Research Output 1977 2019

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2019

3,3′-Disubstituted 5,5′-Bi(1,2,4-triazine) Derivatives with Potent in Vitro and in Vivo Antimalarial Activity

Xue, L., Shi, D. H., Harjani, J. R., Huang, F., Beveridge, J. G., Dingjan, T., Ban, K., Diab, S., Duffy, S., Lucantoni, L., Fletcher, S., Chiu, F. C. K., Blundell, S., Ellis, K., Ralph, S. A., Wirjanata, G., Teguh, S., Noviyanti, R., Chavchich, M., Creek, D. & 10 othersPrice, R. N., Marfurt, J., Charman, S. A., Cuellar, M. E., Strasser, J. M., Dahlin, J. L., Walters, M. A., Edstein, M. D., Avery, V. M. & Baell, J. B., 1 Jan 2019, In : Journal of Medicinal Chemistry. 62, 5, p. 2485-2498 14 p.

Research output: Contribution to journalArticleResearchpeer-review

6-Phenylpyrimidin-4-ones as Positive Allosteric Modulators at the M1 mAChR: The Determinants of Allosteric Activity

Jorg, M. T., van der Westhuizen, E. T., Khajehali, E., Burger, W. A. C., White, J., Choy, K. H. C., Tobin, A. B., Sexton, P. M., Valant, C., Capuano, B., Christopoulos, A. & Scammells, P. J., 20 Mar 2019, In : ACS Chemical Neuroscience. 10, 3, p. 1099-1114 16 p.

Research output: Contribution to journalArticleResearchpeer-review

A ligand-induced structural change in fatty acid-binding protein 1 is associated with potentiation of peroxisome proliferator-activated receptor α agonists

Patil, R., Mohanty, B., Liu, B., Chandrashekaran, I. R., Headey, S. J., Williams, M. L., Clements, C. S., Ilyichova, O., Doak, B. C., Genissel, P., Weaver, R., Vuillard, L., Halls, M. L., Porter, C. J. H. & Scanlon, M. J., 8 Mar 2019, In : Journal of Biological Chemistry. 294, 10, p. 3720-3734 15 p.

Research output: Contribution to journalArticleResearchpeer-review

An apically located hybrid guanylate cyclase-ATPase is critical for the initiation of Ca2+ signaling and motility in Toxoplasma gondii

Yang, L., Uboldi, A. D., Seizova, S., Wilde, M. L., Coffey, M. J., Katris, N. J., Yamaryo-Botté, Y., Kocan, M., Bathgate, R. A. D., Stewart, R. J., McConville, M. J., Thompson, P. E., Botté, C. Y. & Tonkin, C. J., 31 May 2019, In : Journal of Biological Chemistry. 294, 22, p. 8959-8972 14 p.

Research output: Contribution to journalArticleResearchpeer-review

A Nonionic Polyethylene Oxide (PEO) Surfactant Model: Experimental and Molecular Dynamics Studies of Kolliphor EL

Suys, E. J. A., Warren, D. B., Pham, A. C., Nowell, C. J., Clulow, A. J., Benameur, H., Porter, C. J. H., Pouton, C. W. & Chalmers, D. K., 1 Jan 2019, In : Journal of Pharmaceutical Sciences. 108, 1, p. 193-204 12 p.

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Application of a chemical probe to detect neutrophil elastase activation during inflammatory bowel disease

Anderson, B., Poole, D. P., Aurelio, L., Ng, G. Z., Fleischmann, M., Kasperkiewicz, P., Morissette, C., Drag, M., van Driel, I. R., Schmidt, B. L., Vanner, S. J., Bunnett, N. & Edgington-Mitchell, L., 16 Sep 2019, In : Scientific Reports. 9, 12 p., 13295.

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A Thieno[2,3-d]pyrimidine Scaffold is a Novel Negative Allosteric Modulator of the Dopamine D2 Receptor

Fyfe, T. J., Zarzycka, B., Lim, H. D., Kellam, B., Mistry, S. N., Katrich, V., Scammells, P. J., Lane, J. R. & Capuano, B., 1 Oct 2019, In : Journal of Medicinal Chemistry. 62, 1, p. 174-206 33 p.

Research output: Contribution to journalArticleResearchpeer-review

Classification of the human phox homology (PX) domains based on their phosphoinositide binding specificities

Chandra, M., Chin, Y. K. Y., Mas, C., Feathers, J. R., Paul, B., Datta, S., Chen, K. E., Jia, X., Yang, Z., Norwood, S. J., Mohanty, B., Bugarcic, A., Teasdale, R. D., Henne, W. M., Mobli, M. & Collins, B. M., 4 Apr 2019, In : Nature Communications. 10, 1, 14 p., 1528.

