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2016

Enantiomeric two-armed lanthanide-binding tags for complementary effects in paramagnetic NMR spectroscopy

Lee, M. D., Dennis, M. L., Swarbrick, J. D. & Graham, B., 2016, In : Chemical Communications. 52, 51, p. 7954-7957 4 p.

Research output: Contribution to journalArticleResearchpeer-review

Extracellular loop 2 of the adenosine A1 receptor has a key role in orthosteric ligand affinity and agonist efficacy

Nguyen, A. T. N., Baltos, J-A., Thomas, T., Nguyen, T. D., Lopez Munoz, L., Gregory, K. J., White, P. J., Sexton, P. M., Christopoulos, A. & May, L. T., 1 Dec 2016, In : Molecular Pharmacology. 90, 6, p. 703-714 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Fatty acid-binding protein 5 at the blood–brain barrier regulates endogenous brain docosahexaenoic acid levels and cognitive function

Pan, Y., Short, J. L., Choy, K. H. C., Zeng, A. X., Marriott, P. J., Owada, Y., Scanlon, M. J., Porter, C. J. H. & Nicolazzo, J. A., 16 Nov 2016, In : Journal of Neuroscience. 36, 46, p. 11755-11767 13 p.

Research output: Contribution to journalArticleResearchpeer-review

Flipped classroom implementation: A case report of two higher education institutions in the United States and Australia

McLaughlin, J. E., White, P. J., Khanova, J. & Yuriev, E., 2016, In : Computers in the Schools. 33, 1, p. 24-37 14 p.

Research output: Contribution to journalArticleResearchpeer-review

Fragment based strategies for discovery of novel HIV-1 reverse transcriptase and integrase inhibitors

Latham, C. F., La, J., Tinetti, R. N., Chalmers, D. K. & Tachedjian, G., 2016, In : Current Topics in Medicinal Chemistry. 16, 10, p. 1135-1153 19 p.

Research output: Contribution to journalArticleResearchpeer-review

From sphingosine kinase to dihydroceramide desaturase: a structure-activity relationship (SAR) study of the enzyme inhibitory and anticancer activity of 4-((4-(4-chlorophenyl)thiazol-2-yl)amino)phenol (SKI-II)

Aurelio, L., Scullino, C. V., Pitman, M. R., Sexton, A. E., Oliver, V., Davies, L., Rebello, R. J., Furic, L., Creek, D. J., Pitson, S. M. & Flynn, B. L., 11 Feb 2016, In : Journal of Medicinal Chemistry. 59, 3, p. 965-984 20 p.

Research output: Contribution to journalArticleResearchpeer-review

Glyceride-mimetic prodrugs incorporating self-immolative spacers promote lymphatic transport, avoid first-pass metabolism, and enhance oral bioavailability

Hu, L., Quach, T., Han, S., Lim, S. F., Yadav, P., Senyschyn, D., Trevaskis, N. L., Simpson, J. S. & Porter, C. J. H., 2016, In : Angewandte Chemie - International Edition. 55, 44, p. 13700 –13705 6 p.

Research output: Contribution to journalArticleResearchpeer-review

Hit-to-lead optimization of a novel class of potent, broad-spectrum trypanosomacides

Russell, S., Rahmani, R., Jones, A. J., Newson, H. L., Neilde, K., Cotillo, I., Rahmani Khajouei, M., Ferrins, L., Qureishi, S., Nguyen, N., Martinez-Martinez, M. S., Weaver, D. F., Kaiser, M., Riley, J., Thomas, J., De Rycker, M., Read, K. D., Flematti, G. R., Ryan, E., Tanghe, S. & 6 othersRodriguez, A., Charman, S. A., Kessler, A., Avery, V. M., Baell, J. B. & Piggott, M. J., 10 Nov 2016, In : Journal of Medicinal Chemistry. 59, 21, p. 9686-9720 35 p.

Research output: Contribution to journalArticleResearchpeer-review

Identification of a cyanine-dye labeled peptidic ligand for Y1R and Y4R, based upon the neuropeptide y C-terminal analogue, BVD-15

Liu, M., Richardson, R. R., Mountford, S. J., Zhang, L., Tempone, M. H., Herzog, H., Holliday, N. D. & Thompson, P. E., 21 Sep 2016, In : Bioconjugate Chemistry. 27, 9, p. 2166-2175 10 p.

