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Research Output 1990 2019

2019

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 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

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

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

Reply to ‘Antipsychotics with similar association kinetics at dopamine D2 receptors differ in extrapyramidal side-effects’

Sykes, D. A., Lane, J. R., Szabo, M., Capuano, B., Javitch, J. A. & Charlton, S. J., 1 Dec 2018, In : Nature Communications. 9, 1, 5 p., 3568.

Research output: Contribution to journalLetterOtherpeer-review

Open Access
File

Synthesis and Pharmacological Evaluation of Noscapine-Inspired 5-Substituted Tetrahydroisoquinolines as Cytotoxic Agents

Devine, S. M., Yong, C., Amenuvegbe, D., Aurelio, L., Muthiah, D., Pouton, C., Callaghan, R., Capuano, B. & Scammells, P. J., 27 Sep 2018, In : Journal of Medicinal Chemistry. 61, 18, p. 8444-8456 13 p.

Research output: Contribution to journalArticleResearchpeer-review

The action of a negative allosteric modulator at the dopamine D2 receptor is dependent upon sodium ions

Draper-Joyce, C. J., Verma, R. K., Michino, M., Shonberg, J., Kopinathan, A., Klein Herenbrink, C., Scammells, P. J., Capuano, B., Abramyan, A. M., Thal, D. M., Javitch, J. A., Christopoulos, A., Shi, L. & Lane, J. R., 1 Dec 2018, In : Scientific Reports. 8, 1, 12 p., 1208.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File

The structural determinants of the bitopic binding mode of a negative allosteric modulator of the dopamine D2 receptor

Draper-Joyce, C. J., Michino, M., Verma, R. K., Klein Herenbrink, C., Shonberg, J., Kopinathan, A., Scammells, P. J., Capuano, B., Thal, D. M., Javitch, J. A., Christopoulos, A., Shi, L. & Lane, J. R., 1 Feb 2018, In : Biochemical Pharmacology. 148, p. 315-328 14 p.

Research output: Contribution to journalArticleResearchpeer-review

2017

The cationic small molecule GW4869 is cytotoxic to high phosphatidylserine-expressing myeloma cells

Vuckovic, S., Vandyke, K., Rickards, D. A., Mccauley Winter, P., Brown, S. H. J., Mitchell, T. W., Liu, J., Lu, J., Askenase, P. W., Yuriev, E., Capuano, B., Ramsland, P., Hill, G. R., Zannettino, A. C. W. & Hutchinson, A. T., May 2017, In : British Journal of Haematology. 177, 3, p. 423-440 18 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File
2016

4-phenylpyridin-2-one derivatives: a novel class of positive allosteric modulator of the M1 muscarinic acetylcholine receptor

Mistry, S. N., Jorg, M., Lim, H., Vinh, N. B., Sexton, P. M., Capuano, B., Christopoulos, A., Lane, J. R. & Scammells, P. J., 14 Jan 2016, In : Journal of Medicinal Chemistry. 59, 1, p. 388-409 22 p.

Research output: Contribution to journalArticleResearchpeer-review

Crossword puzzles for chemistry education: Learning goals beyond vocabulary

Yuriev, E., Capuano, B. & Short, J. L., 2016, In : Chemistry Education Research and Practice. 17, 3, p. 532-554 23 p.

Research output: Contribution to journalArticleResearchpeer-review

Multivalent approaches and beyond: novel tools for the investigation of dopamine D2 receptor pharmacology

Kopinathan, A., Scammells, P. J., Lane, J. R. & Capuano, B., 1 Jul 2016, In : Future Medicinal Chemistry. 8, 11, p. 1349-1372 24 p.

Research output: Contribution to journalReview ArticleResearchpeer-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

Testing of direct acting antiviral agents purchased overseas: a necessary precaution to protect patients?

Lubel, J., Chivers, S., Taylor, D. & Capuano, B., 1 Sep 2016, In : Internal Medicine Journal. 46, 9, p. 1111-1113 3 p.

Research output: Contribution to journalLetterOtherpeer-review

The dopamine D2 receptor dimer and its interaction with homobivalent antagonists: homology modeling, docking and molecular dynamics

Kaczor, A. A., Jorg, M. & Capuano, B., 1 Sep 2016, In : Journal of Molecular Modeling. 22, 9, 14 p., 203.

Research output: Contribution to journalArticleResearchpeer-review

The role of kinetic context in apparent biased agonism at GPCRs

Herenbrink, C. K., Sykes, D. A., Donthamsetti, P., Canals, M., Coudrat, T., Shonberg, J., Scammells, P. J., Capuano, B., Sexton, P. M., Charlton, S. J., Javitch, J. A., Christopoulos, A. & Lane, J. R., 24 Feb 2016, In : Nature Communications. 7, 14 p., 10842.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
2015

A structure-activity relationship study of the positive allosteric modulator LY2033298 at the M4 muscarinic acetylcholine receptor

Szabo, M., Huynh, T., Valant, C., Lane, J. R., Sexton, P. M., Christopoulos, A. & Capuano, B., 2015, In : MedChemComm. 6, 11, p. 1998-2003 6 p.

