Research Output

2013

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: 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: 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: 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)

Inhibition of tumor angiogenesis and growth by a small-molecule multi-FGF receptor blocker with allosteric properties

Bono, F., De Smet, F., Herbert, C., De Bock, K., Georgiadou, M., Fons, P., Tjwa, M., Alcouffe, C., Ny, A., Bianciotto, M., Jonckx, B., Murakami, M., Lanahan, A. A., Michielsen, C., Sibrac, D., Dol-Gleizes, F., Mazzone, M., Zacchigna, S., Herault, J-P., Fischer, C. & 33 others, Rigon, P., Ruiz de Almodovar, C., Claes, F., Blanc, I., Poesen, K., Zhang, Z., Segura, I., Gueguen, G., Bordes, M-F., Lambrechts, D., Broussy, R., van de Wouwer, M., Michaux, C., Shimada, T., Jean, I., Blacher, S., Noel, A., Motte, P., Rom, E., Rakic, J-M., Katsuma, S., Schaeffer, P., Yayon, A., Van Schepdael, A., Schwalbe, H., Gervasio, F. L., Carmeliet, G., Rozensky, J., Dewerchin, M., Simons, M., Christopoulos, A., Herbert, J-M. & Carmeliet, P., 2013, In : Cancer Cell. 23, 4, p. 477 - 488 12 p.

Research output: Contribution to journalArticleResearchpeer-review

95 Citations (Scopus)
26 Citations (Scopus)

Involvement of rho-kinase signaling pathways in nerve evoked and spontaneous contractions of the guinea pig prostate

Lam, M., Kerr, K. P. & Exintaris, B., 2013, In : Journal of Urology. 189, 3, p. 1147 - 1154 8 p.

Research output: Contribution to journalArticleResearchpeer-review

5 Citations (Scopus)

Lipid-based formulations and drug supersaturation: Harnessing the unique benefits of the lipid digestion/absorption pathway

Williams, H. D., Trevaskis, N., Yeap, Y. Y., Anby, M. U., Pouton, C. W. & Porter, C. J., 2013, In : Pharmaceutical Research. 30, 12, p. 2976 - 2992 17 p.

Research output: Contribution to journalArticleResearchpeer-review

68 Citations (Scopus)

Lymphovascular and neural regulation of metastasis: Shared tumour signalling pathways and novel therapeutic approaches

Le, C. P., Karnezis, T., Achen, M. G., Stacker, S. A. & Sloan, E. K., 2013, In : Bailliere's Best Practice and Research in Clinical Anaesthesiology. 27, 4, p. 409 - 425 17 p.

Research output: Contribution to journalArticleResearchpeer-review

6 Citations (Scopus)

Male contraception via simultaneous knockout of a1A-adrenoceptors and P2X1-purinoceptors in mice

White, C. W., Choong, Y-T., Short, J. L., Exintaris, B., Malone, D. T., Allen, A. M., Evans, R. J. & Ventura, S., 2013, In : Proceedings of the National Academy of Sciences of the United States of America. 110, 51, p. 20825 - 20830 6 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
25 Citations (Scopus)

Measurements of ligand bias and functional affinity

Kenakin, T. & Christopoulos, A., 2013, In : Nature Reviews Drug Discovery. 12, 6, p. 483 - 483 1 p.

Research output: Contribution to journalLetterOther

44 Citations (Scopus)

Memantine transport across the mouse blood-brain barrier is mediated by a cationic influx H+ antiporter

Mehta, D., Short, J. L. & Nicolazzo, J., 2013, In : Molecular Pharmaceutics. 10, 12, p. 4491 - 4498 8 p.

Research output: Contribution to journalArticleResearchpeer-review

21 Citations (Scopus)

Minimum active structure of insulin-like peptide 5

Belgi, A., Bathgate, R., Kocan, M., Patil, N., Zhang, S., Tregear, G. W., Wade, J. D. & Hossain, M. A., 2013, In : Journal of Medicinal Chemistry. 56, 23, p. 9509 - 9516 8 p.

Research output: Contribution to journalArticleResearchpeer-review

18 Citations (Scopus)

Minireview: Signal bias, allosterism, and polymorphic variation at the GLP-1R: implications for drug discovery

Koole, C. R., Savage, E. E., Christopoulos, A., Miller, L. J., Sexton, P. & Wootten, D. L., 2013, In : Molecular Endocrinology. 27, 8, p. 1234 - 1244 11 p.

