2021

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.
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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.
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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.
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Enantioenriched positive allosteric modulators display distinct pharmacology at the dopamine d1 receptor
Fyfe, T.J., Scammells, P.J., Lane, J.R., Capuano, B.
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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
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Senolytics: A Novel Strategy for Neuroprotection in ALS?
Maximova, A., Werry, E.L., Kassiou, M.
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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.
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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.
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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.
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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.
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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.
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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.
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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
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Cannabis and Cannabinoids
Duggan, P.J., Kassiou, M.
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Adventures in Translocation: Studies of the Translocator Protein (TSPO) 18 kDa
Danon, J.J., Tregeagle, D.F.L., Kassiou, M.
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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.
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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.
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The characterization of protein interactions-what, how and how much?
Walport, L.J., Low, J.K.K., Matthews, J.M., Mackay, J.P.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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Conformational dynamics in peptide toxins: Implications for receptor interactions and molecular design
Sanches, K., Wai, D.C.C., Norton, R.S.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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Measuring Affinity of Ligands to the Oxytocin Receptor Using Radioligand Binding
Werry, E.L., Kassiou, M.
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TSPO PET Imaging as a Biomarker of Neuroinflammation in Neurodegenerative Disorders
Werry, E.L., Bright, F.M., Kassiou, M.
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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
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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.
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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.
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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.
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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.
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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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