Research output: Contribution to journalArticleResearchpeer-review

Discovery of a novel class of negative allosteric modulator of the dopamine D2 receptor through fragmentation of a bitopic ligand

Mistry, S. N., Shonberg, J., Draper-Joyce, C. J., Klein Herenbrink, C., Michino, M., Shi, L., Christopoulos, A., Capuano, B., Scammells, P. J. & Lane, J. R. D., 2015, In : Journal of Medicinal Chemistry. 58, 17, p. 6819-6843 25 p.

Research output: Contribution to journalArticleResearchpeer-review

Progress toward the development of noscapine and derivatives as anticancer agents

DeBono, A., Capuano, B. & Scammells, P. J., 2015, In : Journal of Medicinal Chemistry. 58, 15, p. 5699-5727 29 p.

Research output: Contribution to journalArticleResearchpeer-review

Proof of concept study for designed multiple ligands targeting the dopamine D2, serotonin 5-HT2A, and muscarinic M1 acetylcholine receptors

Szabo, M., Lim, H. D., Klein Herenbrink, C., Christopoulos, A., Lane, J. R. D. & Capuano, B., 2015, In : Journal of Medicinal Chemistry. 58, 3, p. 1550 - 1555 6 p.

Research output: Contribution to journalArticleResearchpeer-review

Synthesis and pharmacological evaluation of dual acting ligands targeting the adenosine A2A and dopamine D2 receptors for the potential treatment of Parkinson's disease

Jorg, M. T., May, L. T., Mak, F. S., Lee, K. C. K., Miller, N. D., Scammells, P. J. & Capuano, B., 2015, In : Journal of Medicinal Chemistry. 58, 2, p. 718 - 738 21 p.

Research output: Contribution to journalArticleResearchpeer-review

Synthesis and pharmacological evaluation of M4 muscarinic receptor positive allosteric modulators derived from VU10004

Huynh, T., Valant, C., Crosby, I. T., Sexton, P., Christopoulos, A. & Capuano, B., 2015, In : ACS Chemical Neuroscience. 6, 6, p. 838 - 844 7 p.

Research output: Contribution to journalArticleResearchpeer-review

2014

A new mechanism of allostery in a G protein-coupled receptor dimer

Lane, J. R. D., Donthamsetti, P., Shonberg, J., Draper-Joyce, C. J., Dentry, S., Michino, M., Shi, L., Lopez Munoz, L., Scammells, P. J., Capuano, B., Sexton, P., Javitch, J. A. & Christopoulos, A., 2014, In : Nature Chemical Biology. 10, 9, p. 745 - 752 8 p.

Research output: Contribution to journalArticleResearchpeer-review

Bacterial fatty acid synthesis: Effect of Tween 80 on antibiotic potency against Streptococcus agalactiae and methicillin-resistant Staphylococcus aureus

Krsta, D., Ku, K. U. C., Crosby, I. T., Capuano, B. & Manallack, D. T., 2014, In : Anti-Infective Agents. 12, 1, p. 80 - 84 5 p.

Research output: Contribution to journalArticleResearchpeer-review

Biased agonism at G protein-coupled receptors: The promise and the challenges - A medicinal chemistry perspective

Shonberg, J., Lopez Munoz, L., Scammells, P. J., Christopoulos, A., Capuano, B. & Lane, J. R. D., 2014, In : Medicinal Research Reviews. 34, 6, p. 1286 - 1330 45 p.

Research output: Contribution to journalArticleResearchpeer-review

Development of a photoactivatable allosteric ligand for the M1 muscarinic acetylcholine receptor

Davie, B. J., Sexton, P., Capuano, B., Christopoulos, A. & Scammells, P. J., 2014, In : ACS Chemical Neuroscience. 5, 10, p. 902 - 907 6 p.

Research output: Contribution to journalArticleResearchpeer-review

Investigation of novel ropinirole analogues: Synthesis, pharmacological evaluation and computational analysis of dopamine D2 receptor functionalized congeners and homobivalent ligands

Jorg, M. T., Kaczor, A. A., Mak, F. S., Lee, K. C. K., Poso, A., Miller, N. D., Scammells, P. J. & Capuano, B., 2014, In : MedChemComm. 5, 7, p. 891 - 898 8 p.

Research output: Contribution to journalArticleResearchpeer-review

NMR case study of ropinirole: Concentration-dependent effects of nonexchangeable proton resonances

Jorg, M. T., Headey, S. J., Scammells, P. J. & Capuano, B., 2014, In : Magnetic Resonance in Chemistry. 52, 11, p. 715 - 718 4 p.

Research output: Contribution to journalArticleOtherpeer-review

Structure-activity relationships of privileged structures lead to the discovery of novel biased ligands at the dopamine D2 receptor

Szabo, M., Klein Herenbrink, C., Christopoulos, A., Lane, J. R. D. & Capuano, B., 2014, In : Journal of Medicinal Chemistry. 57, 11, p. 4924 - 4939 16 p.