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Contemporary Anti-Ebola Drug Discovery Approaches and Platforms

Schneider-Futschik, E. K., Hoyer, D., Khromykh, A. A., Baell, J. B., Marsh, G. A., Baker, M. A., Li, J. & Velkov, T., 1 Nov 2019, In : ACS Infectious Diseases. 5, 1, p. 35-48 14 p.

Research output: Contribution to journalArticleResearchpeer-review

Controlled Construction of Cyclic d / l Peptide Nanorods

Silk, M. R., Mohanty, B., Sampson, J. B., Scanlon, M. J., Thompson, P. E. & Chalmers, D. K., 8 Jan 2019, In : Angewandte Chemie - International Edition. 58, 2, p. 596-601 6 p.

Research output: Contribution to journalArticleResearchpeer-review

Effects of VCP979 Novel p38 Mitogen Activated Protein Kinase Inhibitor on Progression of Pancreatic Cancer in Mouse Model with Diabetic Conditions

Xu, T., Ding, J., Ge, H., Xu, X., Scammells, P., Wang, B. & Ju, S., 1 Jun 2019, In : Journal of Biomedical Nanotechnology. 15, 6, p. 1325-1333 9 p.

Research output: Contribution to journalArticleResearchpeer-review

Evolution of cnidarian trans-defensins: Sequence, structure and exploration of chemical space

Mitchell, M. L., Shafee, T., Papenfuss, A. T. & Norton, R. S., 1 Jul 2019, In : Proteins: Structure, Function and Bioinformatics. 87, 7, p. 551-560 10 p.

Research output: Contribution to journalArticleResearchpeer-review

Formation of Highly Substituted Indenes through Acid Promoted Cyclodehydration with Nucleophile Incorporation

Dillon, A. S., Kerr, D. J. & Flynn, B. L., 1 Mar 2019, In : Journal of Organic Chemistry. 84, 5, p. 2756-2767 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Hydroxamic Acid Inhibitors Provide Cross-Species Inhibition of Plasmodium M1 and M17 Aminopeptidases

Vinh, N. B., Drinkwater, N., Malcolm, T. R., Kassiou, M., Lucantoni, L., Grin, P. M., Butler, G. S., Duffy, S., Overall, C. M., Avery, V. M., Scammells, P. J. & McGowan, S., 24 Jan 2019, In : Journal of Medicinal Chemistry. 62, 2, p. 622-640 19 p.

Research output: Contribution to journalArticleResearchpeer-review

Identification of the Binding Site of Apical Membrane Antigen 1 (AMA1) Inhibitors Using a Paramagnetic Probe

Akter, M., Drinkwater, N., Devine, S. M., Drew, S. C., Krishnarjuna, B., Debono, C. O., Wang, G., Scanlon, M. J., Scammells, P. J., McGowan, S., MacRaild, C. A. & Norton, R. S., 5 Mar 2019, In : ChemMedChem. 14, 5, p. 603-612 10 p.

Research output: Contribution to journalArticleResearchpeer-review

Improvement in the Predicted Partitioning of Alcohol and Polyethylene Oxide Groups Between Water and Octanol (logP) in Molecular Dynamics Simulations

Warren, D. B., McPhee, E., Birru, W. A., Benameur, H., Chalmers, D. K. & Pouton, C. W., 1 Jan 2019, In : Journal of Pharmaceutical Sciences. 108, 1, p. 214-222 9 p.

Research output: Contribution to journalArticleResearchpeer-review

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Interaction of merozoite surface protein 2 with lipid membranes

Lu, C., Zheng, X., Zhang, W., Zhao, H., MacRaild, C. A., Norton, R. S., Zhuang, Y., Wang, J. & Zhang, X., Feb 2019, In : FEBS Letters. 593, 3, p. 288-295 8 p.

Research output: Contribution to journalArticleResearchpeer-review

Interaction of Nucleotides with a Trinuclear Terbium(III)-Dizinc(II) Complex: Efficient Sensitization of Terbium Luminescence by Guanosine Monophosphate and Application to Real-Time Monitoring of Phosphodiesterase Activity

Aulsebrook, M. L., Starck, M., Grace, M. R., Graham, B., Thordarson, P., Pal, R. & Tuck, K. L., 7 Jan 2019, In : Inorganic Chemistry. 58, 1, p. 495-505 11 p.

