Research Output

2017

Isoform-specific biased agonism of histamine H3 receptor agonists

Riddy, D. M., Cook, A. E., Diepenhorst, N. A., Bosnyak, S., Brady, R., La Cour, C. M., Mocaer, E., Summers, R. J., Charman, W. N., Sexton, P. M., Christopoulos, A. & Langmead, C. J., 1 Feb 2017, In : Molecular Pharmacology. 91, 2, p. 87-99 13 p.

Research output: Contribution to journalArticleResearchpeer-review

12 Citations (Scopus)

Key determinants of selective binding and activation by the monocyte chemoattractant proteins at the chemokine receptor CCR2

Huma, Z. E., Sanchez, J., Lim, H. D., Bridgford, J. L., Huang, C., Parker, B. J., Pazhamalil, J. G., Porebski, B. T., Pfleger, K. D. G., Lane, J. R., Canals, M. & Stone, M. J., 23 May 2017, In : Science Signaling. 10, 480, 13 p., eaai8529.

Research output: Contribution to journalArticleResearchpeer-review

17 Citations (Scopus)

Live cell imaging and profiling of cysteine cathepsin activity using a quenched activity-based probe

Edgington-Mitchell, L. E., Bogyo, M. & Verdoes, M., 25 Oct 2017, Activity-Based Proteomics: Methods and Protocols. Overkleeft, H. S. & Florea, B. I. (eds.). New York NY USA: Springer, p. 145-159 15 p. (Methods in Molecular Biology; vol. 1491).

Research output: Chapter in Book/Report/Conference proceedingChapter (Book)Otherpeer-review

15 Citations (Scopus)

Loss of the Wnt receptor frizzled 7 in the mouse gastric epithelium is deleterious and triggers rapid repopulation in vivo

Flanagan, D. J., Barker, N., Nowell, C., Clevers, H., Ernst, M., Phesse, T. J. & Vincan, E., 1 Aug 2017, In : Disease Models and Mechanisms. 10, 8, p. 971-980 10 p.

Research output: Contribution to journalArticleResearchpeer-review

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11 Citations (Scopus)

Lysophosphatidylcholine modulates the aggregation of human islet amyloid polypeptide

Xing, Y., Pilkington, E. H., Wang, M., Nowell, C. J., Kakinen, A., Sun, Y., Wang, B., Davis, T. P., Ding, F. & Ke, P. C., 7 Dec 2017, In : Physical Chemistry Chemical Physics. 19, 45, p. 30627-30635 9 p.

Research output: Contribution to journalArticleResearchpeer-review

6 Citations (Scopus)

M1 muscarinic allosteric modulators slow prion neurodegeneration and restore memory loss

Bradley, S. J., Bourgognon, J. M., Sanger, H. E., Verity, N., Mogg, A. J., White, D. J., Butcher, A. J., Moreno, J. A., Molloy, C., Macedo-Hatch, T., Edwards, J. M., Wess, J., Pawlak, R., Read, D. J., Sexton, P. M., Broad, L. M., Steinert, J. R., Mallucci, G. R., Christopoulos, A., Felder, C. C. & 1 others, Tobin, A. B., 1 Feb 2017, In : Journal of Clinical Investigation. 127, 2, p. 487-499 13 p.

Research output: Contribution to journalArticleResearchpeer-review

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28 Citations (Scopus)

ML290 is a biased allosteric agonist at the relaxin receptor RXFP1

Kocan, M., Sarwar, M., Ang, S. Y., Xiao, J., Marugan, J., Hossain, M. A., Wang, C., Hutchinson, D. S., Samuel, C. S., Agoulnik, A. I., Bathgate, R. A. D. & Summers, R. J., 1 Dec 2017, In : Scientific Reports. 7, 1, 14 p., 2968.

