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

2022

A Biodistribution Study of the Radiolabeled Kv1.3-Blocking Peptide DOTA-HsTX1[R14A] Demonstrates Brain Uptake in a Mouse Model of Neuroinflammation Reddiar, S.B., De Veer, M., Paterson, B.M., Sepehrizadeh, T., Wai, D.C.C., Csoti, A., Panyi, G., Nicolazzo, J.A., Norton, R.S. View here

A Fluorescent Peptide Toxin for Selective Visualization of the Voltage-Gated Potassium Channel KV1.3 Wai, D.C.C., Naseem, M.U., Mocsár, G., Babu Reddiar, S., Pan, Y., Csoti, A., Hajdu, P., Nowell, C., Nicolazzo, J.A., Panyi, G., Norton, R.S. View here

A peptide toxin in ant venom mimics vertebrate EGF-like hormones to cause long-lasting hypersensitivity in mammals Eagles, D.A., Saez, N.J., Krishnarjuna, B., Bradford, J.J., Chin, Y.K.-Y., Starobova, H., Mueller, A., Reichelt, M.E., Undheim, E.A.B., Norton, R.S., Thomas, W.G., Vetter, I., King, G.F., Robinson, S.D. View here

Biomarker discovery and development for frontotemporal dementia and amyotrophic lateral sclerosis Katzeff, J.S., Bright, F., Phan, K., Kril, J.J., Ittner, L.M., Kassiou, M., Hodges, J.R., Piguet, O., Kiernan, M.C., Halliday, G.M., Kim, W.S. 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

Development and clinical translation of P2X7 receptor antagonists: A potential therapeutic target in coronary artery disease? Genetzakis, E., Gilchrist, J., Kassiou, M., Figtree, G.A. View here

Development of 1,2,4-Oxadiazole Antimicrobial Agents to Treat Enteric Pathogens within the Gastrointestinal Tract Pitcher, N.P., Harjani, J.R., Zhao, Y., Jin, J., Knight, D.R., Li, L., Putsathit, P., Riley, T.V., Carter, G.P., Baell, J.B. View here

Differential mitochondrial protein interaction profile between human translocator protein and its A147T polymorphism variant Asih, P.R., Poljak, A., Kassiou, M., Ke, Y.D., Ittner, L.M. View here

Discovery of Anti-tubercular Analogues of Bedaquiline with Modified A-, B- and C-Ring Subunits Barbaro, L., Nagalingam, G., Triccas, J.A., Tan, L., West, N.P., Priebbenow, D.L., Baell, J.B. View here

Electrochemical Synthesis of Polysubstituted Sulfonated Pyrazoles via Cascade Intermolecular Condensation, Radical-Radical Cross Coupling Sulfonylation, and Pyrazole Annulation Feng, J., Wang, Y., Gao, L., Yu, Y., Baell, J.B., Huang, F. View here

Enhanced nitric oxide production by macrophages treated with a cell-penetrating peptide conjugate Rahman, A., Matthews, M.A., Nowell, C.J., Chalmers, D.K., Thompson, P.E., Nicholson, S.E., Barlow, N., Norton, R.S. View here

Expression, purification and characterization of the suppressor of copper sensitivity (Scs) B membrane protein from Proteus mirabilis Jarrott, R.J., Furlong, E.J., Petit, G.A., Drew, D., Martin, J.L., Halili, M.A. View here

Fragment screening libraries for the identification of protein hot spots and their minimal binding pharmacophores Whitehouse, R.L., Alwan, W.S., Ilyichova, O.V., Taylor, A.J., Chandrashekaran, I.R., Mohanty, B., Doak, B.C., Scanlon, M.J. View here

Hit-to-lead optimization of novel phenyl imidazole carboxamides that are active against Leishmania donovani McNamara, N., Saunders, E., Varghese, S., Zheng, R., Simpson, K., Varma, D.M., Johnson, M.M., Hasan Zahid, M.S., Bachelder, E.M., Ainslie, K.M., No, J.H., Koh, D., Shum, D., Das, N., Patra, B., Roy, J., Talukdar, A., Ganguly, D., McConville, M., Baell, J. View here

