Research Output 1977 2019

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2019

Derivatives and analogues of resveratrol: Recent advances in structural modification

Li, Q. S., Li, Y., Deora, G. S. & Ruan, B. F., 1 Jan 2019, In : Mini-Reviews in Medicinal Chemistry. 19, 10, p. 809-825 17 p.

Research output: Contribution to journalArticleResearchpeer-review

Discovery of benzoylsulfonohydrazides as potent inhibitors of the histone acetyltransferase KAT6A

Leaver, D. J., Cleary, B., Nguyen, N., Priebbenow, D., Lagiakos, H. R., Sanchez, J., Xue, L., Huang, F., Sun, Y., Mujumdar, P., Mudududdla, R., Varghese, S., Teguh, S., Charman, S. A., White, K. L., Katneni, K., Cuellar, M., Strasser, J. M., Dahlin, J. L., Walters, M. A. & 10 others, Street, I. P., Monahan, B. J., Jarman, K. E., Sabroux, H. J., Falk, H., Chung, M. C., Hermans, S. J., Parker, M. W., Thomas, T. & Baell, J. B., 8 Aug 2019, In : Journal of Medicinal Chemistry. 62, 15, p. 7146-7159 14 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

Estrogen Receptor α (ERα)-targeting Compounds and Derivatives: Recent Advances in Structural Modification and Bioactivity

Guo, W. Y., Zeng, S. M. Z., Deora, G. S., Li, Q. S. & Ruan, B. F., 1 Jan 2019, In : Current Topics in Medicinal Chemistry. 19, 15, p. 1318-1337 20 p.

Research output: Contribution to journalArticleResearchpeer-review

3 Citations (Scopus)

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

Expansion of a novel lead targeting M. tuberculosis DHFR as antitubercular agents

Sharma, K., Tanwar, O., Deora, G. S., Ali, S., Alam, M. M., Zaman, M. S., Krishna, V. S., Sriram, D. & Akhter, M., 1 Jan 2019, In : Bioorganic and Medicinal Chemistry. 27, 7, p. 1421-1429 9 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

Glutathione Transferase Omega-1 Regulates NLRP3 Inflammasome Activation through NEK7 Deglutathionylation

Hughes, M. M., Hooftman, A., Angiari, S., Tummala, P., Zaslona, Z., Runtsch, M. C., McGettrick, A. F., Sutton, C. E., Diskin, C., Rooke, M., Takahashi, S., Sundararaj, S., Casarotto, M. G., Dahlstrom, J. E., Palsson-McDermott, E. M., Corr, S. C., Mills, K. H. G., Preston, R. J. S., Neamati, N., Xie, Y. & 3 others, Baell, J. B., Board, P. G. & O'Neill, L. A. J., 1 Oct 2019, In : Cell Reports. 29, 1, p. 151-161.e5 11 p.

Research output: Contribution to journalArticleResearchpeer-review

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2 Citations (Scopus)

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

2 Citations (Scopus)

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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2 Citations (Scopus)

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

2 Citations (Scopus)

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

1 Citation (Scopus)

Intra-articular Treatment of Osteoarthritis with Diclofenac-Conjugated Polymer Reduces Inflammation and Pain

Sulistio, A., Mansfeld, F. M., Reyes-Ortega, F., D'Souza, A. M., Ng, S. M. Y., Birkett, S., Blencowe, A., Qiao, G. G., Little, C. B., Shu, C. C., Bendele, A. M., Valade, D., Donohue, A. C., Quinn, J. F., Whittaker, M. R., Davis, T. P. & Tait, R. J., 24 May 2019, In : ACS Applied Bio Materials. 2, 7, p. 2822-2832 11 p.

Research output: Contribution to journalArticleResearchpeer-review

2 Citations (Scopus)

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

2 Citations (Scopus)

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.

Research output: Contribution to journalArticleResearchpeer-review

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1 Citation (Scopus)

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

1 Citation (Scopus)

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.

Research output: Contribution to journalArticleResearchpeer-review

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2 Citations (Scopus)

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

1 Citation (Scopus)

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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Production of metabolites of the anti-cancer drug noscapine using a P450BM3 mutant library

Richards, L., Lutz, A., Chalmers, D. K., Jarrold, A., Bowser, T., Stevens, G. W. & Gras, S. L., 22 Aug 2019, In : Biotechnology Reports. 24, p. 1-12 12 p., e00372.

Research output: Contribution to journalArticleResearchpeer-review

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1 Citation (Scopus)

Regulation of PRMT5-MDM4 axis is critical in the response to CDK4/6 inhibitors in melanoma

AbuHammad, S., Cullinane, C., Martin, C., Bacolas, Z., Ward, T., Chen, H., Slater, A., Ardley, K., Kirby, L., Chan, K. T., Brajanovski, N., Smith, L. K., Rao, A. D., Lelliott, E. J., Kleinschmidt, M., Vergara, I. A., Papenfuss, A. T., Lau, P., Ghosh, P., Haupt, S. & 12 others, Haupt, Y., Sanij, E., Poortinga, G., Pearson, R. B., Falk, H., Curtis, D. J., Stupple, P., Devlin, M., Street, I., Davies, M. A., McArthur, G. A. & Sheppard, K. E., 3 Sep 2019, In : Proceedings of the National Academy of Sciences of the United States of America. 116, 36, p. 17990-18000 11 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

1 Citation (Scopus)

Structure-Activity Relationship Studies of Tolfenpyrad Reveal Subnanomolar Inhibitors of Haemonchus contortus Development

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., 2019, In : Journal of Medicinal Chemistry. 62, 2, p. 1036-1053 8 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

2 Citations (Scopus)

Tetrahydroquinoxalines induce a lethal evisceration phenotype in Haemonchus contortus in vitro

Jiao, Y., Preston, S., Garcia-Bustos, J. F., Baell, J. B., Ventura, S., Le, T., McNamara, N., Nguyen, N., Botteon, A., Skinner, C., Danne, J., Ellis, S., Koehler, A. V., Wang, T., Chang, B. C. H., Hofmann, A., Jabbar, A. & Gasser, R. B., 1 Apr 2019, In : International Journal for Parasitology: Drugs and Drug Resistance. 9, p. 59-71 13 p.

Research output: Contribution to journalArticleResearchpeer-review

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1 Citation (Scopus)

The Acid/Base Profile of a Large Food Chemical Database

Santibáñez-Morán, M. G., Rico-Hidalgo, M. P., Manallack, D. T. & Medina-Franco, J. L., 1 Jun 2019, In : Molecular Informatics. 38, 6, 7 p., 1800171.

Research output: Contribution to journalArticleResearchpeer-review

Open Access

The Development Process for Discovery and Clinical Advancement of Modern Antimalarials

Ashton, T. D., Devine, S., Mohrle, J., Laleu, B., Burrows, J. N., Charman, S., Creek, D. & Sleebs, B. E., Aug 2019, (Accepted/In press) In : Journal of Medicinal Chemistry.

Research output: Contribution to journalArticleResearchpeer-review

1 Citation (Scopus)

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., 2019, In : Proteins: Structure, Function and Bioinformatics. 87, 8, p. 699-705 7 p.

Research output: Contribution to journalArticleResearchpeer-review

1 Citation (Scopus)

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., 2019, In : Advanced Drug Delivery Reviews. 142, 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