Search Results - "SUMMERS, ROGER J."

G Protein-Coupled Receptors Targeting Insulin Resistance, Obesity, and Type 2 Diabetes Mellitus by Riddy, Darren M, Delerive, Philippe, Summers, Roger J, Sexton, Patrick M, Langmead, Christopher J

“…G protein-coupled receptors (GPCRs) continue to be important discovery targets for the treatment of type 2 diabetes mellitus (T2DM). Many GPCRs are directly…”
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The actions of relaxin on the human cardiovascular system by Sarwar, Mohsin, Du, Xiao‐Jun, Dschietzig, Thomas B, Summers, Roger J

“…The insulin‐like peptide relaxin, originally identified as a hormone of pregnancy, is now known to exert a range of pleiotropic effects including vasodilatory,…”
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Comparative genotypic and phenotypic analysis of human peripheral blood monocytes and surrogate monocyte-like cell lines commonly used in metabolic disease research by Riddy, Darren M, Goy, Emily, Delerive, Philippe, Summers, Roger J, Sexton, Patrick M, Langmead, Christopher J

“…Monocyte-like cell lines (MCLCs), including THP-1, HL-60 and U-937 cells, are used routinely as surrogates for isolated human peripheral blood mononuclear…”
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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 by Halls, Michelle L, Bathgate, Ross A D, Sutton, Steve W, Dschietzig, Thomas B, Summers, Roger J

“…Relaxin, insulin-like peptide 3 (INSL3), relaxin-3, and INSL5 are the cognate ligands for the relaxin family peptide (RXFP) receptors 1-4, respectively. RXFP1…”
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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 by Koole, Cassandra, Wootten, Denise, Simms, John, Valant, Celine, Sridhar, Rohan, Woodman, Owen L, Miller, Laurence J, Summers, Roger J, Christopoulos, Arthur, Sexton, Patrick M

“…The glucagon-like peptide-1 (GLP-1) receptor is a key regulator of insulin secretion and a major therapeutic target for treatment of diabetes. However, GLP-1…”
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Adrenoceptors—New roles for old players by Michel, Martin C., Bond, Richard A., Summers, Roger J.

“…Linked Articles This article is part of a themed section on Adrenoceptors—New Roles for Old Players. To view the other articles in this section visit…”
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Relaxin requires the angiotensin II type 2 receptor to abrogate renal interstitial fibrosis by Chow, Bryna S Man, Kocan, Martina, Bosnyak, Sanja, Sarwar, Mohsin, Wigg, Belinda, Jones, Emma S, Widdop, Robert E, Summers, Roger J, Bathgate, Ross A D, Hewitson, Tim D, Samuel, Chrishan S

“…Fibrosis is a hallmark of chronic kidney disease, for which there is currently no effective cure. The hormone relaxin is emerging as an effective antifibrotic…”
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Divergent effects of strontium and calcium‐sensing receptor positive allosteric modulators (calcimimetics) on human osteoclast activity by Diepenhorst, Natalie A, Leach, Katie, Keller, Andrew N, Rueda, Patricia, Cook, Anna E, Pierce, Tracie L, Nowell, Cameron, Pastoureau, Philippe, Sabatini, Massimo, Summers, Roger J, Charman, William N, Sexton, Patrick M, Christopoulos, Arthur, Langmead, Christopher J

“…Background and Purpose Strontium ranelate, a drug approved and until recently used for the treatment of osteoporosis, mediates its effects on bone at least in…”
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ML290 is a biased allosteric agonist at the relaxin receptor RXFP1 by Kocan, Martina, Sarwar, Mohsin, Ang, Sheng Y., Xiao, Jingbo, Marugan, Juan J., Hossain, Mohammed A., Wang, Chao, Hutchinson, Dana S., Samuel, Chrishan S., Agoulnik, Alexander I., Bathgate, Ross A. D., Summers, Roger J.

“…Activation of the relaxin receptor RXFP1 has been associated with improved survival in acute heart failure. ML290 is a small molecule RXFP1 agonist with simple…”
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Factors influencing biased agonism in recombinant cells expressing the human α1A‐adrenoceptor by Silva Junior, Edilson Dantas, Sato, Masaaki, Merlin, Jon, Broxton, Natalie, Hutchinson, Dana S, Ventura, Sabatino, Evans, Bronwyn A, Summers, Roger J

“…Background and Purpose Agonists acting at GPCRs promote biased signalling via Gα or Gβγ subunits, GPCR kinases and β‐arrestins. Since the demonstration of…”
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International Union of Pharmacology LVII: Recommendations for the Nomenclature of Receptors for Relaxin Family Peptides by Bathgate, Ross A, Ivell, Richard, Sanborn, Barbara M, Sherwood, O David, Summers, Roger J