Research output: Contribution to journalArticleResearchpeer-review

Location of Solvated Probe Molecules Within Nonionic Surfactant Micelles Using Molecular Dynamics

Warren, D. B., McPhee, E., Birru, W. A., Benameur, H., Chalmers, D. K. & Pouton, C. W., 1 Jan 2019, In : Journal of Pharmaceutical Sciences. 108, 1, p. 205-213 9 p.

Research output: Contribution to journalArticleResearchpeer-review

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Mapping the chemical and sequence space of the ShKT superfamily

Shafee, T., Mitchell, M. L. & Norton, R. S., 1 Jul 2019, In : Toxicon. 165, p. 95-102 8 p.

Research output: Contribution to journalArticleResearchpeer-review

Modulation of the aggregation of an amyloidogenic sequence by flanking-disordered region in the intrinsically disordered antigen merozoite surface protein 2

Zhang, W., Zhang, J., MacRaild, C. A., Norton, R. S., Anders, R. F. & Zhang, X., 2019, In : European Biophysics Journal. 48, 1, p. 99-110 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Molecular Determinants of the Intrinsic Efficacy of the Antipsychotic Aripiprazole

Klein Herenbrink, C., Verma, R., Lim, H. D., Kopinathan, A., Keen, A., Shonberg, J., Draper-Joyce, C. J., Scammells, P. J., Christopoulos, A., Javitch, J. A., Capuano, B., Shi, L. & Lane, J. R., 16 Aug 2019, In : ACS Chemical Biology. 14, 8, p. 1780-1792 13 p.

Research output: Contribution to journalArticleResearchpeer-review

Molecular dissection of an inhibitor targeting the HIV integrase dependent preintegration complex nuclear import

Wagstaff, K. M., Headey, S., Telwatte, S., Tyssen, D., Hearps, A. C., Thomas, D. R., Tachedjian, G. & Jans, D. A., Jan 2019, In : Cellular Microbiology. 21, 1, 13 p., e12953.

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Novel 1-Methyl-1 H-pyrazole-5-carboxamide Derivatives with Potent Anthelmintic Activity

Le, T. G., Kundu, A., Ghoshal, A., Nguyen, N. H., Preston, S., Jiao, Y., Ruan, B., Xue, L., Huang, F., Keiser, J., Hofmann, A., Chang, B. C. H., Garcia-Bustos, J., Wells, T. N. C., Palmer, M. J., Jabbar, A., Gasser, R. B. & Baell, J. B., 11 Apr 2019, In : Journal of Medicinal Chemistry. 62, 7, p. 3367-3380 14 p.

Research output: Contribution to journalArticleResearchpeer-review

Novel Human Aminopeptidase N Inhibitors: Discovery and Optimization of Subsite Binding Interactions

Lee, J., Vinh, N. B., Drinkwater, N., Yang, W., Kannan Sivaraman, K., Schembri, L. S., Gazdik, M., Grin, P. M., Butler, G. S., Overall, C. M., Charman, S. A., McGowan, S. & Scammells, P. J., 8 Aug 2019, In : Journal of Medicinal Chemistry. 62, 15, p. 7185-7209 25 p.

Research output: Contribution to journalArticleResearchpeer-review

Novel RU486 (mifepristone) analogues with increased activity against Venezuelan Equine Encephalitis Virus but reduced progesterone receptor antagonistic activity

DeBono, A., Thomas, D. R., Lundberg, L., Pinkham, C., Cao, Y., Graham, J. D., Clarke, C. L., Wagstaff, K. M., Shechter, S., Kehn-Hall, K. & Jans, D. A., 22 Feb 2019, In : Scientific Reports. 9, 1, 19 p., 2634.

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Overcoming P-Glycoprotein-Mediated Drug Resistance with Noscapine Derivatives

Muthiah, D., Henshaw, G. K., DeBono, A. J., Capuano, B., Scammells, P. J. & Callaghan, R., 1 Feb 2019, In : Drug Metabolism and Disposition. 47, 2, p. 164-172 9 p.

Research output: Contribution to journalArticleResearchpeer-review

Probe dependence of allosteric enhancers on the binding affinity of adenosine A 1 -receptor agonists at rat and human A 1 -receptors measured using NanoBRET

Cooper, S. L., Soave, M., Jörg, M., Scammells, P. J., Woolard, J. & Hill, S. J., Apr 2019, In : British Journal of Pharmacology. 176, 7, p. 864-878 15 p.