Research output: Contribution to journalArticleResearchpeer-review

The dopamine D2 and adenosine A2A receptors: Past, present and future trends for the treatment of parkinson's disease

Jorg, M. T., Scammells, P. J. & Capuano, B., 2014, In : Current Medicinal Chemistry. 21, 27, p. 3188 - 3210 23 p.

Research output: Contribution to journalArticleResearchpeer-review

The synthesis and biological evaluation of multifunctionalised derivatives of noscapine as cytotoxic agents

Debono, A. J., Mistry, S. J., Xie, A., Muthiah, D., Phillips, J. R., Ventura, S., Callaghan, R., Pouton, C. W., Capuano, B. & Scammells, P. J., 2014, In : ChemMedChem. 9, 2, p. 399 - 410 12 p.

Research output: Contribution to journalArticleResearchpeer-review

2013

A structure-activity analysis of biased agonism at the dopamine D2 receptor

Shonberg, J., Klein Herenbrink, C., Lopez, L., Christopoulos, A., Scammells, P. J., Capuano, B. & Lane, J. R. D., 2013, In : Journal of Medicinal Chemistry. 56, 22, p. 9199 - 9221 23 p.

Research output: Contribution to journalArticleResearchpeer-review

Detection and prevention of aggregation-based false positives in STD-NMR-based fragment screening

Vom, A., Headey, S. J., Wang, G., Capuano, B., Yuriev, E., Scanlon, M. & Simpson, J. S., 2013, In : Australian Journal of Chemistry. 66, 12, p. 1518 - 1524 7 p.

Research output: Contribution to journalArticleResearchpeer-review

Probing structural requirements of positive allosteric modulators of the M4 muscarinic receptor

Huynh, T., Valant, C., Crosby, I. T., Sexton, P., Christopoulos, A. & Capuano, B., 2013, In : Journal of Medicinal Chemistry. 56, 20, p. 8196 - 8200 5 p.

Research output: Contribution to journalArticleResearchpeer-review

Synthesis, functional and binding profile of (R)-apomorphine based homobivalent ligands targeting the dopamine D2 receptor

Shonberg, J., Lane, J. R. D., Scammells, P. J. & Capuano, B., 2013, In : MedChemComm. 4, 9, p. 1290 - 1296 7 p.

Research output: Contribution to journalArticleResearchpeer-review

Synthesis, molecular structure, NMR spectroscopic and computational analysis of a selective adenosine A2A antagonist, ZM 241385

Jorg, M., Agostino, M. J., Yuriev, E., Mak, F. S., Miller, N. D., White, J., Scammells, P. J. & Capuano, B., 2013, In : Structural Chemistry. 24, 4, p. 1241 - 1251 11 p.

Research output: Contribution to journalArticleResearchpeer-review

2012

Homobivalent ligands of the atypical antipsychotic clozapine: Design, synthesis, and pharmacological evaluation

McRobb, F. M., Crosby, I. T., Yuriev, E., Lane, J. R. D. & Capuano, B., 2012, In : Journal of Medicinal Chemistry. 55, 4, p. 1622 - 1634 13 p.

Research output: Contribution to journalArticleResearchpeer-review

Simplified platensimycin analogues as antibacterial agents

Krsta, D., Ku, K. U. C., Crosby, I. T., Capuano, B. & Manallack, D. T., 2012, In : MedChemComm. 3, 2, p. 244 - 249 6 p.

Research output: Contribution to journalArticleResearchpeer-review

Synthesis and biological evaluation of N-substituted noscapine analogues

Debono, A. J., Xie, J. H., Ventura, S., Pouton, C. W., Capuano, B. & Scammells, P. J., 2012, In : ChemMedChem. 7, 12, p. 2122 - 2133 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Synthesis and SAR study of 4-arylpiperidines and 4-aryl-1,2,3,6- tetrahydropyridines as 5-HT2C agonists

Conway, R., Valant, C., Christopoulos, A., Robertson, A. D., Capuano, B. & Crosby, I. T., 2012, In : Bioorganic and Medicinal Chemistry Letters. 22, 7, p. 2560 - 2564 5 p.

Research output: Contribution to journalArticleResearchpeer-review

2011

Characterization of the N-methyltransferase activities of the multifunctional polypeptide cyclosporin synthetase

Velkov, T., Horne, J., Scanlon, M., Capuano, B., Yuriev, E. & Lawen, A., 2011, In : Chemistry and Biology. 18, 4, p. 464 - 475 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Design strategies for bivalent ligands targeting GPCRs

Shonberg, J., Scammells, P. & Capuano, B., 2011, In : ChemMedChem. 6, 6, p. 963 - 974 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Schizophrenia: a systematic review of the disease state, current therapeutics and their molecular mechanisms of action

Shin, J., Malone, D., Crosby, I. & Capuano, B., 2011, In : Current Medicinal Chemistry. 18, 9, p. 1380 - 1404 25 p.

Research output: Contribution to journalArticleResearchpeer-review