Research output: Contribution to journalArticleResearchpeer-review

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17 Citations (Scopus)

Molecular insights into allosteric modulation of Class C G protein-coupled receptors

Leach, K. & Gregory, K. J., 1 Feb 2017, In : Pharmacological Research. 116, p. 105-118 14 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

32 Citations (Scopus)

Myoepithelial cell-specific expression of stefin A as a suppressor of early breast cancer invasion

Duivenvoorden, H. M., Rautela, J., Edgington-Mitchell, L. E., Spurling, A., Greening, D. W., Nowell, C. J., Molloy, T. J., Robbins, E., Brockwell, N. K., Lee, C. S., Chen, M., Holliday, A., Selinger, C. I., Hu, M., Britt, K. L., Stroud, D. A., Bogyo, M., Möller, A., Polyak, K., Sloane, B. F. & 2 others, O'Toole, S. A. & Parker, B. S., 1 Dec 2017, In : Journal of Pathology. 243, 4, p. 496-509 14 p.

Research output: Contribution to journalArticleResearchpeer-review

22 Citations (Scopus)

NanoEHS beyond toxicity-focusing on biocorona

Lin, S., Mortimer, M., Chen, R., Kakinen, A., Riviere, J. E., Davis, T. P., Ding, F. & Ke, P-C., 2017, In : Environmental Science: Nano. 4, 7, p. 1433-1454 22 p.

Research output: Contribution to journalArticleResearchpeer-review

24 Citations (Scopus)

Nanotechnology in Medical Research

Mansfeld, F. M., Davis, T. P. & Kavallaris, M., 2017, Micro- and Nanotechnology in Vaccine Development: A volume in Micro and Nano Technologies. Skwarczynski, M. & Toth, I. (eds.). Oxford UK: Elsevier, p. 21-45 25 p.

Research output: Chapter in Book/Report/Conference proceedingChapter (Book)Researchpeer-review

1 Citation (Scopus)
7 Citations (Scopus)

Neurokinin 1 receptor signaling in endosomes mediates sustained nociception and is a viable therapeutic target for prolonged pain relief

Jensen, D. D., Lieu, T., Halls, M. L., Veldhuis, N. A., Imlach, W. L., Mai, Q. N., Poole, D. P., Quach, T., Aurelio, L., Conner, J., Klein Herenbrink, C., Barlow, N., Simpson, J. S., Scanlon, M. J., Graham, B., McCluskey, A., Robinson, P. J., Escriou, V., Nassini, R., Materazzi, S. & 6 others, Geppetti, P., Hicks, G. A., Christie, M. J., Porter, C. J. H., Canals, M. & Bunnett, N. W., 31 May 2017, In : Science Translational Medicine. 9, 392, 15 p., aal3447.

Research output: Contribution to journalArticleResearchpeer-review

53 Citations (Scopus)

Neurovascular Alterations in Alzheimer’s Disease: Transporter Expression Profiles and CNS Drug Access

McInerney, M. P., Short, J. L. & Nicolazzo, J. A., 1 Jul 2017, In : The AAPS Journal. 19, 4, p. 940-956 17 p.

Research output: Contribution to journalArticleResearchpeer-review

8 Citations (Scopus)

New pharmacological approaches to the prevention of myocardial ischemia-reperfusion injury

Chin, K. Y., Qin, C., May, L., Ritchie, R. H. & Woodman, O. L., 1 Jan 2017, In : Current Drug Targets. 18, 15, p. 1689-1711 23 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

10 Citations (Scopus)

Novel inhibitors targeting Venezuelan equine encephalitis virus capsid protein identified using In Silico Structure-Based-Drug-Design

Shechter, S., Thomas, D. R., Lundberg, L., Pinkham, C., Lin, S. C., Wagstaff, K. M., Debono, A., Kehn-Hall, K. & Jans, D. A., 1 Dec 2017, In : Scientific Reports. 7, 1, 16 p., 17705.