“…Although the hormone relaxin was discovered 80 years ago, only in the past 5 years have the receptors for relaxin and three other receptors that respond to…”
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A single-chain derivative of the relaxin hormone is a functionally selective agonist of the G protein-coupled receptor, RXFP1 by Hossain, Mohammed Akhter, Kocan, Martina, Yao, Song T, Royce, Simon G, Nair, Vinojini B, Siwek, Christopher, Patil, Nitin A, Harrison, Ian P, Rosengren, K Johan, Selemidis, Stavros, Summers, Roger J, Wade, John D, Bathgate, Ross A D, Samuel, Chrishan S

“…Human gene-2 relaxin (H2 relaxin) is a pleiotropic hormone with powerful vasodilatory and anti-fibrotic properties which has led to its clinical evaluation and…”
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Editorial: Recent Advances in G Protein-Coupled Receptor Signalling: Impact of Intracellular Location, Environment and Biased Agonism by Halls, Michelle L., Davenport, Anthony P., Summers, Roger J.

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Cardiovascular effects of relaxin: from basic science to clinical therapy by Du, Xiao-Jun, Bathgate, Ross A. D, Samuel, Chrishan S, Dart, Anthony M, Summers, Roger J

“…Over the past two decades, there has been rapid progress in our understanding of the pleiotropic actions of relaxin in the cardiovascular system. In this…”
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Signal transduction pathways activated by insulin‐like peptide 5 at the relaxin family peptide RXFP4 receptor by Ang, Sheng Y, Hutchinson, Dana S, Patil, Nitin, Evans, Bronwyn A, Bathgate, Ross A D, Halls, Michelle L, Hossain, Mohammed A, Summers, Roger J, Kocan, Martina

“…Background and Purpose Insulin‐like peptide 5 (INSL5) is a two‐chain, three‐disulfide‐bonded peptide of the insulin/relaxin superfamily, uniquely expressed in…”
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Murine GPRC6A Mediates Cellular Responses to L-Amino Acids, but Not Osteocalcin Variants by Rueda, Patricia, Harley, Elizabeth, Lu, Yao, Stewart, Gregory D, Fabb, Stewart, Diepenhorst, Natalie, Cremers, Béatrice, Rouillon, Marie-Hélène, Wehrle, Isabelle, Geant, Anne, Lamarche, Gwladys, Leach, Katie, Charman, William N, Christopoulos, Arthur, Summers, Roger J, Sexton, Patrick M, Langmead, Christopher J

“…Phenotyping of Gprc6a KO mice has shown that this promiscuous class C G protein coupled receptor is variously involved in regulation of metabolism,…”
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Modulation of the glucagon-like peptide-1 receptor signaling by naturally occurring and synthetic flavonoids by Wootten, Denise, Simms, John, Koole, Cassandra, Woodman, Owen L, Summers, Roger J, Christopoulos, Arthur, Sexton, Patrick M

“…The glucagon-like peptide 1 receptor (GLP-1R) is a promising target for the treatment of type II diabetes mellitus because of its role in metabolic…”
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Regulation of AMP-activated protein kinase activity by G-protein coupled receptors: potential utility in treatment of diabetes and heart disease by Hutchinson, Dana S, Summers, Roger J, Bengtsson, Tore

“…G-protein coupled receptors (GPCRs) comprise the largest and most diverse family of membrane receptors in the human genome, relaying information from a vast…”
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Rosiglitazone and a β3-Adrenoceptor Agonist Are Both Required for Functional Browning of White Adipocytes in Culture by Merlin, Jon, Sato, Masaaki, Chia, Ling Yeong, Fahey, Richard, Pakzad, Mohsen, Nowell, Cameron J., Summers, Roger J., Bengtsson, Tore, Evans, Bronwyn A., Hutchinson, Dana S.

“…The recruitment of brite (or beige) adipocytes has been advocated as a means to combat obesity, due to their ability to phenotypically resemble brown…”
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Role of G protein‐coupled receptor kinases (GRKs) in β2‐adrenoceptor‐mediated glucose uptake by Ham, Seungmin, Mukaida, Saori, Sato, Masaaki, Keov, Peter, Bengtsson, Tore, Furness, Sebastian, Holliday, Nicholas D., Evans, Bronwyn A., Summers, Roger J., Hutchinson, Dana S.

“…Truncation of the C‐terminal tail of the β2‐AR, transfection of βARKct or over‐expression of a kinase‐dead GRK mutant reduces isoprenaline‐stimulated glucose…”
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