Research Output

2012

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

5 Citations (Scopus)

The best of both worlds? Bitopic orthosteric/allosteric ligands of G protein - coupled receptors

Valant, C., Lane, J., Sexton, P. & Christopoulos, A., 2012, In : Annual Review of Pharmacology and Toxicology. 53, p. 153 - 178 26 p.

Research output: Contribution to journalArticleResearchpeer-review

118 Citations (Scopus)

The expression of calcitonin receptor detected in malignant cells of the brain tumour glioblastoma multiforme and functional properties in the cell line A172

Wookey, P. J., McLean, C. A., Hwang, P. Y. K., Furness, S. G. B., Nguyen, S., Kourakis, A., Hare, D. L. & Rosenfeld, J. V., 2012, In : Histopathology. 60, 6, p. 895 - 910 16 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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12 Citations (Scopus)

The involvement of a Na+ - and Cl- -dependent transporter in the brain uptake of amantadine and rimantadine

Kooijmans, S. A. A., Senyschyn, D., Mezhiselvam, M. M., Morizzi, J., Charman, S. A., Weksler, B., Romero, I-A., Couraud, P. & Nicolazzo, J., 2012, In : Molecular Pharmaceutics. 9, p. 883 - 893 11 p.

Research output: Contribution to journalArticleResearchpeer-review

14 Citations (Scopus)

Themed section: Molecular Pharmacology of G protein-coupled receptors

Summers, R., 2012, In : British Journal of Pharmacology. 165, 6, p. 1609 - 1612 4 p.

Research output: Contribution to journalLetterOther

1 Citation (Scopus)

Toward the establishment of standardized in vitro tests for lipid-based formulations, Part 1: Method parameterization and comparison of in vitro digestion profiles across a range of representative formulations

Williams, H. D., Sassene, P. J., Kleberg, K., Bakala-N'Goma, J-C., Calderone, M., Jannin, V., Igonin, A., Partheil, A., Marchaud, D., Jule, E., Vertommen, J., Maio, M., Blundell, R., Benameur, H., Carriere, F., Mullertz, A., Porter, C. J. & Pouton, C. W., 2012, In : Journal of Pharmaceutical Sciences. 101, 9, p. 3360 - 3380 21 p.

Research output: Contribution to journalArticleResearchpeer-review

156 Citations (Scopus)

Xenobiotics and loss of cell adhesion drive distinct transcriptional outcomes by aryl hydrocarbon receptor signaling

Hao, N., Lee, K. L., Furness, S. G. B., Bosdotter, C., Poellinger, L. & Whitelaw, M. L., 2012, In : Molecular Pharmacology. 82, 6, p. 1082 - 1093 12 p.

Research output: Contribution to journalArticleResearchpeer-review

20 Citations (Scopus)

A critical review of the role of Fc gamma receptor polymorphisms in the response to monoclonal antibodies in cancer

Mellor, J. D., Brown, M., Irving, H. R., Zalcberg, J. R. & Dobrovic, A., 2013, In : Journal of Hematology & Oncology. 6, p. 1 - 10 10 p., 1.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
174 Citations (Scopus)

Activation and allosteric modulation of a muscarinic acetylcholine receptor

Kruse, A. C., Ring, A. M., Manglik, A., Hu, J., Hu, K., Eitel, K., Hubner, H., Pardon, E., Valant, C., Sexton, P., Christopoulos, A., Felder, C. C., Gmeiner, P., Steyaert, J., Weis, W., Garcia, K. C., Wess, J. & Kobilka, B., 2013, In : Nature. 504, 7478, p. 101 - 106 6 p.

Research output: Contribution to journalArticleResearchpeer-review

533 Citations (Scopus)

Activation of G protein-coupled bile acid receptor, TGR5, induces smooth muscle relaxation via both Epac- and PKA-mediated inhibition of RhoA/Rho kinase pathway

Rajagopal, S., Kumar, D. P., Mahavadi, S., Bhattacharya, S., Zhou, R., Corvera, C. U., Bunnett, N. W., Grider, J. R. & Murthy, K. S., 2013, In : American Journal of Physiology - Gastrointestinal and Liver Physiology. 304, 5, p. G527 - G535 9 p.