Identification and characterization of two drug-like fragments that bind to the same cryptic binding pocket of Burkholderia pseudomallei DsbA Petit, G.A., Mohanty, B., McMahon, R.M., Nebl, S., Hilko, D.H., Wilde, K.L., Scanlon, M.J., Martin, J.L., Halili, M.A. View here

IGF-dependent dynamic modulation of a protease cleavage site in the intrinsically disordered linker domain of human IGFBP2 Jaipuria, G., Shet, D., Malik, S., Swain, M., Atreya, H.S., Galea, C.A., Slomiany, M.G., Rosenzweig, S.A., Forbes, B.E., Norton, R.S., Mondal, S. View here

Interferon-γ primes macrophages for pathogen ligand-induced killing via a caspase-8 and mitochondrial cell death pathway Simpson, D.S., Pang, J., Weir, A., Kong, I.Y., Fritsch, M., Rashidi, M., Cooney, J.P., Davidson, K.C., Speir, M., Djajawi, T.M., Hughes, S., Mackiewicz, L., Dayton, M., Anderton, H., Doerflinger, M., Deng, Y., Huang, A.S., Conos, S.A., Tye, H., Chow, S.H., Rahman, A., Norton, R.S., Naderer, T., Nicholson, S.E., Burgio, G., Man, S.M., Groom, J.R., Herold, M.J., Hawkins, E.D., Lawlor, K.E., Strasser, A., Silke, J., Pellegrini, M., Kashkar, H., Feltham, R., Vince, J.E. view here

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

Mechanism of Bloom syndrome complex assembly required for double Holliday junction dissolution and genome stability Hodson, C., Low, J.K.K., van Twest, S., Jones, S.E., Swuec, P., Murphy, V., Tsukada, K., Fawkes, M., Bythell-Douglas, R., Davies, A., Holien, J.K., O’Rourke, J.J., Parker, B.L., Glaser, A., Parker, M.W., Mackay, J.P., Blackford, A.N., Costa, A., Deans, A.J. View here

Membrane Permeating Macrocycles: Design Guidelines from Machine Learning Williams-Noonan, B.J., Speer, M.N., Le, T.C., Sadek, M.M., Thompson, P.E., Norton, R.S., Yuriev, E., Barlow, N., Chalmers, D.K., Yarovsky, I. View here

Methyl probes in proteins for determining ligand binding mode in weak protein–ligand complexes Mohanty, B., Orts, J., Wang, G., Nebl, S., Alwan, W.S., Doak, B.C., Williams, M.L., Heras, B., Mobli, M., Scanlon, M.J. View here

Molecular architecture of nucleosome remodeling and deacetylase sub-complexes by integrative structure determination Arvindekar, S., Jackman, M.J., Low, J.K.K., Landsberg, M.J., Mackay, J.P., Viswanath, S. View here

Mucosal TLR2-activating protein-based vaccination induces potent pulmonary immunity and protection against SARS-CoV-2 in mice Ashhurst, A.S., Johansen, M.D., Maxwell, J.W.C., Stockdale, S., Ashley, C.L., Aggarwal, A., Siddiquee, R., Miemczyk, S., Nguyen, D.H., Mackay, J.P., Counoupas, C., Byrne, S.N., Turville, S., Steain, M., Triccas, J.A., Hansbro, P.M., Payne, R.J., Britton, W.J. View here

Novel plasma protein binding analysis method for a PET tracer and its radiometabolites: A case study with [11C]SMW139 to explain the high uptake of radiometabolites in mouse brain Aarnio, R., Alzghool, O.M., Wahlroos, S., O’Brien-Brown, J., Kassiou, M., Solin, O., Rinne, J.O., Forsback, S., Haaparanta-Solin, M. View here