Research output: Contribution to journalArticleResearchpeer-review

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6 Citations (Scopus)

Phase-plate cryo-EM structure of a class B GPCR-G-protein complex

Liang, Y-L., Khoshouei, M., Radjainia, M., Zhang, Y., Glukhova, A., Tarrasch, J., Thal, D., Furness, S. G. B., Christopoulos, G., Coudrat, T., Danev, R., Baumeister, W., Miller, L. J., Christopoulos, A., Kobilka, B., Wootten, D., Skiniotis, G. & Sexton, P., 1 Jun 2017, In : Nature. 546, 7656, p. 118-123 6 p.

Research output: Contribution to journalArticleResearchpeer-review

242 Citations (Scopus)

Polymers with acyl-protected perthiol chain termini as convenient building blocks for doubly responsive H2S-donating nanoparticles

Yu, S. H., Ercole, F., Veldhuis, N. A., Whittaker, M. R., Davis, T. P. & Quinn, J. F., 7 Nov 2017, In : Polymer Chemistry. 8, 41, p. 6362-6367 6 p.

Research output: Contribution to journalArticleResearchpeer-review

9 Citations (Scopus)

Possible anti-inflammatory mediated wound healing activity of pyrazinamide and clofazemine in Wistar rats

Sonwane, V., Pakhare, A., Kudale, P., Somani, R., Tembhurne, S. & Shenoy, P., 2017, In : World Journal of Pharmaceutical Research. 6, 6, p. 1563-1570 8 p.

Research output: Contribution to journalArticleResearchpeer-review

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Potential toxicity of polymyxins in human lung epithelial cells

Ahmed, M. U., Velkov, T., Lin, Y-W., Yun, B., Nowell, C. J., Zhou, F., Zhou, Q. T., Chan, K., Azad, M. A. K. & Li, J., 1 Jun 2017, In : Antimicrobial Agents and Chemotherapy. 61, 6, 12 p., e02690-16.

Research output: Contribution to journalArticleResearchpeer-review

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13 Citations (Scopus)

Practical chain-end reduction of polymers obtained with ATRP

Gutekunst, W. R., Anastasaki, A., Lunn, D. J., Truong, N. P., Whitfield, R., Jones, G. R., Treat, N. J., Abdilla, A., Barton, B. E., Clark, P. G., Haddleton, D. M., Davis, T. P. & Hawker, C. J., Sep 2017, In : Macromolecular Chemistry and Physics. 218, 18, 7 p., 1700107.

Research output: Contribution to journalArticleResearchpeer-review

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9 Citations (Scopus)

Precise control of drug loading and release of an NSAID-polymer conjugate for long term osteoarthritis intra-articular drug delivery

Sulistio, A., Reyes-Ortega, F., D'Souza, A. M., Ng, S. M. Y., Valade, D., Quinn, J. F., Donohue, A. C., Mansfeld, F., Blencowe, A., Qiao, G., Prankerd, R., Quirk, S., Whittaker, M. R., Davis, T. P. & Tait, R. J., 1 Jan 2017, In : Journal of Materials Chemistry B. 5, 31, p. 6221-6226 6 p.

Research output: Contribution to journalArticleResearchpeer-review

6 Citations (Scopus)

Purinergic Receptor Transactivation by the β2-Adrenergic Receptor Increases Intracellular Ca2+ in Nonexcitable Cells

Stallaert, W., van der Westhuizen, E. T., Schonegge, A-M., Plouffe, B., Hogue, M., Lukashova, V., Inoue, A., Ishida, S., Aoki, J., Le Gouill, C. & Bouvier, M., 1 May 2017, In : Molecular Pharmacology. 91, 5, p. 533-544 12 p.

Research output: Contribution to journalArticleResearchpeer-review

18 Citations (Scopus)

Recent progress in the understanding of relaxin family peptides and their receptors

Summers, R. J., 2017, In : British Journal of Pharmacology. 174, 10, p. 915-920 6 p.

