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Research Output 2000 2019

  • 22 Article
  • 2 Conference Paper
  • 1 Chapter (Book)
  • 1 Comment / Debate
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

Erratum to: Structural insights into binding specificity, efficacy and bias of a β2AR partial agonist (Nature Chemical Biology, (2018), 14, 11, (1059-1066), 10.1038/s41589-018-0145-x)

Masureel, M., Zou, Y., Picard, L. P., van der Westhuizen, E., Mahoney, J. P., Rodrigues, J. P. G. L. M., Mildorf, T. J., Dror, R. O., Shaw, D. E., Bouvier, M., Pardon, E., Steyaert, J., Sunahara, R. K., Weis, W. I., Zhang, C. & Kobilka, B. K., 1 Feb 2019, In : Nature Chemical Biology. 15, 2, 1 p.

Research output: Contribution to journalComment / DebateOtherpeer-review

Exploring use of unsupervised clustering to associate signaling profiles of GPCR ligands to clinical response

Benredjem, B., Gallion, J., Pelletier, D., Dallaire, P., Charbonneau, J., Cawkill, D., Nagi, K., Gosink, M., Lukasheva, V., Jenkinson, S., Ren, Y., Somps, C., Murat, B., Van Der Westhuizen, E., Le Gouill, C., Lichtarge, O., Schmidt, A., Bouvier, M. & Pineyro, G., 9 Sep 2019, In : Nature Communications. 10, 1, 15 p., 4075.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File

Structural insights into binding specificity, efficacy and bias of a β 2 AR partial agonist

Masureel, M., Zou, Y., Picard, L. P., van der Westhuizen, E., Mahoney, J. P., Rodrigues, J. P. G. L. M., Mildorf, T. J., Dror, R. O., Shaw, D. E., Bouvier, M., Pardon, E., Steyaert, J., Sunahara, R. K., Weis, W. I., Zhang, C. & Kobilka, B. K., 1 Nov 2018, In : Nature Chemical Biology. 14, 11, p. 1059-1066 8 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File
2017

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

2015

Endogenous allosteric modulators of G protein-coupled receptors

Van Der Westhuizen, E. T., Valant, C., Sexton, P. & Christopoulos, A., 2015, In : Journal of Pharmacology and Experimental Therapeutics. 353, 2, p. 246 - 260 15 p.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File
2014

Quantification of ligand bias for clinically relevant beta2-adrenergic receptor ligands: Implications for drug taxonomy

van der Westhuizen, E. T., Breton, B., Christopoulos, A. & Bouvier, M., 2014, In : Molecular Pharmacology. 85, 3, p. 492 - 509 18 p.

Research output: Contribution to journalArticleResearchpeer-review

2013

Probing the Functional Selectivity of β-adrenergic Receptors Reveals New Signaling Modes and Potential Therapeutic Applications

van der Westhuizen, E., Stallaert, W., Murat, B., Audet, M., Galandrin, S., Lagacé, M. & Bouvier, M., Dec 2013, Catecholamine Research in the 21st Century: Abstracts and Graphical Abstracts, 10th International Catecholamine Symposium, 2012. Elsevier, p. 112 1 p.

Research output: Chapter in Book/Report/Conference proceedingConference PaperOtherpeer-review

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

2012

Impedance responses reveal beta2-adrenergic receptor signaling pluridimensionality and allow classification of ligands with distinct signaling profiles

Stallaert, W., Dorn, J. F., van der Westhuizen, E. T., Audet, M. & Bouvier, M., 2012, In : PLoS ONE. 7, 1, 14 p., e29420.

Research output: Contribution to journalArticleResearchpeer-review

Open Access
File
2011

Insulin-like peptide 5 (INSL5)

Van Der Westhuizen, E. T., 2011, xPharm: The Comprehensive Pharmacology Reference. Enna, S. J. & Bylund, D. B. (eds.). Elsevier, p. 1-4 4 p.

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

2010

H2 relaxin is a biased ligand relative to H3 relaxin at the relaxin family peptide receptor 3 (RXFP3) [S]

van der Westhuizen, E. T., Christopoulos, A., Sexton, P., Wade, J. & Summers, R., 2010, In : Molecular Pharmacology. 77, 5, p. 759 - 772 14 p.

