Search Results - "Jackson, Clive G."
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Design and Synthesis of a Novel and Potent Series of Inhibitors of Cytosolic Phospholipase A2 Based on a 1,3-Disubstituted Propan-2-one Skeleton
Published in Journal of medicinal chemistry (14-03-2002)“…Using knowledge of the substrate specificity of cPLA2 (phospholipases A2), a novel series of inhibitors of this enzyme were designed based upon a three point…”
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Design of novel and potent cPLA2α inhibitors containing an α-methyl-2-ketothiazole as a metabolically stable serine trap
Published in Bioorganic & medicinal chemistry letters (15-05-2011)“…We report the design of novel, potent cPLA(2)α inhibitors that possess an α-methyl-2-ketothiazole that acts as a serine-reactive moiety. We describe the…”
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Synthesis and evaluation of substrate-mimicking cytosolic phospholipase A2 inhibitors: reducing the lipophilicity of the arachidonyl chain isostere
Published in Bioorganic & medicinal chemistry letters (16-07-2004)“…The high lipophilicity of a series of cytosolic phospholipase A(2) inhibitors has been reduced by the modification of a decyloxyphenyl chain designed to mimic…”
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Discovery of new non-phospholipid inhibitors of the secretory phospholipases A2
Published in Journal of medicinal chemistry (01-03-1994)Get full text
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The regulation by phosphorylation of ‘priming’ of phospholipase A2 activity in the neutrophil model system, differentiated HL60 cells
Published in British journal of pharmacology (01-09-1997)“…1 Differentiated HL60 cells have been utilized as a model system to examine the ‘priming’ of neutrophil phospholipase A2 activity. In control cells activation…”
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Design and synthesis of some substrate analog inhibitors of phospholipase A2 and investigations by NMR and molecular modeling into the binding interactions in the enzyme-inhibitor complex
Published in Journal of medicinal chemistry (01-08-1992)“…A series of substrate analogue inhibitors of pancreatic phospholipase A2 has been designed and synthesized. The compounds were tested in a novel dual-screening…”
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Monocarboxylate transporter MCT1 is a target for immunosuppression
Published in Nature chemical biology (01-12-2005)“…Current immunosuppressive therapies act on T lymphocytes by modulation of cytokine production, modulation of signaling pathways or by inhibition of the enzymes…”
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The regulation by phosphorylation of ‘priming’ of phospholipase A 2 activity in the neutrophil model system, differentiated HL60 cells
Published in British journal of pharmacology (03-02-2009)“…Differentiated HL60 cells have been utilized as a model system to examine the ‘priming’ of neutrophil phospholipase A 2 activity. In control cells activation…”
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Design of novel and potent cPLA sub(2 alpha inhibitors containing an alpha -methyl-2-ketothiazole as a metabolically stable serine trap)
Published in Bioorganic & medicinal chemistry letters (15-05-2011)“…We report the design of novel, potent cPLA sub(2 alpha inhibitors that possess an alpha -methyl-2-ketothiazole that acts as a serine-reactive moiety. We…”
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Design of novel and potent cPLA 2α inhibitors containing an α-methyl-2-ketothiazole as a metabolically stable serine trap
Published in Bioorganic & medicinal chemistry letters (2011)“…We report the design of novel, potent cPLA 2α inhibitors that possess an α-methyl-2-ketothiazole that acts as a serine-reactive moiety. We describe the…”
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Design and synthesis of a novel and potent series of inhibitors of cytosolic phospholipase A(2) based on a 1,3-disubstituted propan-2-one skeleton
Published in Journal of medicinal chemistry (14-03-2002)“…Using knowledge of the substrate specificity of cPLA(2) (phospholipases A(2)), a novel series of inhibitors of this enzyme were designed based upon a three…”
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The isolation and purification of the elvapeptins
Published in FEBS letters (23-08-1982)Get full text
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Antigen receptors on immature, but not mature, B and T cells are coupled to cytosolic phospholipase A2 activation: expression and activation of cytosolic phospholipase A2 correlate with lymphocyte maturation
Published in The Journal of immunology (1950) (15-03-1996)“…The Ag receptors on mature B and T cells are not coupled to the activation of cytosolic phospholipase A2 (cPLA2) and arachidonic acid release. Moreover,…”
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pHG165: a pBR322 copy number derivative of pUC8 for cloning and expression
Published in Plasmid (01-05-1986)“…During the construction of the Messing pUC plasmid series, the rop(rom) gene of pBR322 which mediates the activity of RNAI was deleted. This has resulted in an…”
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Bombesin stimulates the rapid activation of phospholipase A2-catalyzed phosphatidylcholine hydrolysis in Swiss 3T3 cells
Published in The Journal of biological chemistry (25-03-1992)“…In Swiss 3T3 fibroblasts bombesin stimulated the release of arachidonic acid in a time- and dose-dependent manner. Arachidonate levels were significantly…”
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The isolation and purification of the elvapeptins: A family of peptide inhibitors of mitochondrial ATPase activity
Published in FEBS letters (01-01-1982)“…The mould, Tolypocladium inflatum has been shown to produce the efrapeptins, a family of closely related hydrophobic peptide anitibiotics, which are potent…”
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