Research output: Contribution to journalArticleResearchpeer-review

25 Citations (Scopus)

Molecular basis for benzodiazepine agonist action at the type 1 cholecystokinin receptor

Harikumar, K. G., Cawston, E. E., Lam, P. C. H., Patil, A., Orry, A., Henke, B., Abagyan, R., Christopoulos, A., Sexton, P. & Miller, L. J., 2013, In : The Journal of Biological Chemistry. 288, 29, p. 21082 - 21095 14 p.

Research output: Contribution to journalArticleResearchpeer-review

11 Citations (Scopus)

Molecular methods for the study of signal transduction in plants

Irving, H. R. & Gehring, C. A., 2013, Cyclic Nucleotide Signaling in Plants. Gehring, C. (ed.). USA: Humana Press, p. 1 - 11 11 p.

Research output: Chapter in Book/Report/Conference proceedingChapter (Book)Other

6 Citations (Scopus)

N-aryl piperazine metabotropic glutamate receptor 5 positive allosteric modulators possess efficacy in preclinical models of NMDA hypofunction and cognitive enhancement

Gregory, K. J., Herman, E. J., Ramsey, A. J., Hammond, A. S., Byun, N., Stauffer, S. R., Manka, J. T., Jadhav, S. B., Bridges, T. M., Weaver, C. D., Niswender, C. M., Steckler, T., Drinkenburg, W. H., Ahnaou, A., Lavreysen, H., Macdonald, G. J., Bartolome, J., Mackie, C., Hrupka, B. J., Caron, M. G. G. & 4 others, Daigle, T. L., Lindsley, C. W., Conn, P. J. & Jones, C. K., 2013, In : Journal of Pharmacology and Experimental Therapeutics. 347, 2, p. 438 - 457 20 p.

Research output: Contribution to journalArticleResearchpeer-review

35 Citations (Scopus)

Orthosteric binding of rho-Da1a, a natural peptide of snake venom interacting selectively with the alpha(1A)-Adrenoceptor

Maiga, A., Merlin, J., Marcon, E., Rouget, C., Larregola, M., Gilquin, B., Fruchart-Gaillard, C., Lajeunesse, E., Marchetti, C., Lorphelin, A., Bellanger, L., Summers, R. J., Hutchinson, D. S., Evans, B. A., Servent, D. & Gilles, N., 2013, In : PLoS ONE. 8, 7, 11 p., e68841.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File
5 Citations (Scopus)

PEGylation of interferon alpha 2 improves lymphatic exposure after subcutaneous and intravenous administration and improves antitumour efficacy against lymphatic breast cancer metastases

Kaminskas, L. M., Ascher, D. B., McLeod, V. M., Herold, M., Le, C. P., Sloan, E. K. & Porter, C. J., 2013, In : Journal of Controlled Release. 168, 2, p. 200 - 208 9 p.

Research output: Contribution to journalArticleResearchpeer-review

48 Citations (Scopus)

Pharmacology and structure of isolated conformations of the adenosine A2A receptor define ligand efficacy

Bennett, K. A., Tehan, B., Lebon, G., Tate, C. G., Weir, M., Marshall, F. H. & Langmead, C. J., May 2013, In : Molecular Pharmacology. 83, 5, p. 949-958 10 p.

Research output: Contribution to journalArticleResearchpeer-review

40 Citations (Scopus)

Pharmacology of metabotropic glutamate receptor allosteric modulators: Structural basis and therapeutic potential for CNS disorders

Gregory, K. J., Noetzel, M. J. & Niswender, C. M., 2013, Progress in Molecular Biology and Translational Science. Kenakin, T. (ed.). Oxford UK: Elsevier, p. 61 - 121 61 p.

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

30 Citations (Scopus)

Plant natriuretic peptides: Systemic regulators of plant homeostasis and defense that can affect cardiomyoblasts

Gehring, C. A. & Irving, H. R., 2013, In : Journal of Investigative Medicine. 61, 5, p. 823 - 826 4 p.

Research output: Contribution to journalArticleOtherpeer-review

4 Citations (Scopus)

Pluripotent stem cell-derived dopaminergic neurons as models of neurodegeneration

Watmuff, B., Hartley, B. J., Hunt, C., Pouton, C. W. & Haynes, J. M., 2013, In : Future Neurology. 8, 6, p. 649-661 13 p.

Research output: Contribution to journalArticleResearchpeer-review

1 Citation (Scopus)
110 Citations (Scopus)

Polymyxin B induces apoptosis in kidney proximal tubular cells

Azad, M. A. K., Finnin, B. A. L., Poudyal, A., Davis, K. E., Li, J., Hill, P. A., Nation, R. L., Velkov, T. & Li, J., 2013, In : Antimicrobial Agents and Chemotherapy. 57, 9, p. 4329 - 4335 7 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
44 Citations (Scopus)

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

13 Citations (Scopus)

Probing the metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulator (PAM) binding pocket: Discovery of point mutations that engender a "molecular switch" in PAM pharmacology

Gregory, K. J., Nguyen, E. D., Reiff, S. D., Squire, E. F., Stauffer, S. R., Lindsley, C. W., Meiler, J. & Conn, P. J., 2013, In : Molecular Pharmacology. 83, 5, p. 991 - 1006 16 p.

