Search Results - "Gagestein, Berend"
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Anandamide and other N-acylethanolamines: A class of signaling lipids with therapeutic opportunities
Published in Progress in lipid research (01-01-2023)“…N-acylethanolamines (NAEs), including N-palmitoylethanolamine (PEA), N-oleoylethanolamine (OEA), N-arachidonoylethanolamine (AEA, anandamide),…”
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Live‐Cell Imaging of Sterculic Acid—a Naturally Occurring 1,2‐Cyclopropene Fatty Acid—by Bioorthogonal Reaction with Turn‐On Tetrazine‐Fluorophore Conjugates
Published in Angewandte Chemie International Edition (19-09-2022)“…In the field of lipid research, bioorthogonal chemistry has made the study of lipid uptake and processing in living systems possible, whilst minimising…”
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Comparative Photoaffinity Profiling of Omega‑3 Signaling Lipid Probes Reveals Prostaglandin Reductase 1 as a Metabolic Hub in Human Macrophages
Published in Journal of the American Chemical Society (19-10-2022)“…The fish oil constituent docosahexaenoic acid (DHA, 22:6 n-3) is a signaling lipid with anti-inflammatory properties. The molecular mechanisms underlying the…”
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Discovery of isoquinoline sulfonamides as allosteric gyrase inhibitors with activity against fluoroquinolone-resistant bacteria
Published in Nature chemistry (01-09-2024)“…Bacteria have evolved resistance to nearly all known antibacterials, emphasizing the need to identify antibiotics that operate via novel mechanisms. Here we…”
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Previously Published Phosphatase Probes have Limited Utility Due to their Unspecific Reactivity
Published in Chembiochem : a European journal of chemical biology (18-11-2024)“…This study explores the use of activity‐based protein profiling to study protein tyrosine phosphatases. With the discovery of allosteric SHP2 inhibitors, this…”
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Chemical Proteomics Reveals Off-Targets of the Anandamide Reuptake Inhibitor WOBE437
Published in ACS chemical biology (20-05-2022)“…Anandamide or N-arachidonoylethanolamine (AEA) is a signaling lipid that modulates neurotransmitter release via activation of the type 1 cannabinoid receptor…”
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Olaparib‐Based Photoaffinity Probes for PARP‐1 Detection in Living Cells
Published in Chembiochem : a European journal of chemical biology (01-09-2020)“…The poly‐ADP‐ribose polymerase (PARP) is a protein from the family of ADP‐ribosyltransferases that catalyzes polyadenosine diphosphate ribose (ADPR) formation…”
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Comprehensive structure-activity-relationship of azaindoles as highly potent FLT3 inhibitors
Published in Bioorganic & medicinal chemistry (01-03-2019)“…[Display omitted] Acute myeloid leukemia (AML) is characterized by fast progression and low survival rates, in which Fms-like tyrosine kinase 3 (FLT3) receptor…”
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Opportunities for Lipid-Based Probes in the Field of Immunology
Published in Current topics in microbiology and immunology (01-01-2019)“…Lipids perform a wide range of functions inside the cell, ranging from structural building block of membranes and energy storage to cell signaling. The mode of…”
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Synthesis of α- and β-Galactopyranose-Configured Isomers of Cyclophellitol and Cyclophellitol Aziridine
Published in European journal of organic chemistry (01-09-2014)“…Cyclophellitol and cyclophellitol aziridine are potent and irreversible mechanism‐based inhibitors of retaining β‐glucosidases. Alterations in the…”
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11
Live‐Cell Imaging of Sterculic Acid—a Naturally Occurring 1,2‐Cyclopropene Fatty Acid—by Bioorthogonal Reaction with Turn‐On Tetrazine‐Fluorophore Conjugates
Published in Angewandte Chemie (19-09-2022)“…In the field of lipid research, bioorthogonal chemistry has made the study of lipid uptake and processing in living systems possible, whilst minimising…”
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Synthesis of [alpha]- and [beta]-Galactopyranose-Configured Isomers of Cyclophellitol and Cyclophellitol Aziridine
Published in European journal of organic chemistry (01-09-2014)“…Cyclophellitol and cyclophellitol aziridine are potent and irreversible mechanism-based inhibitors of retaining [beta]-glucosidases. Alterations in the…”
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