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2019

AT1R-AT2R-RXFP1 functional crosstalk in myofibroblasts: Impact on the therapeutic targeting of renal and cardiac fibrosis

Chow, B. S. M., Kocan, M., Shen, M., Wang, Y., Han, L., Chew, J. Y., Wang, C., Bosnyak, S., Mirabito-Colafella, K. M., Barsha, G., Wigg, B., Johnstone, E. K. M., Hossain, M. A., Pfleger, K. D. G., Denton, K. M., Widdop, R. E., Summers, R. J., Bathgate, R. A. D., Hewitson, T. D. & Samuel, C. S., 1 Jan 2019, In : Journal of the American Society of Nephrology. 30, 11, p. 2191-2207 17 p.

Research output: Contribution to journalArticleResearchpeer-review

3 Citations (Scopus)

BRL37344 stimulates GLUT4 translocation and glucose uptake in skeletal muscle via β 2 -adrenoceptors without causing classical receptor desensitization

Mukaida, S., Sato, M., Öberg, A. I., Dehvari, N., Olsen, J. M., Kocan, M., Halls, M. L., Merlin, J., Sandström, A. L., Csikasz, R. I., Evans, B. A., Summers, R. J., Hutchinson, D. S. & Bengtsson, T., 1 May 2019, In : American Journal of Physiology - Regulatory Integrative and Comparative Physiology. 316, 5, p. R666-R677 12 p.

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2 Citations (Scopus)

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.

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6 Citations (Scopus)

The concise guide to Pharmacology 2019/20: G protein-coupled receptors

Alexander, S. P. H., Christopoulos, A., Davenport, A. P., Kelly, E., Mathie, A., Peters, J. A., Veale, E. L., Armstrong, J. F., Faccenda, E., Harding, S. D., Pawson, A. J., Sharman, J. L., Southan, C., Davies, J. A. & CGTP Collaborators, 1 Dec 2019, In : British Journal of Pharmacology. 176, S1, p. S21-S141 120 p.

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95 Citations (Scopus)
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.

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5 Citations (Scopus)

Divergent effects of strontium and calcium-sensing receptor positive allosteric modulators (calcimimetics) on human osteoclast activity

Diepenhorst, N. A., Leach, K., Keller, A. N., Rueda, P., Cook, A. E., Pierce, T. L., Nowell, C., Pastoureau, P., Sabatini, M., Summers, R. J., Charman, W. N., Sexton, P. M., Christopoulos, A. & Langmead, C. J., 1 Nov 2018, In : British Journal of Pharmacology. 175, 21, p. 4095-4108 14 p.

Research output: Contribution to journalArticleResearchpeer-review

6 Citations (Scopus)

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 journalArticleResearchpeer-review

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2 Citations (Scopus)

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.

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9 Citations (Scopus)

The PPARγ agonist rosiglitazone promotes the induction of brite adipocytes, increasing β-adrenoceptor-mediated mitochondrial function and glucose uptake

Merlin, J., Sato, M., Nowell, C., Pakzad, M., Fahey, R., Gao, J., Dehvari, N., Summers, R. J., Bengtsson, T., Evans, B. A. & Hutchinson, D. S., 1 Jan 2018, In : Cellular Signalling. 42, p. 54-66 13 p.

Research output: Contribution to journalArticleResearchpeer-review

18 Citations (Scopus)

α1A-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 journalArticleResearchpeer-review

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6 Citations (Scopus)
2017

Factors influencing biased agonism in recombinant cells expressing the human α1A-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 journalArticleResearchpeer-review

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8 Citations (Scopus)

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 journalArticleResearchpeer-review

2 Citations (Scopus)

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 journalArticleResearchpeer-review

11 Citations (Scopus)

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 journalArticleResearchpeer-review

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17 Citations (Scopus)

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 journalArticleResearchpeer-review

14 Citations (Scopus)

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

Research output: Contribution to journalArticleResearchpeer-review

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3 Citations (Scopus)

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 journalArticleResearchpeer-review

4 Citations (Scopus)

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 journalArticleResearchpeer-review

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155 Citations (Scopus)
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 journalArticleResearchpeer-review

Open Access
33 Citations (Scopus)

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 journalArticleResearchpeer-review

14 Citations (Scopus)

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 journalArticleResearchpeer-review

17 Citations (Scopus)

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 journalArticleResearchpeer-review

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25 Citations (Scopus)

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 journalArticleResearchpeer-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 journalArticleResearchpeer-review

8 Citations (Scopus)
2015
73 Citations (Scopus)

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 journalArticleResearchpeer-review

41 Citations (Scopus)
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 journalArticleResearchpeer-review

50 Citations (Scopus)

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 journalArticleResearchpeer-review

67 Citations (Scopus)

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 journalArticleResearchpeer-review

15 Citations (Scopus)
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 journalArticleResearchpeer-review

1 Citation (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

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5 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

269 Citations (Scopus)
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 journalArticleResearchpeer-review

18 Citations (Scopus)

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 : The Journal of Biological Chemistry. 287, 24, p. 20674 - 20688 15 p.

