Research Output

2013

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)
27 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)
111 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

277 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)

Strategies to address low drug solubility in discovery and development

Williams, H. D., Trevaskis, N., Charman, S. A., Shanker, R., Charman, W. N., Pouton, C. W. & Porter, C. J., 2013, In : Pharmacological Reviews. 65, 1, p. 315 - 499 185 p.

Research output: Contribution to journalArticleResearchpeer-review

769 Citations (Scopus)

Structural and functional characterization of receptor kinases with nucleotide cyclase activity

Muleya, V., Wheeler, J. & Irving, H. R., 2013, Cyclic Nucleotide Signaling in Plants. Gehring, C. (ed.). USA: Humana Press, p. 175 - 194 20 p.

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

5 Citations (Scopus)

Structural basis for modulation of a G-protein-coupled receptor by allosteric drugs

Dror, R., Green, H. F., Valant, C., Borhani, D. W., Valcourt, J. R., Pan, A. C., Arlow, D. H., Canals, M., Lane, J. R. D., Rahmani, R. S., Baell, J. B., Sexton, P., Christopoulos, A. & Shaw, D. E., 2013, In : Nature. 503, 7475, p. 295 - 299 5 p.

Research output: Contribution to journalArticleResearchpeer-review

268 Citations (Scopus)

Structural biology: meet the B family

Sexton, P. & Wootten, D. L., 2013, In : Nature. 499, 7459, p. 417 - 418 2 p.

Research output: Contribution to journalLetterOther

5 Citations (Scopus)

Structure-based ligand discovery targeting orthosteric and allosteric pockets of dopamine receptors

Lane, J. R. D., Chubukov, P., Liu, W., Canals, M., Cherezov, V., Abagyan, R., Stevens, R. C. & Katritch, V., 2013, In : Molecular Pharmacology. 84, 6, p. 794 - 807 14 p.

Research output: Contribution to journalArticleResearchpeer-review

61 Citations (Scopus)

Supra-physiological efficacy at GPCRs: superstition or super agonists?

Langmead, C. J. & Christopoulos, A., 2013, In : British Journal of Pharmacology. 169, 2, p. 353 - 356 4 p.

Research output: Contribution to journalArticleOtherpeer-review

20 Citations (Scopus)

Sympathetic nervous system regulation of metastasis

Pimentel, M., Chai, M. G., Le, C. P., Cole, S. W. & Sloan, E. K., 2013, Metastatic Cancer: Clinical and Biological Perspectives. Jandial, R. (ed.). Austin Texas USA: Landes Bioscience, p. 169 - 179 11 p.

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

6 Citations (Scopus)

The bile acid receptor TGR5 does not interact with b-arrestins or traffic to endosomes but transmits sustained signals from plasma membrane rafts

Jensen, D. D., Godfrey, C. B., Niklas, C., Canals, M., Kocan, M., Poole, D. P., Murphy, J. E., Alemi, F., Cottrell, G. S., Korbmacher, C., Lambert, N., Bunnett, N. W. & Corvera, C. U., 2013, In : The Journal of Biological Chemistry. 288, 32, p. 22942 - 22960 19 p.

Research output: Contribution to journalArticleResearchpeer-review

59 Citations (Scopus)

The receptor TGR5 mediates the prokinetic actions of intestinal bile acids and is required for normal defecation in mice

Alemi, F., Poole, D. P., Chiu, J. V., Schoonjans, K., Cattaruzza, F., Grider, J. R., Bunnett, N. W. & Corvera, C. U., 2013, In : Gastroenterology. 144, 1, p. 145 - 154 10 p.

Research output: Contribution to journalArticleResearchpeer-review

133 Citations (Scopus)

The TGR5 receptor mediates bile acid-induced itch and analgesia

Alemi, F., Kwon, E., Poole, D. P., Lieu, T. M., Lyo, V., Cattaruzza, F., Cevikbas, F., Steinhoff, M., Nassini, R., Materazzi, S., Guerrero-Alba, R., Valdez-Morales, E., Cottrell, G. S., Schoonjans, K., Geppetti, P., Vanner, S., Bunnett, N. W. & Corvera, C. U., 2013, In : Journal of Clinical Investigation. 123, 4, p. 1513 - 1530 18 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
186 Citations (Scopus)

Toward the establishment of standardized in vitro tests for lipid-based formulations, part 3: Understanding supersaturation versus precipitation potential during the in vitro digestion of type I, II, IIIA, IIIB and IV lipid-based formulations

Williams, H. D., Sassene, P. J., Kleberg, K., Calderone, M., Igonin, A., Jule, E., Vertommen, J., Blundell, R., Benameur, H., Mullertz, A., Pouton, C. W. & Porter, C. J., 2013, In : Pharmaceutical Research. 30, 12, p. 3059 - 3076 18 p.

Research output: Contribution to journalArticleResearchpeer-review

69 Citations (Scopus)

Transient receptor potential ankyrin 1 mediates chronic pancreatitis pain in mice

Cattaruzza, F., Johnson, C., Leggit, A., Grady, E. F., Schenk, A. K., Cevikbas, F., Cedron, W., Bondada, S., Kirkwood, R., Malone, B., Steinhoff, M., Bunnett, N. W. & Kirkwood, K. S., 2013, In : American Journal of Physiology - Gastrointestinal and Liver Physiology. 304, 11, p. 1002 - 1012 11 p.

Research output: Contribution to journalArticleResearchpeer-review

26 Citations (Scopus)