Research output: Contribution to journalArticleResearchpeer-review

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Structural and functional characterisation of a novel peptide from the Australian sea anemone Actinia tenebrosa

Elnahriry, K. A., Wai, D. C. C., Krishnarjuna, B., Badawy, N. N., Chittoor, B., MacRaild, C. A., Williams-Noonan, B. J., Surm, J. M., Chalmers, D. K., Zhang, A. H., Peigneur, S., Mobli, M., Tytgat, J., Prentis, P. & Norton, R. S., 1 Oct 2019, In : Toxicon. 168, p. 104-112 9 p.

Research output: Contribution to journalArticleResearchpeer-review

Structure-Kinetic Profiling of Haloperidol Analogues at the Human Dopamine D2 Receptor

Fyfe, T., Kellam, B., Sykes, D. A., Capuano, B., Scammells, P., Lane, R., Charlton, S. J. & Mistry, S., 3 Oct 2019, (Accepted/In press) In : Journal of Medicinal Chemistry. 79 p.

Research output: Contribution to journalArticleResearchpeer-review

Substituted Pyridazin-3(2 H)-ones as Highly Potent and Biased Formyl Peptide Receptor Agonists

Deora, G. S., Qin, C. X., Vecchio, E. A., Debono, A. J., Priebbenow, D. L., Brady, R. M., Beveridge, J., Teguh, S. C., Deo, M., May, L. T., Krippner, G., Ritchie, R. H. & Baell, J. B., 23 May 2019, In : Journal of Medicinal Chemistry. 62, 10, p. 5242-5248 7 p.

Research output: Contribution to journalArticleResearchpeer-review

Subtle modifications to a thieno[2,3-d]pyrimidine scaffold yield negative allosteric modulators and agonists of the dopamine D 2 receptor

Fyfe, T. J., Kellam, B., Mistry, S. N., Scammells, P. J., Lane, J. R. & Capuano, B., 15 Apr 2019, In : European Journal of Medicinal Chemistry. 168, p. 474-490 17 p.

Research output: Contribution to journalArticleResearchpeer-review

The three-dimensional structure of an H-superfamily conotoxin reveals a granulin fold arising from a common ICK cysteine framework

Nielsen, L. D., Foged, M. M., Albert, A., Bertelsen, A. B., Søltoft, C. L., Robinson, S. D., Petersen, S. V., Purcell, A. W., Olivera, B. M., Norton, R. S., Vasskog, T., Safavi-Hemami, H., Teilum, K. & Ellgaard, L., 1 Jan 2019, In : Journal of Biological Chemistry. 294, 22, p. 8745-8759 15 p.

Research output: Contribution to journalArticleResearchpeer-review

The uncharacterized bacterial protein YejG has the same architecture as domain III of elongation factor G

Mohanty, B., Hanson-Manful, P., Finn, T. J., Chambers, C. R., McKellar, J. L. O., Macindoe, I., Helder, S., Setiyaputra, S., Zhong, Y., Mackay, J. P. & Patrick, W. M., 8 Apr 2019, (Accepted/In press) In : Proteins: Structure, Function and Bioinformatics. 7 p.

Research output: Contribution to journalArticleResearchpeer-review

Unlocking the full potential of lipid-based formulations using lipophilic salt/ionic liquid forms

Williams, H. D., Ford, L., Igonin, A., Shan, Z., Botti, P., Morgen, M. M., Hu, G., Pouton, C. W., Scammells, P. J., Porter, C. J. H. & Benameur, H., 29 May 2019, (Accepted/In press) In : Advanced Drug Delivery Reviews. 16 p.

Research output: Contribution to journalArticleResearchpeer-review

Visible light-triggered cargo release from donor acceptor Stenhouse adduct (DASA)-doped lyotropic liquid crystalline nanoparticles

Jia, S., Tan, A., Hawley, A., Graham, B. & Boyd, B. J., 15 Jul 2019, In : Journal of Colloid and Interface Science. 548, p. 151-159 9 p.

Research output: Contribution to journalArticleResearchpeer-review

2018

1,2,4-Oxadiazole antimicrobials act synergistically with daptomycin and display rapid kill kinetics against MDR Enterococcus faecium

Carter, G. P., Harjani, J. R., Li, L., Pitcher, N. P., Nong, Y., Riley, T. V., Williamson, D. A., Stinear, T. P., Baell, J. B. & Howden, B. P., 1 Jun 2018, In : Journal of Antimicrobial Chemotherapy. 73, 6, p. 1562-1569 8 p.

