., Beecher, K., Belmer, A., Alvarez Cooper, I., Morgan, M., Hume, D.A., Irvine, K.M., Bartlett, S.E., Nasrallah, F., Cumming, P. View here

A single dose, BCG-adjuvanted COVID-19 vaccine provides sterilising immunity against SARS-CoV-2 infection Counoupas, C., Johansen, M.D., Stella, A.O., Nguyen, D.H., Ferguson, A.L., Aggarwal, A., Bhattacharyya, N.D., Grey, A., Hutchings, O., Patel, K., Siddiquee, R., Stewart, E.L., Feng, C.G., Hansbro, N.G., Palendira, U., Steain, M.C., Saunders, B.M., Low, J.K.K., Mackay, J.P., Kelleher, A.D., Britton, W.J., Turville, S.G., Hansbro, P.M., Triccas, J.A. View here

Global phosphoproteomics reveals DYRK1A regulates CDK1 activity in glioblastoma cells Recasens, A., Humphrey, S.J., Ellis, M., Hoque, M., Abbassi, R.H., Chen, B., Longworth, M., Needham, E.J., James, D.E., Johns, T.G., Day, B.W., Kassiou, M., Yang, P., Munoz, L. View here

Structural Features of Iperoxo-BQCA Muscarinic Acetylcholine Receptor Hybrid Ligands Determining Subtype Selectivity and Efficacy Wakeham, M.C.L., Davie, B.J., Chalmers, D.K., Christopoulos, A., Capuano, B., Valant, C., Scammells, P.J. View here

Discovery of Cyclic Peptide Ligands to the SARS-CoV-2 Spike Protein Using mRNA Display Norman, A., Franck, C., Christie, M., Hawkins, P.M.E., Patel, K., Ashhurst, A.S., Aggarwal, A., Low, J.K.K., Siddiquee, R., Ashley, C.L., Steain, M., Triccas, J.A., Turville, S., Mackay, J.P., Passioura, T., Payne, R.J. View here

Alkyne-Bridged α-Conotoxin Vc1.1 Potently Reverses Mechanical Allodynia in Neuropathic Pain Models Belgi, A., Burnley, J.V., MacRaild, C.A., Chhabra, S., Elnahriry, K.A., Robinson, S.D., Gooding, S.G., Tae, H.-S., Bartels, P., Sadeghi, M., Zhao, F.-Y., Wei, H., Spanswick, D., Adams, D.J., Norton, R.S., Robinson, A.J. View here

1-Methyl-1 H-pyrazole-5-carboxamide Derivatives Exhibit Unexpected Acute Mammalian Toxicity Preston, S., Garcia-Bustos, J., Hall, L.G., Martin, S.D., Le, T.G., Kundu, A., Ghoshal, A., Nguyen, N.H., Jiao, Y., Ruan, B., Xue, L., Huang, F., Chang, B.C.H., McGee, S.L., Wells, T.N.C., Palmer, M.J., Jabbar, A., Gasser, R.B., Baell, J.B. View here

Structure-Guided Development of Potent Benzoylurea Inhibitors of BCL-XLand BCL-2 Roy, M.J., Vom, A., Okamoto, T., Smith, B.J., Birkinshaw, R.W., Yang, H., Abdo, H., White, C.A., Segal, D., Huang, D.C.S., Baell, J.B., Colman, P.M., Czabotar, P.E., Lessene, G. View here

Blockade of Microglial Kv1.3 Potassium Channels by the Peptide HsTX1[R14A] Attenuates Lipopolysaccharide-mediated Neuroinflammation Nicolazzo, J.A., Pan, Y., Di Stefano, I., Choy, K.H.C., Reddiar, S.B., Low, Y.L., Wai, D.C.C., Norton, R.S., Jin, L. View here

Prolonged Plasma Exposure of the Kv1.3-Inhibitory Peptide HsTX1[R14A] by Subcutaneous Administration of a Poly(Lactic-co-Glycolic Acid) (PLGA) Microsphere Formulation Jin, L., Pan, Y., Pham, A.C., Boyd, B.J., Norton, R.S., Nicolazzo, J.A. View here

Conformational dynamics in peptide toxins: Implications for receptor interactions and molecular design Sanches, K., Wai, D.C.C., Norton, R.S. View here

Modulation of human T-type calcium channels by synthetic cannabinoid receptor agonists in vitro Bladen, C., Mirlohi, S., Santiago, M., Longworth, M., Kassiou, M., Banister, S., Connor, M. View here

A disulfide-stabilised helical hairpin fold in acrorhagin I: An emerging structural motif in peptide toxins Krishnarjuna, B., Sunanda, P., Villegas-Moreno, J., Csoti, A., A.V. Morales, R., Wai, D.C.C., Panyi, G., Prentis, P., Norton, R.S. View here

Conformational Flexibility of A Highly Conserved Helix Controls Cryptic Pocket Formation in FtsZ Alnami, A., Norton, R.S., Pena, H.P., Haider, S., Kozielski, F. View here