Research output: Contribution to journalArticleResearchpeer-review

Implications of the complete basis set limit in valence bond theory: a case study of molecular hydrogen

Duke, B. J. & Havenith, R. W. A., 1 Mar 2016, In : Theoretical Chemistry Accounts. 135, 3, 9 p., 82.

Research output: Contribution to journalArticleResearchpeer-review

Installation of a rigid EDTA-like motif into a protein α-helix for paramagnetic NMR spectroscopy with cobalt(II) ions

Swarbrick, J. D., Ung, P., Dennis, M. L., Lee, M. D., Chhabra, S. & Graham, B., 22 Jan 2016, In : Chemistry - A European Journal. 22, 4, p. 1228-1232 5 p.

Research output: Contribution to journalArticleResearchpeer-review

Legumain is activated in macrophages during pancreatitis

Edgington-Mitchell, L. E., Wartmann, T., Fleming, A. K., Gocheva, V., van der Linden, W. A., Withana, N. P., Verdoes, M., Aurelio, L., Edgington-Mitchell, D., Lieu, T., Parker, B. S., Graham, B., Reinheckel, T., Furness, J. B., Joyce, J. A., Storz, P., Halangk, W., Bogyo, M. & Bunnett, N. W., Sep 2016, In : American Journal of Physiology - Gastrointestinal and Liver Physiology. 311, 3, p. G548-G560 13 p.

Research output: Contribution to journalArticleResearchpeer-review

Ligand binding pathways of clozapine and haloperidol in the dopamine D2 and D3 receptors

Thomas, T., Yuriev, E. & Chalmers, D. K., 22 Feb 2016, In : Journal of Chemical Information and Modeling. 56, 2, p. 308-321 14 p.

Research output: Contribution to journalArticleResearchpeer-review

Luminescent alkyne-bearing terbium(III) complexes and their application to bioorthogonal protein labeling

O'Malley, W., Abdelkader, E. H., Aulsebrook, M., Rubbiani, R., Loh, C. T., Grace, M., Spiccia, L., Gasser, G., Otting, G., Tuck, K. & Graham, B., 15 Feb 2016, In : Inorganic Chemistry. 55, 4, p. 1674-1682 9 p.

Research output: Contribution to journalArticleResearchpeer-review

Lymphatic transport and lymphocyte targeting of a triglyceride mimetic prodrug is enhanced in a large animal model: studies in greyhound dogs

Han, S., Hu, L., Gracia, G., Quach, T., Simpson, J. S., Edwards, G. A., Trevaskis, N. L. & Porter, C. J. H., 3 Oct 2016, In : Molecular Pharmaceutics. 13, 10, p. 3351-3361 11 p.

Research output: Contribution to journalArticleResearchpeer-review

Metabolomics and lipidomics reveal perturbation of sphingolipid metabolism by a novel anti-trypanosomal 3-(oxazolo[4,5-b]pyridine-2-yl)anilide

Stoessel, D., Nowell, C. J., Jones, A. J., Ferrins, L., Ellis, K. M., Riley, J., Rahmani, R., Read, K. D., McConville, M. J., Avery, V. M., Baell, J. B. & Creek, D. J., 1 Jul 2016, In : Metabolomics. 12, 7, 14 p., 126.

Research output: Contribution to journalArticleResearchpeer-review

Modeling the influence of fatty acid incorporation on mesophase formation in amphiphilic therapeutic delivery systems

Le, T. C., Tran, N., Mulet, X. & Winkler, D. A., 2016, In : Molecular Pharmaceutics. 13, 3, p. 996-1003 8 p.

Research output: Contribution to journalArticleResearchpeer-review

Neomycin B-cyclen conjugates and their Zn(II) complexes as RNA-binding agents

Kong, B., Joshi, T., Belousoff, M. J., Tor, Y., Graham, B. & Spiccia, L., 2016, In : Journal of Inorganic Biochemistry. 162, p. 334-342 9 p.

Research output: Contribution to journalArticleResearchpeer-review

Neutron reflection study of the interaction of the eukaryotic pore-forming actinoporin equinatoxin II with lipid membranes reveals intermediate states in pore formation

Wacklin, H. P., Bremec, B. B., Moulin, M., Rojko, N., Haertlein, M., Forsyth, T., Anderluh, G. & Norton, R., 1 Apr 2016, In : Biochimica et Biophysica Acta - Biomembranes. 1858, 4, p. 640-652 13 p.

Research output: Contribution to journalArticleResearchpeer-review

New synthetic approaches towards analogues of bedaquiline

Priebbenow, D. L., Barbaro, L. & Baell, J. B., 28 Oct 2016, In : Organic and Biomolecular Chemistry. 14, 40, p. 9622-9628 7 p.

