Search Results - "De Los Frailes, Maite"
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Identification of novel isoform-selective inhibitors within class I histone deacetylases
Published in The Journal of pharmacology and experimental therapeutics (01-11-2003)“…Histone deacetylases (HDACs) represent an expanding family of protein modifying-enzymes that play important roles in cell proliferation, chromosome remodeling,…”
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Discovery of Substituted Maleimides as Liver X Receptor Agonists and Determination of a Ligand-Bound Crystal Structure
Published in Journal of medicinal chemistry (25-08-2005)“…Substituted 3-(phenylamino)-1H-pyrrole-2,5-diones were identified from a high throughput screen as inducers of human ATP binding cassette transporter A1…”
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Discovery of Novel Inhibitors of the Tautomerase Activity of Macrophage Migration Inhibitory Factor (MIF)
Published in Journal of biomolecular screening (01-06-2016)“…Macrophage migration inhibitory factor (MIF) is a proinflammatory cytokine associated with multiple diseases, including neurodegenerative disorders. With the…”
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Discovery of Enhancers of the Secretion of Leukemia Inhibitory Factor for the Treatment of Multiple Sclerosis
Published in Journal of biomolecular screening (01-06-2016)“…Multiple sclerosis (MS) is an autoimmune neurodegenerative disease that involves activation of T cells, microglia, and astrocytes. There is a clear unmet…”
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Screening technologies for G protein-coupled receptors: from HTS to uHTS
Published in Methods in molecular biology (Clifton, N.J.) (01-01-2009)“…The discovery of drugs for G protein-coupled receptors (GPCRs) has traditionally been very successful, even before the structural nature of these molecular…”
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Discovery of 3-Aryl-4-isoxazolecarboxamides as TGR5 Receptor Agonists
Published in Journal of medicinal chemistry (24-12-2009)“…A series of 3-aryl-4-isoxazolecarboxamides identified from a high-throughput screening campaign as novel, potent small molecule agonists of the human TGR5…”
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The identification of structurally novel, selective, orally bioavailable positive modulators of mGluR2
Published in Bioorganic & medicinal chemistry letters (15-01-2010)“…The optimisation of an HTS hit series ( 1) leading to the identification of structurally novel, selective, orally bioavailable mGluR2 positive modulators…”
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Potent achiral agonists of the ghrelin (growth hormone secretagogue) receptor. Part I: Lead identification
Published in Bioorganic & medicinal chemistry letters (01-12-2007)“…A series of indolines showing potent in vitro ghrelin receptor agonism and acceleration of gastric emptying in rats is described. High throughput screening…”
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