Research output: Contribution to journalEditorialOtherpeer-review

Role of Nonneuronal TRPV4 Signaling in Inflammatory Processes

Rajasekhar, P., Poole, D. P. & Veldhuis, N. A., 2017, Ion Channels DownUnder. Geraghty, D. P. & Rash, L. D. (eds.). Cambridge MA USA: Academic Press, Vol. 79. p. 117-139 23 p. (Advances in Pharmacology; vol. 79).

Research output: Chapter in Book/Report/Conference proceedingChapter (Book)Researchpeer-review

6 Citations (Scopus)

Scaffolding the development of problem-solving skills in chemistry: Guiding novice students out of dead ends and false starts

Yuriev, E., Naidu, S., Schembri, L. S. & Short, J. L., 1 Jan 2017, In : Chemistry Education Research and Practice. 18, 3, p. 486-504 19 p.

Research output: Contribution to journalArticleResearchpeer-review

10 Citations (Scopus)

Signal transduction pathways activated by insulin-like peptide 5 at the relaxin family peptide RXFP4 receptor

Ang, S. Y., Hutchinson, D. S., Patil, N., Evans, B. A., Bathgate, R. A. D., Halls, M. L., Hossain, M. A., Summers, R. J. & Kocan, M., 1 May 2017, In : British Journal of Pharmacology. 174, 10, p. 1077-1089 13 p.

Research output: Contribution to journalArticleResearchpeer-review

15 Citations (Scopus)

Small-molecule-biased formyl peptide receptor agonist compound 17b protects against myocardial ischaemia-reperfusion injury in mice

Qin, C. X., May, L. T., Li, R., Cao, N., Rosli, S., Deo, M., Alexander, A. E., Horlock, D., Bourke, J. E., Yang, Y. H., Stewart, A. G., Kaye, D. M., Du, X. J., Sexton, P. M., Christopoulos, A., Gao, X. M. & Ritchie, R. H., 7 Feb 2017, In : Nature Communications. 8, 13 p., 14232.

Research output: Contribution to journalArticleResearchpeer-review

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36 Citations (Scopus)

Social regulation of the lymph node transcriptome in rhesus macaques (Macaca mulatta)

Chun, K., Capitanio, J. P., Lamkin, D. M., Sloan, E. K., Arevalo, J. M. G. & Cole, S. W., 1 Feb 2017, In : Psychoneuroendocrinology. 76, p. 107-113 7 p.

Research output: Contribution to journalArticleResearchpeer-review

4 Citations (Scopus)

Specific and Differential Binding of N-Acetylgalactosamine Glycopolymers to the Human Macrophage Galactose Lectin and Asialoglycoprotein Receptor

Tanaka, J., Gleinich, A. S., Zhang, Q., Whitfield, R., Kempe, K., Haddleton, D., Davis, T. P., Perrier, S., Mitchell, D. A. & Wilson, P., 8 May 2017, In : Biomacromolecules. 18, 5, p. 1624-1633 10 p.

Research output: Contribution to journalArticleResearchpeer-review

22 Citations (Scopus)

Specification of murine ground state pluripotent stem cells to regional neuronal populations

Alsanie, W. F., Niclis, J. C., Hunt, C. P., De Luzy, I. R., Penna, V., Bye, C. R., Pouton, C. W., Haynes, J., Firas, J., Thompson, L. H. & Parish, C. L., 22 Nov 2017, In : Scientific Reports. 7, 1, 16 p., 16001.

Research output: Contribution to journalArticleResearchpeer-review

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2 Citations (Scopus)

Stress activates pronociceptive endogenous opioid signalling in DRG neurons during chronic colitis

Guerrero-Alba, R., Valdez-Morales, E., Jimenez-Vargas, N. N., Lopez, C. L., Polanco, J. J., Okamoto, T., Nasser, Y., Bunnett, N. W., Lomax, A. E. & Vanner, S. J., 1 Dec 2017, In : Gut. 66, 12, p. 2121-2131 11 p.