Research output: Contribution to journalArticleResearchpeer-review

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19 Citations (Scopus)
2011

alpha{2}-Adrenoceptors activate noradrenaline-mediated glycogen turnover in chick astrocytes

Hutchinson, D. S., Catus, S. L., Merlin, J., Summers, R. J. & Gibbs, M. E., 2011, In : Journal of Neurochemistry. 117, 5, p. 915 - 926 12 p.

Research output: Contribution to journalArticleResearchpeer-review

20 Citations (Scopus)

Evolution of beta-blockers: from anti-anginal drugs to ligand-directed signalling

Baker, J. G., Hill, S. J. & Summers, R. J., 2011, In : Trends in Pharmacological Sciences. 32, 4, p. 227 - 234 8 p.

Research output: Contribution to journalArticleResearchpeer-review

73 Citations (Scopus)

Modulation of the glucagon-like peptide-1 receptor signaling by naturally occurring and synthetic flavonoids

Wootten, D., Simms, J., Koole, C., Woodman, O., Summers, R., Christopoulos, A. & Sexton, P., 2011, In : Journal of Pharmacology and Experimental Therapeutics. 336, 2, p. 540 - 550 11 p.

Research output: Contribution to journalArticleResearchpeer-review

48 Citations (Scopus)

Quantification of functional selectivity at the human {alpha}1A-adrenoceptor

Evans, B. A., Broxton, N., Merlin, J., Sato, M., Hutchinson, D. S., Christopoulos, A. & Summers, R. J., 2011, In : Molecular Pharmacology. 79, 2, p. 298 - 307 10 p.

Research output: Contribution to journalArticleResearchpeer-review

51 Citations (Scopus)

Role of beta-adrenoceptors in glucose uptake in astrocytes using beta-adrenoceptor knockout mice

Catus, S. L., Gibbs, M. E., Sato, M., Summers, R. J. & Hutchinson, D. S., 2011, In : British Journal of Pharmacology. 162, 8, p. 1700 - 1715 16 p.

Research output: Contribution to journalArticleResearchpeer-review

33 Citations (Scopus)
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 journalArticleResearchpeer-review

136 Citations (Scopus)

Cardiovascular effects of relaxin: from basic science to clinical therapy

Du, X-J., Bathgate, R. A. D., Samuel, C. S., Dart, A. M. & Summers, R. J., 2010, In : Nature Reviews Cardiology. 7, 1, p. 48 - 58 11 p.

Research output: Contribution to journalArticleResearchpeer-review

124 Citations (Scopus)

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

23 Citations (Scopus)

Ligand-directed signalling at beta-adrenoceptors

Evans, B., Sato, M., Sarwar, M., Hutchinson, D. & Summers, R., 2010, In : British Journal of Pharmacology. 159, 5, p. 1022 - 1038 17 p.

Research output: Contribution to journalArticleResearchpeer-review

110 Citations (Scopus)

Memory loss caused by beta-amyloid protein is rescued by a beta3-adrenoceptor agonist

Gibbs, M. E., Maksel, D. M., Gibbs, Z., Hou, X., Summers, R. J. & Small, D. H., 2010, In : Neurobiology of Aging. 31, p. 614 - 624 10 p.

Research output: Contribution to journalArticleResearchpeer-review

34 Citations (Scopus)

Molecular pharmacology of G protein-coupled receptors: Editorial

Summers, R., 2010, In : British Journal of Pharmacology. 159, 5, p. 983 - 985 3 p.

Research output: Contribution to journalArticleResearchpeer-review

3 Citations (Scopus)

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 journalArticleResearchpeer-review

56 Citations (Scopus)

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 journalArticleResearchpeer-review

27 Citations (Scopus)

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 journalArticleResearchpeer-review

26 Citations (Scopus)