Purification of an insect juvenile hormone receptor complex enables insights into its post-translational phosphorylation Jindra M, McKinstry WJ, Nebl T, Bittova L, Ren B, Shaw J, Phan T, Lu L, Low JKK, Mackay JP, Sparrow LG, Lovrecz GO, Hill RJ. View here

Binding of a pyrimidine RNA base-mimic to SARS-CoV-2 nonstructural protein 9 Littler, D.R., Mohanty, B., Lowery, S.A., Colson, R.N., Gully, B.S., Perlman, S., Scanlon, M.J., Rossjohn, J. View here

Merozoite surface protein 2 adsorbed onto acetalated dextran microparticles for malaria vaccination Stiepel, R.T., Batty, C.J., MacRaild, C.A., Norton, R.S., Bachelder, E., Ainslie, K.M. View here

Pharmacological characterization of a structural hybrid P2X7R antagonist using ATP and LL-37 Jackson, A., Werry, E.L., O’Brien-Brown, J., Schiavini, P., Wilkinson, S., Wong, E.C.N., McKenzie, A.D.J., Maximova, A., Kassiou, M. View here

Tobramycin and Colistin display anti-inflammatory properties in CuFi-1 cystic fibrosis cell line Sheikh, Z., Bradbury, P., Reekie, T.A., Pozzoli, M., Robinson, P.D., Kassiou, M., Young, P.M., Ong, H.X., Traini, D. View here

Development of [18F]MIPS15692, a radiotracer with in vitro proof-of-concept for the imaging of MER tyrosine kinase (MERTK) in neuroinflammatory disease Wong, S.W., Vivash, L., Mudududdla, R., Nguyen, N., Hermans, S.J., Shackleford, D.M., Field, J., Xue, L., Aprico, A., Hancock, N.C., Haskali, M., Stashko, M.A., Frye, S.V., Wang, X., Binder, M.D., Ackermann, U., Parker, M.W., Kilpatrick, T.J., Baell, J.B. View here

The discovery of a potent and selective pyrazolo-[2,3-e]-[1,2,4]-triazine cannabinoid type 2 receptor agonist Moir, M., Lane, S., Montgomery, A.P., Hibbs, D., Connor, M., Kassiou, M. View here

Elaboration of a benzofuran scaffold and evaluation of binding affinity and inhibition of Escherichia coli DsbA: A fragment-based drug design approach to novel antivirulence compounds Duncan, L.F., Wang, G., Ilyichova, O.V., Dhouib, R., Totsika, M., Scanlon, M.J., Heras, B., Abbott, B.M. View here

Assessing the cellular toxicity of peptide inhibitors of intracellular protein-protein interactions by microinjection Babu Reddiar, S., Al-Wassiti, H., Pouton, C.W., Nowell, C.J., Matthews, M.A., Rahman, A., Barlow, N., Norton, R.S. View here

MerTK activity is not necessary for the proliferation of glioblastoma stem cells Hoque, M., Wai Wong, S., Recasens, A., Abbassi, R., Nguyen, N., Zhang, D., Stashko, M.A., Wang, X., Frye, S., Day, B.W., Baell, J., Munoz, L. View here

Measuring Affinity of Ligands to the Oxytocin Receptor Using Radioligand Binding Werry, E.L., Kassiou, M. View here

TSPO PET Imaging as a Biomarker of Neuroinflammation in Neurodegenerative Disorders Werry, E.L., Bright, F.M., Kassiou, M. View here

Selective binding of small molecules to Vibrio cholerae DsbA offers a starting point for the design of novel antibacterials Wang G, Mohanty B, Williams ML, Doak BC, Dhouib R, Totsika M, McMahon R, Sharma G, Zheng D, Bentley MR, Chin YK, Horne J, Chalmers DK, Heras B, Scanlon MJ View here

Development of AC265347-Inspired Calcium-Sensing Receptor Ago-Positive Allosteric Modulators Dinh, L.V., DeBono, A., Keller, A.N., Josephs, T.M., Gregory, K.J., Leach, K., Capuano, B. View here

1,3-Benzodioxole-Modified Noscapine Analogues: Synthesis, Antiproliferative Activity, and Tubulin-Bound Structure Yong, C., Devine, S.M., Abel, A.-C., Tomlins, S.D., Muthiah, D., Gao, X., Callaghan, R., Steinmetz, M.O., Prota, A.E., Capuano, B., Scammells, P.J. View here

Development of Novel 4-Arylpyridin-2-one and 6-Arylpyrimidin-4-one Positive Allosteric Modulators of the M1 Muscarinic Acetylcholine Receptor Jörg, M., Khajehali, E., van der Westhuizen, E.T., C. Choy, K.H., Shackleford, D.M., Tobin, A.B., Sexton, P.M., Valant, C., Capuano, B., Christopoulos, A., Scammells, P.J. View here

Structure-Activity Studies of Truncated Latrunculin Analogues with Antimalarial Activity Varghese, S., Rahmani, R., Drew, D.R., Beeson, J.G., Baum, J., Smith, B.J., Baell, J.B. View here

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