Research output: Contribution to journalArticleResearchpeer-review

62 Citations (Scopus)

Protease-activated receptor 2 (PAR2) protein and transient receptor potential vanilloid 4 (TRPV4) protein coupling is required for sustained inflammatory signaling

Poole, D. P., Amadesi, S., Veldhuis, N. A., Abogadie, F. C., Lieu, T. M., Darby, W., Liedtke, W., Lew, M. J., McIntyre, P. B. & Bunnett, N. W., 2013, In : The Journal of Biological Chemistry. 288, 8, p. 5790 - 5802 13 p.

Research output: Contribution to journalArticleResearchpeer-review

91 Citations (Scopus)

Recent advances in understanding GLP-1R (glucagon-like peptide-1 receptor) function

Koole, C. R., Pabreja, K., Savage, E. E., Wootten, D. L., Furness, S. G. B., Miller, L. J., Christopoulos, A. & Sexton, P., 2013, In : Biochemical Society Transactions. 41, 1, p. 172 - 179 8 p.

Research output: Contribution to journalArticleResearchpeer-review

46 Citations (Scopus)

Receptor activity-modifying protein-dependent impairment of calcitonin receptor splice variant Delta(1-47)hCT((a)) function

Qi, T., Dong, M. DONG., Watkins, H. A., Wootten, D. L., Miller, L. J. & Hay, D. L., 2013, In : British Journal of Pharmacology. 168, 3, p. 644 - 657 14 p.

Research output: Contribution to journalArticleResearchpeer-review

28 Citations (Scopus)
10 Citations (Scopus)

Regulation of G protein-coupled receptors by allosteric ligands

Lane, J. R. D., Abdul Ridha, A. & Canals, M., 2013, In : ACS Chemical Neuroscience. 4, 4, p. 527 - 534 8 p.

Research output: Contribution to journalArticleResearchpeer-review

31 Citations (Scopus)

Relaxin family peptides and their receptors

Bathgate, R., Halls, M. L., van der Westhuizen, E. T., Callander, G., Kocan, M. & Summers, R. J., 2013, In : Physiological Reviews. 93, 1, p. 405 - 480 76 p.

Research output: Contribution to journalArticleResearchpeer-review

276 Citations (Scopus)

Rho kinase activation mediates adrenergic and cholinergic smooth muscle contractile responses in the mouse prostate gland

White, C. W., Short, J. L. & Ventura, S., 2013, In : European Journal of Pharmacology. 721, p. 313 - 321 9 p.

Research output: Contribution to journalArticleResearchpeer-review

7 Citations (Scopus)

Sensitization of peripheral sensory nerves by mediators from colonic biopsies of diarrhea-predominant irritable bowel syndrome patients: A role for PAR2

Valdez-Morales, E., Overington, J., Guerrero-Alba, R., Ochoa-Cortes, F., Ibeakanma, C., Spreadbury, I., Bunnett, N. W., Beyak, M. & Vanner, S., 2013, In : The American Journal of Gastroenterology. 108, 10, p. 1634 - 1643 10 p.

Research output: Contribution to journalArticleResearchpeer-review

60 Citations (Scopus)

Signalling bias in new drug discovery: detection, quantification and therapeutic impact

Kenakin, T. & Christopoulos, A., 2013, In : Nature Reviews Drug Discovery. 12, 3, p. 205 - 216 12 p.

Research output: Contribution to journalArticleResearchpeer-review

460 Citations (Scopus)

Social stress up-regulates inflammatory gene expression in the leukocyte transcriptome via ?-adrenergic induction of myelopoiesis

Powell, N. D., Sloan, E. K., Bailey, M. T., Arevalo, J. MG., Miller, G. E., Chen, E., Kobor, M. S., Reader, B. F., Sheridan, J. F. & Cole, S. W., 2013, In : Proceedings of the National Academy of Sciences of the United States of America. 110, 41, p. 16574 - 16579 6 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
256 Citations (Scopus)

Strategies for the development of conotoxins as new therapeutic leads

Brady, R., Baell, J. B. & Norton, R. S., 2013, In : Marine Drugs. 11, 7, p. 2293 - 2313 21 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
22 Citations (Scopus)