Research output: Contribution to journalArticleResearchpeer-review

Novel fused arylpyrimidinone based allosteric modulators of the M1 muscarinic acetylcholine receptor

Mistry, S. N., Lim, H., Jorg, M., Capuano, B., Christopoulos, A., Lane, J. R. & Scammells, P. J., 18 May 2016, In : ACS Chemical Neuroscience. 7, 5, p. 647-661 15 p.

Research output: Contribution to journalArticleResearchpeer-review

Novel irreversible agonists acting at the A1 adenosine receptor

Jorg, M., Glukhova, A., Abdul Ridha, A., Vecchio, E. A., Nguyen, A., Sexton, P., White, P., May, L., Christopoulos, A. & Scammells, P., 22 Dec 2016, In : Journal of Medicinal Chemistry. 59, 24, p. 11182-11194 13 p.

Research output: Contribution to journalArticleResearchpeer-review

Open source drug discovery: Highly potent antimalarial compounds derived from the tres cantos arylpyrroles

Williamson, A. E., Ylioja, P. M., Robertson, M. N., Antonova-Koch, Y., Avery, V., Baell, J., Batchu, H., Batra, S., Burrows, J. N., Bhattacharyya, S., Calderon, F., Charman, S., Clark, J., Crespo, B., Dean, M., Debbert, S. L., Delves, M. J., Dennis, A. S. M., Deroose, F., Duffy, S. & 3 othersRyan, E., Wells, T. & White, K., 26 Oct 2016, In : ACS Central Science. 2, 10, p. 687-701 15 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access

Optically pure, structural, and fluorescent analogues of a dimeric Y4 receptor agonist derived by an olefin metathesis approach

Liu, M., Mountford, S. J., Richardson, R. R., Groenen, M., Holliday, N. D. & Thompson, P. E., 14 Jul 2016, In : Journal of Medicinal Chemistry. 59, 13, p. 6059-6069 11 p.

Research output: Contribution to journalArticleResearchpeer-review

Overcoming artificial broadening in Gd3+-Gd3+ distance distributions arising from dipolar pseudo-secular terms in DEER experiments

Cohen, M. F. R., Frydman, V., Milko, P., Iron, M. A., Abdelkader, E. H., Lee, M. D., Swarbrick, J. D., Raitsimring, A., Otting, G., Graham, B., Feintuch, A. & Goldfarb, D., 2016, In : Physical Chemistry Chemical Physics. 18, 18, p. 12847-12859 13 p.

Research output: Contribution to journalArticleResearchpeer-review

Phosphorylation of the dimeric cytoplasmic domain of the phytosulfokine receptor, PSKR1

Muleya, V., Marondedze, C., Wheeler, J. I., Thomas, L., Mok, Y. F., Griffin, M. D. W., Manallack, D. T., Kwezi, L., Lilley, K. S., Gehring, C. & Irving, H. R., 2016, In : Biochemical Journal. 473, 19, p. 3081-3098 18 p.

Research output: Contribution to journalArticleResearchpeer-review

Potent dual inhibitors of Plasmodium falciparum M1 and M17 aminopeptidases through optimization of S1 pocket interactions

Drinkwater, N., Vinh, N. B., Mistry, S. N., Bamert, R. S., Ruggeri, C., Holleran, J. P., Loganathan, S., Paiardini, A., Charman, S. A., Powell, A. K., Avery, V. M., McGowan, S. & Scammells, P. J., 3 Mar 2016, In : European Journal of Medicinal Chemistry. 110, p. 43-64 22 p.

Research output: Contribution to journalArticleResearchpeer-review

Protein unfolding is essential for cleavage within the α-helix of a model protein substrate by the serine protease, thrombin

Robertson, A. L., Headey, S. J., Ng, N. M., Wijeyewickrema, L. C., Scanlon, M. J., Pike, R. N. & Bottomley, S. P., Mar 2016, In : Biochimie. 122, p. 227-234 8 p.

Research output: Contribution to journalArticleResearchpeer-review

Pulmonary delivery of the Kv1.3-blocking peptide HsTX1[R14A] for the treatment of autoimmune diseases

Jin, L., Zhou, Q. T., Chan, H-K., Larson, I. C., Pennington, M. W., Morales, R. A. V., Boyd, B. J., Norton, R. S. & Nicolazzo, J. A., 1 Feb 2016, In : Journal of Pharmaceutical Sciences. 105, 2, p. 650-656 7 p.