Research output: Contribution to journalArticleResearchpeer-review

43 Citations (Scopus)

A cyclic nucleotide sensitive promoter reporter system suitable for bacteria and plant cells

Wheeler, J., Freihat, L. & Irving, H. R., 2013, In : BMC Biotechnology. 13, 97, p. 1 - 10 10 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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10 Citations (Scopus)

Age-related changes in the innervation of the prostate gland: implications for prostate cancer initiation and progression

White, C. W., Xie, J. H. & Ventura, S., Jul 2013, In : Organogenesis. 9, 3, p. 206-215 10 p.

Research output: Contribution to journalReview ArticleResearchpeer-review

23 Citations (Scopus)

Agonist-biased trafficking of somatostatin receptor 2A in enteric neurons

Zhao, P., Canals, M., Murphy, J. E., Klingler, D., Eriksson, E. M., Pelayo, J-C., Hardt, M., Bunnett, N. W. & Poole, D. P., 2013, In : The Journal of Biological Chemistry. 288, 36, p. 25689 - 25700 12 p.

Research output: Contribution to journalArticleResearchpeer-review

24 Citations (Scopus)

Allosteric approaches to GPCR drug discovery

Lane, J. R. & Ijzerman, A. P., 2013, In : Drug Discovery Today: Technologies. 10, 2

Research output: Contribution to journalEditorialOtherpeer-review

3 Citations (Scopus)

Allosteric modulation of a chemogenetically modified G protein-coupled receptor

Abdul Ridha, A., Lane, J. R. D., Sexton, P., Canals, M. & Christopoulos, A., 2013, In : Molecular Pharmacology. 83, 2, p. 521 - 530 10 p.

Research output: Contribution to journalArticleResearchpeer-review

16 Citations (Scopus)

Altered brain uptake of therapeutics in a triple transgenic mouse model of alzheimer's disease

Mehta, D., Short, J. L. & Nicolazzo, J., 2013, In : Pharmaceutical Research. 30, 11, p. 2868 - 2879 12 p.

Research output: Contribution to journalArticleResearchpeer-review

35 Citations (Scopus)

An allosteric modulator of the adenosine A1 receptor improves cardiac function following ischaemia in murine isolated hearts

Butcher, A., Scammells, P. J., White, P. J., Devine, S. & Rose'Meyer, R. B., 2013, In : Pharmaceuticals. 6, 4, p. 546 - 556 11 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
6 Citations (Scopus)

An anti-inflammatory role for leukemia inhibitory factor receptor signaling in regenerating skeletal muscle

Hunt, L. C., Upadhyay, A., Jazayeri, J., Tudor, E. M. & White, J. D., 2013, In : Histochemistry and Cell Biology. 139, 1, p. 13 - 34 22 p.

Research output: Contribution to journalArticleResearchpeer-review

26 Citations (Scopus)

An examination of cardiovascular collapse induced by eastern brown snake (Pseudonaja textilis) venom

Chaisakul, J., Isbister, G. K., Kuruppu, D. M. S., Konstantakopoulos, N. & Hodgson, W. C., 2013, In : Toxicology Letters. 221, 3, p. 205 - 211 7 p.

Research output: Contribution to journalArticleResearchpeer-review

11 Citations (Scopus)

A novel androgen signalling pathway uses dihydrotestosterone, but not testosterone, to activate the EGF receptor signalling cascade in prostate stromal cells

Oliver, V. L., Poulios, K., Ventura, S. & Haynes, J. M., 2013, In : British Journal of Pharmacology. 170, 3, p. 592 - 601 10 p.