Research output: Contribution to journalArticleResearchpeer-review

8-Mercaptoguanine Derivatives as Inhibitors of Dihydropteroate Synthase

Dennis, M. L., Lee, M. D., Harjani, J. R., Ahmed, M., Debono, A. J., Pitcher, N. P., Wang, Z-C., Chhabra, S., Barlow, N., Rahmani, R., Cleary, B., Dolezal, O., Hattarki, M., Aurelio, L., Shonberg, J., Graham, B., Peat, T. S., Baell, J. B. & Swarbrick, J. D., 6 Feb 2018, In : Chemistry - A European Journal. 24, 8, p. 1922-1930 9 p.

Research output: Contribution to journalArticleResearchpeer-review

A Cyclic Peptide Inhibitor of the iNOS-SPSB Protein-Protein Interaction as a Potential Anti-Infective Agent

Sadek, M. M., Barlow, N., Leung, E. W. W., Williams-Noonan, B. J., Yap, B. K., Shariff, F. M., Caradoc-Davies, T. T., Nicholson, S. E., Chalmers, D. K., Thompson, P. E., Law, R. H. P. & Norton, R. S., 19 Oct 2018, In : ACS Chemical Biology. 13, 10, p. 2930-2938 9 p.

Research output: Contribution to journalArticleResearchpeer-review

Anti-Infective Peptides to Enhance the Host Innate Response: Design, Development and Delivery

Norton, R. S., 2018, In : Protein and Peptide Letters. 25, 12, p. 1101-1107 7 p.

Research output: Contribution to journalArticleResearchpeer-review

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Assay Guidance Manual: Quantitative Biology and Pharmacology in Preclinical Drug Discovery

Coussens, N. P., Sittampalam, G. S., Guha, R., Brimacombe, K., Grossman, A., Chung, T. D. Y., Weidner, J. R., Riss, T., Trask, O. J., Auld, D., Dahlin, J. L., Devanaryan, V., Foley, T. L., McGee, J., Kahl, S. D., Kales, S. C., Arkin, M., Baell, J., Bejcek, B., Gal-Edd, N. & 25 othersGlicksman, M., Haas, J. V., Iversen, P. W., Hoeppner, M., Lathrop, S., Sayers, E., Liu, H., Trawick, B., McVey, J., Lemmon, V. P., Li, Z., McManus, O., Minor, L., Napper, A., Wildey, M. J., Pacifici, R., Chin, W. W., Xia, M., Xu, X., Lal-Nag, M., Hall, M. D., Michael, S., Inglese, J., Simeonov, A. & Austin, C. P., 1 Sep 2018, In : Clinical and Translational Science. 11, 5, p. 461-470 10 p.

Research output: Contribution to journalArticleOtherpeer-review

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Asymmetric synthesis of multiple quaternary stereocentre-containing cyclopentyls by oxazolidinone-promoted Nazarov cyclizations

Volpe, R., Lepage, R. J., White, J. M., Krenske, E. H. & Flynn, B. L., 20 Apr 2018, In : Chemical Science. 9, 20, p. 4644-4649 6 p.

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Broad activity of diphenyleneiodonium analogues against Mycobacterium tuberculosis, malaria parasites and bacterial pathogens

Nguyen, N., Wilson, D. W., Nagalingam, G., Triccas, J. A., Schneider, E. K., Li, J., Velkov, T. & Baell, J., 25 Mar 2018, In : European Journal of Medicinal Chemistry. 148, p. 507-518 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Characterisation of peptide interactions that regulate PKCε activation

Chandrashekaran, I. R., Norton, R. S. & Schmitz-Peiffer, C., 1 Jan 2018, In : FEBS Letters. 592, 2, p. 179-189 11 p.

Research output: Contribution to journalArticleResearchpeer-review

Cyclic Hexapeptide Mimics of the LEDGF Integrase Recognition Loop in Complex with HIV-1 Integrase

Northfield, S. E., Wielens, J., Headey, S. J., Williams-Noonan, B. J., Mulcair, M., Scanlon, M., Parker, M. W., Thompson, P. E. & Chalmers, D. K., 10 Aug 2018, In : ChemMedChem. 13, 15, p. 1555-1565 11 p.

Research output: Contribution to journalArticleResearchpeer-review

Decoding the Rich Biological Properties of Noble Gases: How Well Can We Predict Noble Gas Binding to Diverse Proteins?

Winkler, D. A., Katz, I., Farjot, G., Warden, A. C. & Thornton, A. W., 19 Sep 2018, In : ChemMedChem. 13, 18, p. 1931-1938 8 p.

Research output: Contribution to journalArticleResearchpeer-review