Search Results - "George, Sven"
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Synthesis and In Vitro Biological Evaluation of p -Carborane-Based Di- tert -butylphenol Analogs
Published in Molecules (Basel, Switzerland) (04-06-2023)“…Targeting inflammatory mediators and related signaling pathways may offer a rational strategy for the treatment of cancer. The incorporation of metabolically…”
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Structural Modifications Yield Novel Insights Into the Intriguing Pharmacodynamic Potential of Anti-inflammatory Nitro-Fatty Acids
Published in Frontiers in pharmacology (18-11-2021)“…Endogenous nitro-fatty acids (NFA) are potent electrophilic lipid mediators that exert biological effects in vitro and in vivo via selective covalent…”
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Novel and Potent Inhibitors of 5-Lipoxygenase Product Synthesis Based on the Structure of Pirinixic Acid
Published in Journal of medicinal chemistry (11-09-2008)“…A novel class of potent 5-lipoxygenase (5-LO) product synthesis inhibitors based on the structure of pirinixic acid…”
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4
3-O-acetyl-11-keto-boswellic acid decreases basal intracellular Ca2+ levels and inhibits agonist-induced Ca2+ mobilization and mitogen-activated protein kinase activation in human monocytic cells
Published in The Journal of pharmacology and experimental therapeutics (01-01-2006)“…Previously, we showed that 11-keto-boswellic acid and 3-O-acetyl-11-keto-BA (AKBA) stimulate Ca(2+) mobilization and activate mitogen-activated protein kinases…”
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5
On the biosynthesis of specialized pro-resolving mediators in human neutrophils and the influence of cell integrity
Published in Biochimica et biophysica acta. Molecular and cell biology of lipids (01-03-2022)“…Neutrophils are key players in inflammation initiation and resolution. Little attention has been paid to the detailed biosynthesis of specialized pro-resolving…”
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Unlocking the potential: unveiling tyrphostins with Michael-reactive cyanoacrylate motif as promising inhibitors of human 5-lipoxygenase
Published in Pflügers Archiv (30-09-2024)“…Human 5-lipoxygenase (5-LO) is the key enzyme in the biosynthesis of leukotrienes, mediators of the innate immune system that also play an important role in…”
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Thiazole derivatives as dual inhibitors of deoxyribonuclease I and 5-lipoxygenase: A promising scaffold for the development of neuroprotective drugs
Published in Chemico-biological interactions (25-08-2023)“…A library of 43 thiazole derivatives, including 31 previously and 12 newly synthesized in the present study, was evaluated in vitro for their inhibitory…”
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Design, Synthesis, and Structure–Activity Relationship Studies of Dual Inhibitors of Soluble Epoxide Hydrolase and 5‑Lipoxygenase
Published in Journal of medicinal chemistry (22-10-2020)“…Inhibition of multiple enzymes of the arachidonic acid cascade leads to synergistic anti-inflammatory effects. Merging of 5-lipoxygenase (5-LOX) and soluble…”
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9
Systematic Assessment of Fragment Identification for Multitarget Drug Design
Published in ChemMedChem (08-04-2021)“…Designed multitarget ligands are a popular approach to generating efficient and safe drugs, and fragment‐based strategies have been postulated as a versatile…”
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Repurposing of 8‐Hydroxyquinoline‐Based Butyrylcholinesterase and Cathepsin B Ligands as Potent Nonpeptidic Deoxyribonuclease I Inhibitors
Published in ChemMedChem (04-03-2022)“…A library of 31 butyrylcholinesterase (BChE) and cathepsin B (CatB) inhibitors was screened in vitro for inhibition of deoxyribonuclease I (DNase I). Compounds…”
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Carborane‐Based Tebufelone Analogs and Their Biological Evaluation In Vitro
Published in ChemMedChem (17-07-2023)“…The presence of inflammatory mediators in the tumor microenvironment, such as cytokines, growth factors or eicosanoids, indicate cancer‐related inflammatory…”
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Borcalein: a Carborane‐Based Analogue of Baicalein with 12‐Lipoxygenase‐Independent Toxicity
Published in ChemMedChem (05-01-2022)“…12‐Lipoxygenase is crucial for tumour angiogenesis. 5,6,7‐Trihydroxy‐2‐phenyl‐4H‐1‐benzopyran‐4‐one (baicalein) is a suitable inhibitor for this enzyme but is…”
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Characterization of the interaction of human 5-lipoxygenase with its activating protein FLAP
Published in Biochimica et biophysica acta (01-11-2015)“…Human 5-lipoxygenase (5-LO) is the key enzyme in the formation of leukotrienes (LTs), important mediators of inflammation. Cellular 5-LO activity is regulated…”
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In Vitro Cytostatic Effect on Tumor Cells by Carborane‐Based Dual Cyclooxygenase‐2 and 5‐Lipoxygenase Inhibitors (Adv. Therap. 4/2023)
Published in Advanced therapeutics (01-04-2023)“…Cyclooxygenase‐2 (COX‐2) and 5‐lipoxygenase (5‐LO) are key enzymes in the biosynthesis of pro‐inflammatory and tumor‐inducing eicosanoids. Thus, dual…”
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In Vitro Cytostatic Effect on Tumor Cells by Carborane‐Based Dual Cyclooxygenase‐2 and 5‐Lipoxygenase Inhibitors
Published in Advanced therapeutics (01-04-2023)“…The selective inhibition of enzymes that catalyze the conversion of arachidonic acid to inflammatory eicosanoids represents a promising approach for cancer…”
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Carborane‐Based Analogues of 5‐Lipoxygenase Inhibitors Co‐inhibit Heat Shock Protein 90 in HCT116 Cells
Published in ChemMedChem (22-01-2019)“…5‐Lipoxygenase converts arachidonic acid into leukotrienes, which are involved in inflammation and angiogenesis. The introduction of carboranes can improve the…”
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CarbORev‐5901: The First Carborane‐Based Inhibitor of the 5‐Lipoxygenase Pathway
Published in ChemMedChem (06-07-2017)“…The progression of cancer is accelerated by increased proliferation, angiogenesis, and inflammation. These processes are mediated by leukotrienes. Several…”
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Synthesis and Structure–Activity Relationship Studies of Novel Dual Inhibitors of Soluble Epoxide Hydrolase and 5‑Lipoxygenase
Published in Journal of medicinal chemistry (28-02-2013)“…Current research leads to the assumption that drugs affecting more than one target could result in a more efficient treatment of diseases and fewer safety…”
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Design and Synthesis of Novel 2-Amino-5-hydroxyindole Derivatives That Inhibit Human 5-Lipoxygenase
Published in Journal of medicinal chemistry (13-07-2006)“…Compounds that inhibit 5-lipoxygenase (5-LO), the key enzyme in the biosynthesis of leukotrienes (LTs), possess potential for the treatment of inflammatory and…”
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Identification of Natural-Product-Derived Inhibitors of 5-Lipoxygenase Activity by Ligand-Based Virtual Screening
Published in Journal of medicinal chemistry (31-05-2007)“…A natural product collection and natural-product-derived combinatorial libraries were virtually screened for potential inhibitors of human 5-lipoxygenase…”
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