Search Results - "Bernier, Sylvie"
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sGC stimulator praliciguat suppresses stellate cell fibrotic transformation and inhibits fibrosis and inflammation in models of NASH
Published in Proceedings of the National Academy of Sciences - PNAS (28-05-2019)“…Endothelial dysfunction and reduced nitric oxide (NO) signaling are a key element of the pathophysiology of nonalcoholic steatohepatitis (NASH). Stimulators of…”
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Discovery of stimulator binding to a conserved pocket in the heme domain of soluble guanylyl cyclase
Published in The Journal of biological chemistry (02-02-2018)“…Soluble guanylyl cyclase (sGC) is the receptor for nitric oxide and a highly sought-after therapeutic target for the management of cardiovascular diseases. New…”
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3
Rapid discovery and evolution of nanosensors containing fluorogenic amino acids
Published in Nature communications (05-09-2024)“…Binding-activated optical sensors are powerful tools for imaging, diagnostics, and biomolecular sensing. However, biosensor discovery is slow and requires…”
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The CNS-penetrant soluble guanylate cyclase stimulator CYR119 attenuates markers of inflammation in the central nervous system
Published in Journal of neuroinflammation (18-09-2021)“…Inflammation in the central nervous system (CNS) is observed in many neurological disorders. Nitric oxide-soluble guanylate cyclase-cyclic guanosine…”
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Olinciguat, a stimulator of soluble guanylyl cyclase, attenuates inflammation, vaso‐occlusion and nephropathy in mouse models of sickle cell disease
Published in British journal of pharmacology (01-09-2021)“…Background and Purpose Reduced bioavailability of NO, a hallmark of sickle cell disease (SCD), contributes to intravascular inflammation, vasoconstriction,…”
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Pharmacological Characterization of IW-1973, a Novel Soluble Guanylate Cyclase Stimulator with Extensive Tissue Distribution, Antihypertensive, Anti-Inflammatory, and Antifibrotic Effects in Preclinical Models of Disease
Published in The Journal of pharmacology and experimental therapeutics (01-06-2018)“…Soluble guanylate cyclase (sGC), a key signal-transduction enzyme, increases the conversion of guanosine-5'-triphosphate to cGMP upon binding of nitric oxide…”
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The CNS-Penetrant Soluble Guanylate Cyclase Stimulator CY6463 Reveals its Therapeutic Potential in Neurodegenerative Diseases
Published in Frontiers in pharmacology (24-05-2021)“…Effective treatments for neurodegenerative diseases remain elusive and are critically needed since the burden of these diseases increases across an aging…”
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The Soluble Guanylate Cyclase Stimulator IWP-953 Increases Conventional Outflow Facility in Mouse Eyes
Published in Investigative ophthalmology & visual science (01-03-2016)“…The nitric oxide (NO)-cyclic guanosine-3',5'-monophosphate (cGMP) pathway regulates aqueous humor outflow and therefore, intraocular pressure. We investigated…”
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Olinciguat, an Oral sGC Stimulator, Exhibits Diverse Pharmacology Across Preclinical Models of Cardiovascular, Metabolic, Renal, and Inflammatory Disease
Published in Frontiers in pharmacology (08-04-2020)“…Nitric oxide (NO)-soluble guanylate cyclase (sGC)-cyclic 3',5' GMP (cGMP) signaling plays a central role in regulation of diverse processes including smooth…”
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Discovery of CYR715: A novel carboxylic acid-containing soluble guanylate cyclase stimulator
Published in Bioorganic & medicinal chemistry letters (15-05-2021)“…[Display omitted] Soluble guanylate cyclase (sGC) is a clinically validated therapeutic target in the treatment of pulmonary hypertension. Modulators of sGC…”
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Discovery and Characterization of a Potent Interleukin-6 Binding Peptide with Neutralizing Activity In Vivo
Published in PloS one (10-11-2015)“…Interleukin-6 (IL-6) is an important member of the cytokine superfamily, exerting pleiotropic actions on many physiological processes. Over-production of IL-6…”
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Discovery of Clinical Candidate GSK1842799 As a Selective S1P1 Receptor Agonist (Prodrug) for Multiple Sclerosis
Published in ACS medicinal chemistry letters (10-10-2013)“…To develop effective oral treatment for multiple sclerosis (MS), we discovered a series of alkyl-substituted biaryl amino alcohols as selective S1P1…”
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A Methionine Aminopeptidase-2 Inhibitor, PPI-2458, for the Treatment of Rheumatoid Arthritis
Published in Proceedings of the National Academy of Sciences - PNAS (20-07-2004)“…The hallmark of rheumatoid arthritis (RA) is the progressive destruction of articular joints, characterized by invasive synovial hyperplasia and pathological…”
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Modulation of Pro-inflammatory Gene Expression by Nuclear Lysophosphatidic Acid Receptor Type-1
Published in The Journal of biological chemistry (03-10-2003)“…Lysophosphatidic acid (LPA) is a bioactive molecule involved in inflammation, immunity, wound healing, and neoplasia. Its pleiotropic actions arise presumably…”
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Exploring amino acids derivatives as potent, selective, and direct agonists of sphingosine-1-phosphate receptor subtype-1
Published in Bioorganic & medicinal chemistry letters (15-01-2013)“…In the quest to discover a potent and selective class of direct agonists to the sphingosine-1-phosphate receptor, we explored the carboxylate functional group…”
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Gastrointestinal pain: Unraveling a novel endogenous pathway through uroguanylin/guanylate cyclase-C/cGMP activation
Published in Pain (Amsterdam) (01-09-2013)“…Uroguanylin activation of the guanylate cyclase-C/cyclic guanosine monophosphate pathway elicits analgesic effects in animal models of colonic…”
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Methionine aminopeptidases type I and type II are essential to control cell proliferation
Published in Journal of cellular biochemistry (15-08-2005)“…The dependence of cell growth on methionine aminopeptidase (MetAP) function in bacteria and yeast is firmly established. Here we report experimental evidence…”
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Regulation of eNOS Expression in Brain Endothelial Cells by Perinuclear EP3 Receptors
Published in Circulation research (05-04-2002)“…We reported upregulation of endothelial nitric oxide synthase (eNOS) by PGE2 in tissues and presence of perinuclear PGE2 receptors (EP). We presently studied…”
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Proinflammatory Gene Induction by Platelet-Activating Factor Mediated Via Its Cognate Nuclear Receptor
Published in The Journal of immunology (1950) (01-12-2002)“…It has been postulated that intracellular binding sites for platelet-activating factor (PAF) contribute to proinflammatory responses to PAF. Isolated nuclei…”
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Altered vascular function in fetal programming of hypertension
Published in Stroke (1970) (01-12-2002)“…Reduced endothelium-dependent vasorelaxation partly due to loss of nitric oxide (NO) bioavailability occurs in most cases of chronic hypertension. Intrauterine…”
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