Roger Summers – Research Output

2019

Drug-receptor kinetics and sigma-1 receptor affinity differentiate clinically evaluated histamine H₃ receptor antagonists

Riddy, D. M., Cook, A. E., Shackleford, D. M., Pierce, T. L., Mocaer, E., Mannoury la Cour, C., Sors, A., Charman, W. N., Summers, R. J., Sexton, P. M., Christopoulos, A. & Langmead, C. J., 1 Jan 2019, In : Neuropharmacology. 144, p. 244-255 12 p.

Research output: Contribution to journal › Article › Research › peer-review

Open Access

File

2018

Comparative genotypic and phenotypic analysis of human peripheral blood monocytes and surrogate monocyte-like cell lines commonly used in metabolic disease research

Riddy, D. M., Goy, E., Delerive, P., Summers, R. J. & Langmead, C. J., 1 May 2018, In : PLoS ONE. 13, 5, 19 p., e0197177.

Research output: Contribution to journal › Article › Research › peer-review

Open Access

File

INSL5 activates multiple signalling pathways and regulates GLP-1 secretion in NCI-H716 cells

Ang, S. Y., Evans, B. A., Poole, D. P., Bron, R., DiCello, J. J., Bathgate, R. A. D., Kocan, M., Hutchinson, D. S. & Summers, R. J., 1 Apr 2018, In : Journal of Molecular Endocrinology. 60, 3, p. 213-224 12 p.

Research output: Contribution to journal › Article › Research › peer-review

Open Access

File

Rosiglitazone and a β₃-adrenoceptor agonist are both required for functional browning of white adipocytes in culture

Merlin, J., Sato, M., Chia, L. Y., Fahey, R., Pakzad, M., Nowell, C. J., Summers, R. J., Bengtsson, T., Evans, B. A. & Hutchinson, D. S., 30 May 2018, In : Frontiers in Endocrinology. 9, MAY, 17 p., 249.

Research output: Contribution to journal › Article › Research › peer-review

Open Access

File

α_1A-Adrenoceptors activate mTOR signalling and glucose uptake in cardiomyocytes

Sato, M., Evans, B. A., Sandström, A. L., Chia, L. Y., Mukaida, S., Thai, B. S., Nguyen, A., Lim, L., Tan, C. Y. R., Baltos, J. A., White, P. J., May, L. T., Hutchinson, D. S., Summers, R. J. & Bengtsson, T., 1 Feb 2018, In : Biochemical Pharmacology. 148, p. 27-40 14 p.

Research output: Contribution to journal › Article › Research › peer-review

Open Access

File

2017

Factors influencing biased agonism in recombinant cells expressing the human α_1A-adrenoceptor

da Silva Junior, E. D., Sato, M., Merlin, J., Broxton, N., Hutchinson, D. S., Ventura, S., Evans, B. A. & Summers, R. J., 1 Jul 2017, In : British Journal of Pharmacology. 174, 14, p. 2318-2333 16 p.

Research output: Contribution to journal › Article › Research › peer-review

Open Access

File

High throughput, quantitative analysis of human osteoclast differentiation and activity

Diepenhorst, N., Nowell, C., Rueda, P., Henriksen, K., Pierce, T., Cook, A., Pastoureau, P., Sabatini, M., Charman, W., Christopoulos, A., Summers, R., Sexton, P. & Langmead, C., 15 Feb 2017, In : Analytical Biochemistry. 519, p. 51-56 6 p.

Research output: Contribution to journal › Article › Research › peer-review

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 journal › Article › Research › peer-review

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 journal › Article › Research › peer-review

Open Access

File

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 journal › Article › Research › peer-review

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 : Journal of Biological Chemistry. 292, 36, p. 15143-15158 16 p.

Research output: Contribution to journal › Article › Research › peer-review

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 journal › Article › Research › peer-review

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 journal › Article › Research › peer-review

Open Access

File

2016

A single-chain derivative of the relaxin hormone is a functionally selective agonist of the G protein-coupled receptor, RXFP1

Hossain, M. A., Kocan, M., Yao, S. T., Royce, S. G., Nair, V. B., Siwek, C., Patil, N. A., Harrison, I. P., Rosengren, K. J., Selemidis, S., Summers, R. J., Wade, J. D., Bathgate, R. A. D. & Samuel, C. S., 2016, In : Chemical Science. 7, 6, p. 3805-3819 15 p.