Research output: Contribution to journalArticleResearchpeer-review

16 Citations (Scopus)

Structural features embedded in G protein-coupled receptor co-crystal structures are key to their success in virtual screening

Coudrat, T., Christopoulos, A., Sexton, P. M. & Wootten, D., 1 Apr 2017, In : PLoS ONE. 12, 4, 29 p., e0174719.

Research output: Contribution to journalArticleResearchpeer-review

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3 Citations (Scopus)

Structure-Based Design and Discovery of New M2 Receptor Agonists

Fish, I., Stößel, A., Eitel, K., Valant, C., Albold, S., Huebner, H., Möller, D., Clark, M. J., Sunahara, R. K., Christopoulos, A., Shoichet, B. K. & Gmeiner, P., 22 Nov 2017, In : Journal of Medicinal Chemistry. 60, 22, p. 9239-9250 12 p.

Research output: Contribution to journalArticleResearchpeer-review

12 Citations (Scopus)

Structure-function analyses of a pertussis-like toxin from pathogenic Escherichia coli reveal a distinct mechanism of inhibition of trimeric G-proteins

Littler, D. R., Ang, S. Y., Moriel, D. G., Kocan, M., Kleifeld, O., Johnson, M. D., Tran, M. T., Paton, A. W., Paton, J. C., Summers, R. J., Schembri, M. A., Rossjohn, J. & Beddoe, T., 8 Sep 2017, In : The Journal of Biological Chemistry. 292, 36, p. 15143-15158 16 p.

Research output: Contribution to journalArticleResearchpeer-review

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3 Citations (Scopus)

Structure of the adenosine A1 receptor reveals the basis for subtype selectivity

Glukhova, A., Thal, D. M., Nguyen, A. T., Vecchio, L., Jorg, M., Scammells, P. J., May, L. T., Sexton, P. M. & Christopoulos, A., 23 Feb 2017, In : Cell. 168, 5, p. 867-877.e13

Research output: Contribution to journalArticleResearchpeer-review

107 Citations (Scopus)

Student engagement with a flipped classroom teaching design affects pharmacology examination performance in a manner dependent on question type

White, P. J., Naidu, S., Yuriev, E., Short, J. L., McLaughlin, J. E. & Larson, I. C., 2017, In : American Journal of Pharmaceutical Education. 81, 9, p. 10-23 14 p., 5931.

Research output: Contribution to journalArticleResearchpeer-review

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13 Citations (Scopus)

Synergistic effect of IL-12 and IL-18 induces TIM3 regulation of γδ T cell function and decreases the risk of clinical malaria in children living in Papua New Guinea

Schofield, L., Ioannidis, L. J., Karl, S., Robinson, L. J., Tan, Q. Y., Poole, D. P., Betuela, I., Hill, D. L., Siba, P. M., Hansen, D. S., Mueller, I. & Eriksson, E. M., 15 Jun 2017, In : BMC Medicine. 15, 1, 15 p., 114.

Research output: Contribution to journalArticleResearchpeer-review

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16 Citations (Scopus)

Synthesis and Pharmacological Characterization of Novel trans-Cyclopropylmethyl-Linked Bivalent Ligands That Exhibit Selectivity and Allosteric Pharmacology at the Dopamine D3 Receptor (D3R)

Kumar, V., Moritz, A. E., Keck, T. M., Bonifazi, A., Ellenberger, M. P., Sibley, C. D., Free, R. B., Shi, L., Lane, J. R., Sibley, D. R. & Newman, A. H., 23 Feb 2017, In : Journal of Medicinal Chemistry. 60, 4, p. 1478-1494 17 p.