Research output: Contribution to journalArticleResearchpeer-review

Relaxin family peptide receptor (RXFP1) coupling to Galphai3, involves the C-terminal Arg752 and localization within membrane raft microdomains

Halls, M. L., van der Westhuizen, E. T., Wade, J. D., Evans, B. A., Bathgate, R. A. D. & Summers, R. J., 2009, In : Molecular Pharmacology. 75, 2, p. 415 - 428 14 p.

Research output: Contribution to journalArticleResearchpeer-review

Roles of the receptor, the ligand, and the cell in the signal transduction pathways utilized by the relaxin family peptide receptors 1-3

Summers, R. J., Bathgate, R. A. D., Wade, J. D., van der Westhuizen, E. T. & Halls, M. L., 2009, In : Annals of the New York Academy of Sciences. 1160, p. 99 - 104 6 p.

Research output: Contribution to journalArticleResearchpeer-review

2008

Relaxin family peptide receptors - from orphans to therapeutic targets

van der Westhuizen, E. T., Halls, M. L., Samuel, C. S., Bathgate, R., Unemori, E. N., Sutton, S. W. & Summers, R. J., 2008, In : Drug Discovery Today. 13, 15-16, p. 640 - 651 12 p.

Research output: Contribution to journalArticleResearchpeer-review

2007

Relaxin family peptide receptors - Former orphans reunite with their parent ligands to activate multiple signalling pathways

Halls, M. L., van der Westhuizen, E. T., Bathgate, R. & Summers, R. J., 2007, In : British Journal of Pharmacology. 150, 6, p. 677 - 691 15 p.

Research output: Contribution to journalArticleResearchpeer-review

Relaxin receptors - new drug targets for multiple disease states

van der Westhuizen, E. T., Summers, R. J., Halls, M. L., Bathgate, R. & Sexton, P., 2007, In : Current Drug Targets. 8, 1, p. 91 - 104 14 p.

Research output: Contribution to journalArticleResearchpeer-review

The relaxin family peptide receptor 3 activates extracellular signal-regulated kinase 1/2 through a protein kinase C-dependent mechanism

van der Westhuizen, E. T., Werry, T. D., Sexton, P. & Summers, R. J., 2007, In : Molecular Pharmacology. 71, 6, p. 1618 - 1629 12 p.

Research output: Contribution to journalArticleResearchpeer-review

2005

Responses of GPCR135 to human gene 3 (H3) relaxin in CHO-K1 cells determined by microphysiometry

van der Westhuizen, E. T., Sexton, P. M., Bathgate, R. A. D. & Summers, R. J., 2005, Relaxin and Related Peptides: Fourth International Conference. Sherwood, O. D., Fields, P. A. & Steinetz, B. G. (eds.). New York USA: New York Academy of Sciences, Vol. 1041. p. 332 - 337 6 p.

Research output: Chapter in Book/Report/Conference proceedingConference PaperResearchpeer-review

2002

FSH-regulated gene expression profiles in ovarian tumours and normal ovaries

Chu, S., Rushdi, S., Zumpe, E. T., Mamers, P., Healy, D., Jobling, T., Burger, H. & Fuller, P. J., 2002, In : Molecular Human Reproduction. 8, 5, p. 426 - 433 8 p.

Research output: Contribution to journalArticleResearchpeer-review

Inhibin-Activin Receptor Subunit Gene Expression in Ovarian Tumors

Fuller, P. J., Zumpe, E. T., Chu, S., Mamers, P. & Burger, H., 2002, In : Journal of Clinical Endocrinology and Metabolism. 87, p. 1395 - 1401 7 p.

Research output: Contribution to journalArticleResearchpeer-review

2000

Amylin receptor phenotypes derived from human calcitonin receptor/RAMP coexpression exhibit pharmacological differences dependent on receptor isoform and host cell environment.

Tilakaratne, N., Christopoulos, G., Zumpe, E. T., Foord, S. M. & Sexton, P. M., Jul 2000, In : Journal of Pharmacology and Experimental Therapeutics. 294, 1, p. 61-72 12 p.

Research output: Contribution to journalArticleResearchpeer-review

Multiple ramp domains are required for generation of amylin receptor phenotype from the calcitonin receptor gene product.

Zumpe, E. T., Tilakaratne, N., Fraser, NJ., Christopoulos, G., Foord, S. M. & Sexton, P., 7 Jan 2000, In : Biochemical and Biophysical Research Communications. 267, 1, p. 368-372

Research output: Contribution to journalArticleResearchpeer-review