Search Results - "Todderud, Gordon"
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Discovery of the Selective CYP17A1 Lyase Inhibitor BMS-351 for the Treatment of Prostate Cancer
Published in ACS medicinal chemistry letters (14-01-2016)“…Efforts to identify a potent, reversible, nonsteroidal CYP17A1 lyase inhibitor with good selectivity over CYP17A1 hydroxylase and CYPs 11B1 and 21A2 for the…”
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BMS-190394, a selectin inhibitor, prevents rat cutaneous inflammatory reactions
Published in The Journal of pharmacology and experimental therapeutics (01-09-1997)“…Selectin binding is the first step in extravasation of leukocytes through the endothelium. Infiltration of leukocytes is a hallmark of an inflammatory…”
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Trends in Kinase Selectivity: Insights for Target Class-Focused Library Screening
Published in Journal of medicinal chemistry (13-01-2011)“…A kinome-wide selectivity screen of >20000 compounds with a rich representation of many structural classes has been completed. Analysis of the selectivity…”
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Multiple and Single Binding Modes of Fragment-Like Kinase Inhibitors Revealed by Molecular Modeling, Residue Type-Selective Protonation, and Nuclear Overhauser Effects
Published in Journal of medicinal chemistry (09-10-2008)“…Fragment-like inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK2) include 5-hydroxyisoquinoline (IC50 ∼ 85 μM). Modeling studies…”
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Synthesis and SAR of p38α MAP kinase inhibitors based on heterobicyclic scaffolds
Published in Bioorganic & medicinal chemistry letters (15-09-2007)“…The synthesis and structure–activity relationships (SAR) of p38α MAP kinase inhibitors based on heterobicyclic scaffolds are described. This effort led to the…”
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Stimulation of Phospholipase C-γ1 Membrane Association by Epidermal Growth Factor
Published in Science (American Association for the Advancement of Science) (20-07-1990)“…Epidermal growth factor (EGF) treatment of A-431 epidermoid carcinoma cells elicited a redistribution of phospholipase C-γ1 (PLC-γ1) from a predominantly…”
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Elevated Content of the Tyrosine Kinase Substrate Phospholipase C-γ1 in Primary Human Breast Carcinomas
Published in Proceedings of the National Academy of Sciences - PNAS (01-12-1991)“…Phospholipase C-γ1 (PLC-γ1) is a substrate for several receptor tyrosine kinases and its catalytic activity is increased by tyrosine phosphorylation. However,…”
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Synthesis and SAR of p38alpha MAP kinase inhibitors based on heterobicyclic scaffolds
Published in Bioorganic & medicinal chemistry letters (15-09-2007)“…The synthesis and structure-activity relationships (SAR) of p38alpha MAP kinase inhibitors based on heterobicyclic scaffolds are described. This effort led to…”
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De novo design, synthesis, and in vitro activity of LFA-1 antagonists based on a bicyclic[5.5]hydantoin scaffold
Published in Bioorganic & medicinal chemistry letters (15-02-2005)“…LFA-1 is a member of the β2-integrin family and is expressed on all leukocytes. This paper describes the de novo design, synthesis, and in vitro activity of…”
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Cytosolic [Ca2+] homeostasis and tyrosine phosphorylation of phospholipase Cγ2 in HL60 granulocytes
Published in The Journal of biological chemistry (15-02-1993)Get full text
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Novel mimics of sialyl Lewis X: design, synthesis and biological activity of a series of 2- and 3-malonate substituted galactoconjugates
Published in Bioorganic & medicinal chemistry (01-06-2001)“…A series of potent inhibitors of P-selectin as potential anti-inflammatory agents is reported. These compounds are derivatives of galactocerebrosides bearing a…”
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Novel mimics of sialyl Lewis X
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Isolation and Structure Determination of Sulfonoquinovosyl Dipalmitoyl Glyceride, a P-Selectin Receptor Inhibitor from the Alga Dictyochloris fragrans
Published in Journal of natural products (Washington, D.C.) (01-04-1997)“…Bioassay-guided fractionation of the marine alga Dictyochloris fragrans led to the isolation and identification of sulfonoquinovosyl dipalmitoyl glyceride (1)…”
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Sulfated Galactocerebrosides as Potential Antiinflammatory Agents
Published in Journal of medicinal chemistry (26-09-1997)“…Native sulfatides, as well as many sulfated glycolipids, have been shown to avidly bind to the selectin receptors. In vivo, native sulfatides significantly…”
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Phorbol Ester-Induced Upregulation of Polymorphonuclear Leukocyte P-Selectin Ligand Expression
Published in Cellular immunology (01-11-1995)“…Proinflammatory stimuli cause the vascular endothelium to express P-selectin that tethers leukocytes by binding surface glycoprotein carbohydrate. While the…”
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Stimulation of Phospholipase C-(gamma)1 Membrane Association by Epidermal Growth Factor
Published in Science (American Association for the Advancement of Science) (20-07-1990)“…Epidermal growth factor treatment of A-431 epidermoid carcinoma cells elicited a redistribution of phospholipase C-gamma1 from a predominantly cytosolic…”
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PMN binding to P-selectin is inhibited by sulfatide
Published in Journal of leukocyte biology (01-07-1992)“…The endothelial adhesion protein P-selectin binds to a ligand present on the surface of leukocytes. We have characterized the binding interaction between…”
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Stimulation of Phospholipase C-γl Membrane Association by Epidermal Growth Factor
Published in Science (American Association for the Advancement of Science) (20-07-1990)“…Epidermal growth factor (EGF) treatment of A-431 epidermoid carcinoma cells elicited a redistribution of phospholipase C-γ1 (PLC-γ1) from a predominantly…”
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