Research output: Contribution to journal › Article › Research › peer-review

Open Access

Engineering of a novel simplified human insulin-like peptide 5 agonist

Patil, N. A., Hughes, R. A., Rosengren, K. J., Kocan, M., Ang, S. Y., Tailhades, J., Separovic, F., Summers, R. J., Grosse, J., Wade, J., Bathgate, R. A. D. & Hossain, M. A., 10 Mar 2016, In : Journal of Medicinal Chemistry. 59, 5, p. 2118-2125 8 p.

Research output: Contribution to journal › Article › Research › peer-review

Enhanced serelaxin signalling in co-cultures of human primary endothelial and smooth muscle cells

Sarwar, M., Samuel, C. S., Bathgate, R., Stewart, D. R. & Summers, R. J., 2016, In : British Journal of Pharmacology. 173, 3, p. 484 - 496 13 p.

Research output: Contribution to journal › Article › Research › peer-review

Murine GPRC6A mediates cellular responses to L-amino acids, but not osteocalcin variants

Rueda, P., Harley, E., Lu, Y., Stewart, G. D., Fabb, S., Diepenhorst, N., Cremers, B., Rouillon, M-H., Wehrle, I., Geant, A., Lamarche, G., Leach, K., Charman, W. N., Christopoulos, A., Summers, R. J., Sexton, P. M. & Langmead, C. J., 1 Jan 2016, In : PLoS ONE. 11, 1, p. 1-19 19 p., e0146846.

Research output: Contribution to journal › Article › Research › peer-review

Open Access

Orthosteric, allosteric and biased signalling at the relaxin-3 receptor RXFP3

Kocan, M., Ang, S. Y. & Summers, R. J., 2016, In : Neurochemical Research. 41, 3, p. 610-619 10 p.

Research output: Contribution to journal › Article › Research › peer-review

The C-terminus of the B-chain of human insulin-like peptide 5 is critical for cognate RXFP4 receptor activity

Patil, N. A., Bathgate, R. A. D., Kocan, M., Ang, S. Y., Tailhades, J., Separovic, F., Summers, R., Grosse, J., Hughes, R. A., Wade, J. D. & Hossain, M. A., 1 Apr 2016, In : Amino Acids. 48, 4, p. 987-992 6 p.

Research output: Contribution to journal › Article › Research › peer-review

2015

International union of basic and clinical pharmacology. XCV. Recent advances in the understanding of the pharmacology and biological roles of relaxin family peptide receptors 1-4, the receptors for relaxin family peptides

Halls, M. L., Bathgate, R. A. D., Sutton, S. W., Dschietzig, T. B. & Summers, R. J., 2015, In : Pharmacological Reviews. 67, 2, p. 389-440 52 p.

Research output: Contribution to journal › Article › Research › peer-review

Label-free kinetics: exploiting functional hemi-equilibrium to derive rate constants for muscarinic receptor antagonists

Riddy, D. M., Valant, C., Rueda, P., Charman, W. N., Sexton, P. M., Summers, R. J., Christopoulos, A. & Langmead, C. J., 2015, In : Molecular Pharmacology. 88, 4, p. 779-790 12 p.

Research output: Contribution to journal › Article › Research › peer-review

Serelaxin-mediated signal transduction in human vascular cells: bell-shaped concentration-response curves reflect differential coupling to G proteins

Sarwar, M., Samuel, C. S., Bathgate, R. A., Stewart, D. R. & Summers, R. J., 2015, In : British Journal of Pharmacology. 172, 4, p. 1005-1019 15 p.

Research output: Contribution to journal › Article › Research › peer-review

2014

Improving type 2 diabetes through a distinct adrenergic signaling pathway involving mTORC2 that mediates glucose uptake in skeletal muscle

Sato, M., Dehvari, N., Oberg, A., Dallner, O. S., Sandstrom, A. L., Olsen, J. M., Csikasz, R. I., Summers, R. J., Hutchinson, D. S. & Bengtsson, T., 2014, In : Diabetes. 63, 12, p. 4115 - 4129 15 p.