Research output: Contribution to journalArticleResearchpeer-review

Pulse EPR-enabled interpretation of scarce pseudocontact shifts induced by lanthanide binding tags

Abdelkader, E. H., Yao, X., Feintuch, A., Adams, L. A., Aurelio, L., Graham, B., Goldfarb, D. & Otting, G., 2016, In : Journal of Biomolecular NMR. 64, 1, p. 39-51 13 p.

Research output: Contribution to journalArticleResearchpeer-review

Quantitation of polymyxin-lipopolysaccharide interactions using an image-based fluorescent probe

McInerney, M. P., Roberts, K. D., Thompson, P. E., Li, J., Nation, R. L., Velkov, T. & Nicolazzo, J. A., 2016, In : Journal of Pharmaceutical Sciences. 105, 2, p. 1006-1010 5 p.

Research output: Contribution to journalArticleResearchpeer-review

Recent advances, and unresolved issues, in the application of computational modelling to the prediction of the biological effects of nanomaterials

Winkler, D. A., 2016, In : Toxicology and Applied Pharmacology. 299, SI, p. 96-100 5 p.

Research output: Contribution to journalArticleResearchpeer-review

Redox-stable cyclic peptide inhibitors of the SPSB2-iNOS interaction

Yap, B. K., Harjani, J. R., Leung, E. W. W., Nicholson, S. E., Scanlon, M. J., Chalmers, D. K., Thompson, P. E., Baell, J. B. & Norton, R. S., 1 Mar 2016, In : FEBS Letters. 590, 6, p. 696-704 9 p.

Research output: Contribution to journalArticleResearchpeer-review

RIDME distance measurements using Gd(III) tags with a narrow central transition

Collauto, A., Frydman, V., Lee, M. D., Abdelkader, E. H., Feintuch, A., Swarbrick, J. D., Graham, B., Otting, G. & Goldfarb, D., 2016, In : Physical Chemistry Chemical Physics. 18, 28, p. 19037-19049 13 p.

Research output: Contribution to journalArticleResearchpeer-review

Role of the second extracellular loop of the adenosine A1 receptor on allosteric modulator binding, signaling, and cooperativity

Nguyen, A. T. N., Vecchio, E. A., Thomas, T., Nguyen, T. D., Aurelio, L., Scammells, P. J., White, P. J., Sexton, P. M., Gregory, K. J., May, L. T. & Christopoulos, A., 1 Dec 2016, In : Molecular Pharmacology. 90, 6, p. 715-725 11 p.

Research output: Contribution to journalArticleResearchpeer-review

Selective inhibition of apicoplast tryptophanyl-tRNA synthetase causes delayed death in Plasmodium falciparum

Pasaje, C. F. A., Cheung, V., Kennedy, K., Lim, E. E., Baell, J. B., Griffin, M. D. W. & Ralph, S. A., 9 Jun 2016, In : Scientific Reports. 6, 13 p., 27531.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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Selenophene and thiophene-core estrogen receptor ligands that inhibit motility and development of parasitic stages of Haemonchus contortus

Preston, S., Luo, J., Zhang, Y., Jabbar, A., Crawford, S., Baell, J., Hofmann, A., Hu, M., Zhou, H-B. & Gasser, R. B., 16 Jun 2016, In : Parasites and Vectors. 9, 1, 11 p., 346.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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Sensitive NMR approach for determining the binding mode of tightly binding ligand molecules to protein targets

Chen, W-N., Nitsche, C., Pilla, K. B., Graham, B., Huber, T., Klein, C. D. & Otting, G., 2016, In : Journal of the American Chemical Society. 138, 13, p. 4539-4546 8 p.

Research output: Contribution to journalArticleResearchpeer-review

Sequence-specific assignment of methyl groups from the neuronal SNARE complex using lanthanide-induced pseudocontact shifts

Pan, Y-Z., Quade, B., Brewer, K. D., Szabo, M., Swarbrick, J. D., Graham, B. & Rizo, J., 1 Dec 2016, In : Journal of Biomolecular NMR. 66, 4, p. 281-293 13 p.

Research output: Contribution to journalArticleResearchpeer-review

Solution NMR characterization of apical membrane antigen 1 and small molecule interactions as a basis for designing new antimalarials

Krishnarjuna, B., Lim, S. S., Devine, S. M., Debono, C. O., Lam, R., Chandrashekaran, I. R., Jaipuria, G., Yagi, H., Atreya, H. S., Scanlon, M. J., MacRaild, C. A., Scammells, P. J. & Norton, R. S., 1 Jun 2016, In : Journal of Molecular Recognition. 29, 6, p. 281-291 11 p.