Novel small molecules that increase the susceptibility of Neisseria gonorrhoeae to cationic antimicrobial peptides by inhibiting lipid A phosphoethanolamine transferase Mullally, C., Stubbs, K.A., Thai, V.C., Anandan, A., Bartley, S., Scanlon, M.J., Jarvis, G.A., John, C.M., Lim, K.Y.L., Sullivan, C.M., Sarkar-Tyson, M., Vrielink, A., Kahler, C.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

Porous Silicon Nanocarriers with Stimulus-Cleavable Linkers for Effective Cancer Therapy Xue, Y., Bai, H., Peng, B., Tieu, T., Jiang, J., Hao, S., Li, P., Richardson, M., Baell, J., Thissen, H., Cifuentes, A., Li, L., Voelcker, N.H. View here

Purinergic P2X7Receptor: A Therapeutic Target in Amyotrophic Lateral Sclerosis McKenzie, A.D.J., Garrett, T.R., Werry, E.L., Kassiou, M. View here

Quantification of the purinergic P2X7 receptor with [11C]SMW139 improves through correction for brain-penetrating radiometabolites Brumberg, J., Aarnio, R., Forsberg, A., Marjamäki, P., Kerstens, V., Moein, M.M., Nag, S., Wahlroos, S., Kassiou, M., Windhorst, A.D., Halldin, C., Haaparanta-Solin, M., Fazio, P., Oikonen, V., Rinne, J.O., Varrone, A. View here

Recent Scaffold Hopping Applications in Central Nervous System Drug Discovery Callis, T.B., Garrett, T.R., Montgomery, A.P., Danon, J.J., Kassiou, M. View here

RNA inhibits dMi-2/CHD4 chromatin binding and nucleosome remodeling Ullah, I., Thölken, C., Zhong, Y., John, M., Rossbach, O., Lenz, J., Gößringer, M., Nist, A., Albert, L., Stiewe, T., Hartmann, R., Vázquez, O., Chung, H.-R., Mackay, J.P., Brehm, A. 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, M.L., Doak, B.C., Dhouib, R., Totsika, M., McMahon, R.M., Sharma, G., Zheng, D., Bentley, M.R., Ka-Yan Chin, Y., Horne, J., Chalmers, D.K., Heras, B., Scanlon, M.J. View here

Site-selective photocatalytic functionalization of peptides and proteins at selenocysteine Dowman, L.J., Kulkarni, S.S., Alegre-Requena, J.V., Giltrap, A.M., Norman, A.R., Sharma, A., Gallegos, L.C., Mackay, A.S., Welegedara, A.P., Watson, E.E., van Raad, D., Niederacher, G., Huhmann, S., Proschogo, N., Patel, K., Larance, M., Becker, C.F.W., Mackay, J.P., Lakhwani, G., Huber, T., Paton, R.S., Payne, R.J. View here

Strategies for targeting the P2Y12 receptor in the central nervous system Ma, B.B., Montgomery, A.P., Chen, B., Kassiou, M., Danon, J.J. 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

Structure-function analysis of the AMPK activator SC4 and identification of a potent pan AMPK activator Ovens, A.J., Gee, Y.S., Ling, N.X.Y., Yu, D., Hardee, J.P., Chung, J.D., Ngoei, K.R.W., Waters, N.J., Hoffman, N.J., Scott, J.W., Loh, K., Spengler, K., Heller, R., Parker, M.W., Lynch, G.S., Huang, F., Galic, S., Kemp, B.E., Baell, J.B., Oakhill, J.S., Langendorf, C.G. View here