Research output: Contribution to journal › Article › Research › peer-review

Relaxin requires the angiotensin II type 2 receptor to abrogate renal interstitial fibrosis

Chow, B. SM., Kocan, M., Bosnyak, S., Sarwar, M., Wigg, B., Jones, E. S., Widdop, R. E., Summers, R. J., Bathgate, R. A. D., Hewitson, T. D. & Samuel, C. S., 2014, In : Kidney International. 86, 1, p. 75 - 85 11 p.

Research output: Contribution to journal › Article › Research › peer-review

Signalling profiles of H3 relaxin, H2 relaxin and R3(B?23-27)R/I5 acting at the relaxin family peptide receptor 3 (RXFP3)

Kocan, M., Sarwar, M., Hossain, M. A., Wade, J. D. & Summers, R. J., 2014, In : British Journal of Pharmacology. 171, 11, p. 2827 - 2841 15 p.

Research output: Contribution to journal › Article › Research › peer-review

2013

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 journal › Article › Research › peer-review

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 journal › Article › Research › peer-review

Open Access

File

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 journal › Article › Research › peer-review

2012

Beta(2)-adrenoceptors increase translocation of GLUT4 via GPCR kinase sites in the receptor C-terminal tail

Dehvari, N., Hutchinson, D., Nevzorova, J., Dallner, O., Sato, M., Kocan, M., Merlin, J., Evans, B., Summers, R. & Bengtsson, T., 2012, In : British Journal of Pharmacology. 165, 5, p. 1442 - 1456 15 p.

Research output: Contribution to journal › Article › Research › peer-review

Interaction with caveolin-1 modulates G protein coupling of the mouse beta3-adrenoceptor

Sato, M., Hutchinson, D. S., Halls, M. L., Furness, S. G. B., Bengtsson, T., Evans, B. A. & Summers, R. J., 2012, In : Journal of Biological Chemistry. 287, 24, p. 20674 - 20688 15 p.

Research output: Contribution to journal › Article › Research › peer-review

Open Access

File

2011

2010

Allosteric ligands of the glucagon-like peptide 1 receptor (GLP-1R) differentially modulate endogenous and exogenous peptide responses in a pathway-selective manner: Implications for drug screening

Koole, C., Wootten, D., Simms, J., Valant, C., Sridhar, R., Woodman, O., Miller, L. J., Summers, R., Christopoulos, A. & Sexton, P. M., 2010, In : Molecular Pharmacology. 78, 3, p. 456 - 465 10 p.

Research output: Contribution to journal › Article › Research › peer-review

Noradrenaline release in the locus coeruleus modulates memory formation and consolidation; roles for alpha- and beta-adrenergic receptors

Gibbs, M. E., Hutchinson, D. S. & Summers, R. J., 2010, In : Neuroscience. 170, 4, p. 1209 - 1222 14 p.

Research output: Contribution to journal › Article › Research › peer-review

The M3-muscarinic acetylcholine receptor stimulates glucose uptake in L6 skeletal muscle cells by a CaMKK-AMPK-dependent mechanism

Merlin, J., Evans, B. A., Csikasz, R. I., Bengtsson, T., Summers, R. J. & Hutchinson, D. S., 2010, In : Cellular Signalling. 22, 7, p. 1104 - 1113 10 p.

Research output: Contribution to journal › Article › Research › peer-review

Tissue functions mediated by beta3-adrenoceptors-Findings and challenges

Michel, M., Ochodnicky, P. & Summers, R., 2010, In : Naunyn-Schmiedeberg's Archives of Pharmacology. 382, 2, p. 103 - 108 6 p.

Research output: Contribution to journal › Article › Research › peer-review

2009

Addition of a carboxy-terminal green fluorescent protein does not alter the binding and signaling properties of relaxin family peptide receptor 3

van der Westhuizen, E. T., Wade, J. D., Sexton, P. M. & Summers, R. J., 2009, In : Annals of the New York Academy of Sciences. 1160, p. 105 - 107 3 p.

Research output: Contribution to journal › Article › Research › peer-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 journal › Article › Research › peer-review

Relaxin inhibits renal myofibroblast differentiation via RXFP1, the nitric oxide pathway, and Smad2

Mookerjee, I., Hewitson, T. D., Halls, M. L., Summers, R. J., Mathai, M. L., Bathgate, R., Tregear, G. W. & Samuel, C. S., 2009, In : FASEB Journal. 23, p. 1219 - 1229 10 p.

Research output: Contribution to journal › Article › Research › peer-review