Research output: Contribution to journalArticleResearchpeer-review

24 Citations (Scopus)

Systematic high-content genome-wide RNAi screens of endothelial cell migration and morphology

Williams, S. P., Gould, C. M., Nowell, C. J., Karnezis, T., Achen, M. G., Simpson, K. J. & Stacker, S. A., 1 Mar 2017, In : Scientific Data. 4, 11 p., 170009.

Research output: Contribution to journalArticleResearchpeer-review

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10 Citations (Scopus)

Targeting adenosine receptors for the treatment of cardiac fibrosis

Vecchio, E. A., White, P. J. & May, L. T., 5 May 2017, In : Frontiers in Pharmacology. 8, MAY, 7 p., 243.

Research output: Contribution to journalReview ArticleOtherpeer-review

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17 Citations (Scopus)

The actions of relaxin family peptides on signal transduction pathways activated by the relaxin family peptide receptor RXFP4

Ang, S. Y., Hutchinson, D. S., Evans, B. A., Hossain, M. A., Patil, N., Bathgate, R. A. D., Kocan, M. & Summers, R. J., Jan 2017, In : Naunyn-Schmiedeberg's Archives of Pharmacology. 390, 1, p. 105-111 7 p.

Research output: Contribution to journalArticleResearchpeer-review

4 Citations (Scopus)

The actions of relaxin on the human cardiovascular system

Sarwar, M., Du, X. J., Dschietzig, T. B. & Summers, R. J., 1 May 2017, In : British Journal of Pharmacology. 174, 10, p. 933-949 17 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

29 Citations (Scopus)

The concise guide to Pharmacology 2017/18: G protein-coupled receptors

CGTP Collaborators, 1 Dec 2017, In : British Journal of Pharmacology. 174, p. S17-S129

Research output: Contribution to journalArticleOtherpeer-review

Open Access
472 Citations (Scopus)

THE CONCISE GUIDE TO PHARMACOLOGY 2017/18: Overview

Alexander, S. P. H., Kelly, E., Marrion, N. V., Peters, J. A., Faccenda, E., Harding, S. D., Pawson, A. J., Sharman, J. L., Southan, C., Buneman, O. P., Cidlowski, J. A., Christopoulos, A., Davenport, A. P., Fabbro, D., Spedding, M., Striessnig, J., Davies, J. A. & CGTP Collaborators, 1 Dec 2017, In : British Journal of Pharmacology. 174, S1, p. S1-S16 16 p.

Research output: Contribution to journalArticleResearchpeer-review

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159 Citations (Scopus)

The potential of stem cells for 21st century neuroscience, II

Haynes, J. M. & Halliwell, R. F., 1 Jun 2017, In : Neurochemistry International. 106, p. 1-2 2 p.

Research output: Contribution to journalEditorialOtherpeer-review

Ticks from diverse genera encode chemokine-inhibitory evasin proteins

Hayward, J., Sanchez, J., Perry, A., Huang, C., Rodriguez Valle, M., Canals, M., Payne, R. J. & Stone, M. J., 22 Sep 2017, In : The Journal of Biological Chemistry. 292, 38, p. 15670-15680 11 p.

Research output: Contribution to journalArticleResearchpeer-review

18 Citations (Scopus)

What determines the magnitude of cellular response for activation of G protein-coupled receptors?

Furness, S. G. B., Wootten, D. & Sexton, P. M., 6 Feb 2017, In : Cell Cycle. 16, 5, p. 392-394 3 p.

Research output: Contribution to journalEditorialOtherpeer-review

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

25 Citations (Scopus)

Accelerated structure-based design of chemically diverse allosteric modulators of a muscarinic G protein-coupled receptor

Miao, Y., Goldfeld, D. A., Moo, E. V., Sexton, P. M., Christopoulos, A., McCammon, J. A. & Valant, C., 20 Sep 2016, In : Proceedings of the National Academy of Sciences of the United States of America. 113, 38, p. E5675-E5684 10 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
48 Citations (Scopus)