Target 2035-update on the quest for a probe for every protein Müller, S., Ackloo, S., Al Chawaf, A., Al-Lazikani, B., Antolin, A., Baell, J.B., Beck, H., Beedie, S., Betz, U.A.K., Bezerra, G.A., Brennan, P.E., Brown, D., Brown, P.J., Bullock, A.N., Carter, A.J., Chaikuad, A., Chaineau, M., Ciulli, A., Collins, I., Dreher, J., Drewry, D., Edfeldt, K., Edwards, A.M., Egner, U., Frye, S.V., Fuchs, S.M., Hall, M.D., Hartung, I.V., Hillisch, A., Hitchcock, S.H., Homan, E., Kannan, N., Kiefer, J.R., Knapp, S., Kostic, M., Kubicek, S., Leach, A.R., Lindemann, S., Marsden, B.D., Matsui, H., Meier, J.L., Merk, D., Michel, M., Morgan, M.R., Mueller-Fahrnow, A., Owen, D.R., Perry, B.G., Rosenberg, S.H., Saikatendu, K.S., Schapira, M., Scholten, C., Sharma, S., Simeonov, A., Sundström, M., Superti-Furga, G., Todd, M.H., Tredup, C., Vedadi, M., Von Delft, F., Willson, T.M., Winter, G.E., Workman, P., Arrowsmith, C.H. View here

Targeting cell cycle and apoptosis to overcome chemotherapy resistance in acute myeloid leukemia Ling, V.Y., Straube, J., Godfrey, W., Haldar, R., Janardhanan, Y., Cooper, L., Bruedigam, C., Cooper, E., Tavakoli Shirazi, P., Jacquelin, S., Tey, S.-K., Baell, J., Huang, F., Jin, J., Zhao, Y., Bullinger, L., Bywater, M.J., Lane, S.W. View here

The acetyltransferase KAT7 is required for thymic epithelial cell expansion, expression of AIRE target genes, and thymic tolerance Heinlein, M., Gandolfo, L.C., Zhao, K., Teh, C.E., Nguyen, N., Baell, J.B., Goldfarb, Y., Abramson, J., Wichmann, J., Voss, A.K., Strasser, A., Smyth, G.K., Thomas, T., Gray, D.H.D. View here

The Design, Synthesis, and Evaluation of Novel 9-Arylxanthenedione-Based Allosteric Modulators for the δ -Opioid Receptor Deo, O., Alvi, S., Pham, V., Christopoulos, A., Thal, D.M., Jörg, M., Capuano, B., Valant, C., Scammells, P.J. View here

The role of auxiliary domains in modulating CHD4 activity suggests mechanistic commonality between enzyme families Zhong, Y., Moghaddas Sani, H., Paudel, B.P., Low, J.K.K., Silva, A.P.G., Mueller, S., Deshpande, C., Panjikar, S., Reid, X.J., Bedward, M.J., van Oijen, A.M., Mackay, J.P. View here

The suppressor of copper sensitivity protein C from Caulobacter crescentus is a trimeric disulfide isomerase that binds copper(I) with subpicomolar affinity Petit, G.A., Hong, Y., Djoko, K.Y., Whitten, A.E., Furlong, E.J., McCoy, A.J., Gulbis, J.M., Totsika, M., Martin, J.L., Halili, M.A. View here

TNP Analogues Inhibit the Virulence Promoting IP3-4 Kinase Arg1 in the Fungal Pathogen Cryptococcus neoformans Desmarini, D., Truong, D., Wilkinson-White, L., Desphande, C., Torrado, M., Mackay, J.P., Matthews, J.M., Sorrell, T.C., Lev, S., Thompson, P.E., Djordjevic, J.T. View here

Toxicon and Toxicon: X – 2022 and beyond Norton, R.S., Tambourgi, D.V. View here

Tracer development for PET imaging of proteinopathies Kallinen, A., 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

Understanding In Vitro Pathways to Drug Discovery for TDP-43 Proteinopathies Cheng, H.W.A., Callis, T.B., Montgomery, A.P., Danon, J.J., Jorgensen, W.T., Ke, Y.D., Ittner, L.M., Werry, E.L., Kassiou, 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