Research output: Contribution to journalArticleResearchpeer-review

7 Citations (Scopus)

A novel metabotropic glutamate receptor 5 positive allosteric modulator acts at a unique site and confers stimulus bias to mGlu5 signaling

Noetzel, M. J., Gregory, K. J., Vinson, P. N., Manka, J. T., Stauffer, S. R., Lindsley, C. W., Niswender, C. M., Xiang, Z. & Conn, P. J., Apr 2013, In : Molecular Pharmacology. 83, 4, p. 835-847 13 p.

Research output: Contribution to journalArticleResearchpeer-review

62 Citations (Scopus)

Arresting inflammation: Contributions of plasma membrane and endosomal signalling to neuropeptide-driven inflammatory disease

Cattaruzza, F., Poole, D. P. & Bunnett, N. W., 2013, In : Biochemical Society Transactions. 41, 1, p. 137 - 143 7 p.

Research output: Contribution to journalArticleResearchpeer-review

10 Citations (Scopus)

A simple method to generate stable cell lines for the analysis of transient protein-protein interactions

Savage, E. E., Wootten, D. L., Christopoulos, A., Sexton, P. & Furness, S. G. B., 2013, In : BioTechniques. 54, 4, p. 217 - 221 5 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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11 Citations (Scopus)

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

62 Citations (Scopus)

Bioluminescent orthotopic model of pancreatic cancer progression

Chai, M. G., Kim-Fuchs, C., Angst, E. & Sloan, E. K., 1 Jun 2013, In : Journal of Visualized Experiments. 2013, 76, e50395.

Research output: Contribution to journalArticleResearchpeer-review

19 Citations (Scopus)

Bridging the gap: bitopic ligands of G-protein-coupled receptors

Lane, J. R. D., Sexton, P. M. & Christopoulos, A., 2013, In : Trends in Pharmacological Sciences. 34, 1, p. 59 - 66 8 p.

Research output: Contribution to journalArticleResearchpeer-review

102 Citations (Scopus)

Calcium-sensing receptor-dependent activation of CREB phosphorylation in HEK293 cells and human parathyroid cells

Avlani, V. A., Ma, W., Mun, H., Leach, K., Delbridge, L., Christopoulos, A. & Conigrave, A., 2013, In : American Journal of Physiology - Endocrinology and Metabolism. 304, 10, p. 1097 - 1104 8 p.

Research output: Contribution to journalArticleResearchpeer-review

24 Citations (Scopus)

CGRP/adrenomedullin

Wootten, D. L., Tilakaratne, N., Christopoulos, A. & Sexton, P., 2013, Handbook of Biologically Active Peptides. Kastin, A. J. (ed.). Second Edition ed. San Diego CA USA: Elsevier, p. 744 - 751 8 p.

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

1 Citation (Scopus)

Characterization of forebrain neurons derived from late-onset Huntington's disease human embryonic stem cell lines

Niclis, J. C., Pinar, A., Haynes, J. M., Alsanie, W. F., Jenny, R. A., Dottori, M. & Cram, D. S., 2013, In : Frontiers in Cellular Neuroscience. 7, 37, p. 1 - 13 13 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
25 Citations (Scopus)

Chronic activation of the low affinity site of beta -adrenoceptors stimulates haemodynamics but exacerbated pressure-overload cardiac remodelling

Kiriazis, H., Tugiono, N., Xu, Q., Gao, X-M., Jennings, N., Ming, Z., Su, Y., Klenowski, P., Summers, R. J., Kaumann, A., Molenaar, P. & Du, X-J., 2013, In : British Journal of Pharmacology. 170, 2, p. 352 - 365 14 p.

Research output: Contribution to journalArticleResearchpeer-review

1 Citation (Scopus)

Correction to: A novel metabotropic glutamate receptor 5 positive allosteric modulator acts at a unique site and confers stimulus bias to mGlu5 signaling

Noetzel, M. J., Gregory, K. J., Vinson, P. N., Manka, J. T., Stauffer, S. R., Lindsley, C. W., Niswender, C. M., Xiang, Z. & Conn, P. J., Oct 2013, In : Molecular Pharmacology. 84, 4, p. 654 1 p.