Research output: Contribution to journalArticleResearchpeer-review

Stereoselective synthesis and structural elucidation of dicarba peptides

Gleeson, E. C., Wang, Z. J., Robinson, S. D., Chhabra, S., MacRaild, C. A., Jackson, W. R., Norton, R. S. & Robinson, A. J., 2016, In : Chemical Communications. 52, 24, p. 4446-4449 4 p.

Research output: Contribution to journalArticleResearchpeer-review

Strain-transcending immune response generated by chimeras of the malaria vaccine candidate merozoite surface protein 2

Krishnarjuna, B., Andrew, D., MacRaild, C. A., Morales, R. A. V., Beeson, J. G., Anders, R. F., Richards, J. S. & Norton, R. S., 11 Feb 2016, In : Scientific Reports. 6, 12 p., 20613.

Research output: Contribution to journalArticleResearchpeer-review

Open Access

Structural basis for the inhibition of voltage-gated sodium channels by conotoxin μO§-GVIIJ

Green, B. R., Gajewiak, J., Chhabra, S., Skalicky, J. J., Zhang, M. M., Rivier, J. E., Bulaj, G., Olivera, B. M., Yoshikami, D. & Norton, R., 25 Mar 2016, In : Journal of Biological Chemistry. 291, 13, p. 7205-7220 16 p.

Research output: Contribution to journalArticleResearchpeer-review

Structural basis for the selective binding of inhibitors to 6-hydroxymethyl-7,8-dihydropterin pyrophosphokinase from Staphylococcus aureus and Escherichia coli

Dennis, M. L., Pitcher, N. P., Lee, M. D., Debono, A. J., Wang, Z-C., Harjani, J. R., Rahmani, R., Cleary, B., Peat, T. S., Baell, J. B. & Swarbrick, J. D., 9 Jun 2016, In : Journal of Medicinal Chemistry. 59, 11, p. 5248-5263 16 p.

Research output: Contribution to journalArticleResearchpeer-review

Structure–activity studies of β-hairpin peptide inhibitors of the Plasmodium falciparum AMA1–RON2 interaction

Wang, G., Drinkwater, N., Drew, D. R., MacRaild, C. A., Chalmers, D. K., Mohanty, B., Lim, S. S., Anders, R. F., Beeson, J. G., Thompson, P. E., McGowan, S., Simpson, J. S., Norton, R. S. & Scanlon, M. J., 9 Oct 2016, In : Journal of Molecular Biology. 428, 20, p. 3986-3998 13 p.

Research output: Contribution to journalArticleResearchpeer-review

Structure and substrate fingerprint of aminopeptidase P from Plasmodium falciparum

Drinkwater, N., Kannan Sivaraman, K., Bamert, R. S., Rut, W., Mohamed, K., Vinh, N. B., Scammells, P. J., Drag, M. & McGowan, S., 27 Sep 2016, In : Biochemical Journal. 473, 19, p. 3189-3204 16 p.

Research output: Contribution to journalArticleResearchpeer-review

Subtype-selective small molecule inhibitors reveal a fundamental role for Nav1.7 in nociceptor electrogenesis, axonal conduction and presynaptic release

Alexandrou, A. J., Brown, A. R., Chapman, M. L., Estacion, M., Turner, J., Mis, M. A., Wilbrey, A., Payne, E. C., Gutteridge, A., Cox, P. J., Doyle, R., Printzenhoff, D., Lin, Z., Marron, B. E., West, C., Swain, N. A., Storer, R. I., Stupple, P. A., Castle, N. A., Hounshell, J. A. & 8 othersRivara, M., Randall, A., Dib-Hajj, S. D., Krafte, D. S., Waxman, S. G., Patel, M. K., Butt, R. P. & Stevens, E. B., 1 Apr 2016, In : PLoS ONE. 11, 4, 22 p., e0152405.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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Synthesis, structure elucidation, DNA-PK and PI3K and anti-cancer activity of 8- and 6-aryl-substituted-1-3-benzoxazines

Morrison, R., Al-Rawi, J. M. A., Jennings, I. G., Thompson, P. E. & Angove, M. J., 3 Mar 2016, In : European Journal of Medicinal Chemistry. 110, p. 326-339 14 p.

Research output: Contribution to journalArticleResearchpeer-review