Research output: Contribution to journalComment / DebateOtherpeer-review

Deleterious effects of soluble beta amyloid on cognition, antagonism by saline and noradrenaline, a role for microglia

Gibbs, M. E. & Gibbs, C. L., 2013, In : Neuroscience. 230, p. 62 - 71 10 p.

Research output: Contribution to journalArticleResearchpeer-review

5 Citations (Scopus)

Development of M1 mAChR allosteric and bitopic ligands: Prospective therapeutics for the treatment of cognitive deficits

Davie, B. J., Christopoulos, A. & Scammells, P. J., 2013, In : ACS Chemical Neuroscience. 4, 7, p. 1026 - 1048 23 p.

Research output: Contribution to journalArticleResearchpeer-review

55 Citations (Scopus)

Differential activation and modulation of the glucagon-like peptide-1 receptor by small molecule ligands

Wootten, D. L., Savage, E. E., Willard, F. S., Bueno, A. B., Sloop, K. W., Christopoulos, A. & Sexton, P., 2013, In : Molecular Pharmacology. 83, 4, p. 822 - 834 13 p.

Research output: Contribution to journalArticleResearchpeer-review

56 Citations (Scopus)
5 Citations (Scopus)

DNA-dependent protein kinase is a context dependent regulator of Lmx1a and midbrain specification

Hunt, C. J., Fabb, S. A., Pouton, C. W. & Haynes, J. M., 2013, In : PLoS ONE. 8, 10, 12 p., e78759.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
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3 Citations (Scopus)

Does the autonomic nervous system contribute to the initiation and progression of prostate cancer?

Ventura, S. & Evans, B. A., 2013, In : Asian Journal of Andrology. 15, 6, p. 715 - 716 2 p.

Research output: Contribution to journalArticleResearchpeer-review

5 Citations (Scopus)

Effects of imatinib mesylate on the spontaneous activity generated by the guinea-pig prostate

Lam, M. H. S., Dey, A., Lang, R. J. & Exintaris, B., 2013, In : BJU International. 112, 4, p. 398 - 405 8 p.

Research output: Contribution to journalArticleResearchpeer-review

3 Citations (Scopus)

Emerging paradigms in GPCR allostery: implications for drug discovery

Wootten, D. L., Christopoulos, A. & Sexton, P., 2013, In : Nature Reviews Drug Discovery. 12, 8, p. 630 - 644 15 p.

Research output: Contribution to journalArticleResearchpeer-review

254 Citations (Scopus)

Erratum: Glucose-Neopentyl Glycol (GNG) amphiphiles for membrane protein study (Chemical Communications (2013) 49 (2287-2289) DOI: 10.1039/c2cc36844g)

Chae, P. S., Rana, R. R., Gotfryd, K., Rasmussen, S. G. F., Kruse, A. C., Cho, K. H., Capaldi, S., Carlsson, E., Kobilka, B., Loland, C. J., Gether, U., Banerjee, S., Byrne, B., Lee, J. K. & Gellman, S. H., 2013, In : Chemical Communications. 49, 100, p. 11821-11822 2 p.

Research output: Contribution to journalComment / DebateResearchpeer-review

Erratum: A new class of amphiphiles bearing rigid hydrophobic groups for solubilization and stabilization of membrane protein (Chemistry - A European Journal (2012) 31)

Chae, P. S., Rasmussen, S. G. F., Rana, R. R., Gotfryd, K., Kruse, A. C., Manglik, A., Cho, K. H-Y., Nurva, S., Gether, U., Guan, L., Loland, C. J., Byrne, B. G., Kobilka, B. K. & Gellman, S. H., 15 Apr 2013, In : Chemistry - A European Journal. 19, 16, p. 4964 1 p.

Research output: Contribution to journalComment / DebateOtherpeer-review

Erratum: Differential activation and modulation of the glucagon-like peptide-1 receptor by small molecular ligands (Molecular Pharmacology (2013) 83 (822-834))

Wootten, D., Savage, E. E., Willard, F. S., Bueno, A. B., Sloop, K. W., Christopoulos, A. & Sexton, P. M., Jul 2013, In : Molecular Pharmacology. 84, 1, p. 170 1 p.

Research output: Contribution to journalComment / DebateOtherpeer-review

Evaluation of the structural determinants of polymeric precipitation inhibitors using solvent shift methods and principle component analysis

Warren, D., Bergstrom, C. A. S., Benameur, H., Porter, C. J. & Pouton, C. W., 2013, In : Molecular Pharmaceutics. 10, 8, p. 2823 - 2848 26 p.

Research output: Contribution to journalArticleResearchpeer-review

42 Citations (Scopus)

Exploration of allosteric agonism structure-activity relationships within an acetylene series of metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulators (PAMs)...

Turlington, M. L., Noetzel, M. J., Chun, A. C., Zhou, Y., Gogliotti, R. D., Nguyen, E. D., Gregory, K. J., Vinson, P. N., Rook, J. M., Gogi, K., Xiang, Z., Bridges, T. M., Daniels, J. S., Jones, C. K., Niswender, C. M., Meiler, J., Conn, P. J., Lindsley, C. W. & Stauffer, S. R., 2013, In : Journal of Medicinal Chemistry. 56, 20, p. 7976 - 7996 21 p.

Research output: Contribution to journalArticleResearchpeer-review

24 Citations (Scopus)

Fine-tuning of GPCR signals by intracellular G protein modulators

Zhao, P., Cladman, W., Van Tol, H. H. M. & Chidiac, P., 2013, Oligomerization and Allosteric Modulation in G-Protein Coupled Receptors. Kenakin, T. (ed.). 1st ed. Oxford UK: Elsevier, Vol. 115. p. 421-453 33 p. (Progress in Molecular Biology and Translational Science; vol. 115).

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

10 Citations (Scopus)

Functional characterization on invertebrate and vertebrate tissues of tachykinin peptides from octopus venoms

Ruder, T., Ali, S. A., Ormerod, K., Brust, A., Roymanchadi, M-L., Ventura, S., Undheim, E. A. B., Jackson, T. N. W., Mercier, A. J., King, G. F., Alewood, P. F. & Fry, B. G., 2013, In : Peptides. 47, p. 71 - 76 6 p.

Research output: Contribution to journalArticleResearchpeer-review

9 Citations (Scopus)

Glyceride lipid formulations: Molecular dynamics modeling of phase behavior during dispersion and molecular interactions between drugs and excipients

Warren, D., King, D. T., Benameur, H., Pouton, C. W. & Chalmers, D. K., 2013, In : Pharmaceutical Research. 30, 12, p. 3238 - 3253 16 p.

Research output: Contribution to journalArticleResearchpeer-review

19 Citations (Scopus)

Impact of chronic congestive heart failure on pharmacokinetics and vasomotor effects of infused nitrite

Maher, A. R., Arif, S., Madhani, M., Abozguia, K., Ahmed, I., Fernandez, B. O., Feelisch, M., O'Sullivan, A. G., Christopoulos, A., Sverdlov, A. L., Ngo, D., Dautov, R., James, P. E., Horowitz, J. D. & Frenneaux, M. P., 2013, In : British Journal of Pharmacology. 169, 3, p. 659 - 670 12 p.

Research output: Contribution to journalArticleResearchpeer-review

19 Citations (Scopus)

Impact of clinically relevant mutations on the pharmacoregulation and signaling bias of the calcium-sensing receptor by positive and negative allosteric modulators

Leach, K., Wen, C., Cook, A. E., Sexton, P., Conigrave, A. & Christopoulos, A., 2013, In : Endocrinology. 154, 3, p. 1105 - 1116 12 p.

Research output: Contribution to journalArticleResearchpeer-review

54 Citations (Scopus)