Search Results - "De Brabander, Jef"
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Identification of NPC1 as the target of U18666A, an inhibitor of lysosomal cholesterol export and Ebola infection
Published in eLife (08-12-2015)“…Niemann-Pick C1 (NPC1) is a lysosomal membrane protein that exports cholesterol derived from receptor-mediated uptake of LDL, and it also mediates cellular…”
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Structural basis for itraconazole-mediated NPC1 inhibition
Published in Nature communications (09-01-2020)“…Niemann-Pick C1 (NPC1), a lysosomal protein of 13 transmembrane helices (TMs) and three lumenal domains, exports low-density-lipoprotein (LDL)-derived…”
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Gboxin is an oxidative phosphorylation inhibitor that targets glioblastoma
Published in Nature (London) (01-03-2019)“…Cancer-specific inhibitors that reflect the unique metabolic needs of cancer cells are rare. Here we describe Gboxin, a small molecule that specifically…”
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Evaluation of the efficacy of the hypocretin/orexin receptor agonists TAK‐925 and ARN‐776 in narcoleptic orexin/tTA; TetO‐DTA mice
Published in Journal of sleep research (01-08-2023)“…Summary The sleep disorder narcolepsy, a hypocretin deficiency disorder thought to be due to degeneration of hypothalamic hypocretin/orexin neurons, is…”
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Systematic Identification of Molecular Subtype-Selective Vulnerabilities in Non-Small-Cell Lung Cancer
Published in Cell (24-10-2013)“…Context-specific molecular vulnerabilities that arise during tumor evolution represent an attractive intervention target class. However, the frequency and…”
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Molecular mechanism of the wake-promoting agent TAK-925
Published in Nature communications (25-05-2022)“…The OX 2 orexin receptor (OX 2 R) is a highly expressed G protein-coupled receptor (GPCR) in the brain that regulates wakefulness and circadian rhythms in…”
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Triazoles inhibit cholesterol export from lysosomes by binding to NPC1
Published in Proceedings of the National Academy of Sciences - PNAS (03-01-2017)“…Niemann–Pick C1 (NPC1), amembrane protein of lysosomes, is required for the export of cholesterol derived from receptor-mediated endocytosis of LDL. Lysosomal…”
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Selective targeting of mutant adenomatous polyposis coli (APC) in colorectal cancer
Published in Science translational medicine (19-10-2016)“…Mutations in the adenomatous polyposis coli (APC) gene are common in colorectal cancer (CRC), and more than 90% of those mutations generate stable truncated…”
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Total Synthesis and Structure Revision of the Marine Metabolite Palmerolide A
Published in Journal of the American Chemical Society (23-05-2007)“…We describe a highly convergent and flexible synthesis of the novel antarctic marine metabolite palmerolide Aan effort leading to a reformulation of…”
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Reply to: The G protein preference of orexin receptors is currently an unresolved issue
Published in Nature communications (01-06-2023)Get full text
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A Concise Synthesis of Berkelic Acid Inspired by Combining the Natural Products Spicifernin and Pulvilloric Acid
Published in Journal of the American Chemical Society (19-08-2009)“…We describe a concise synthesis of the structurally novel fungal extremophile metabolite berkelic acid, an effort leading to an unambiguous assignment of C22…”
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Rifamycin Biosynthetic Congeners: Isolation and Total Synthesis of Rifsaliniketal and Total Synthesis of Salinisporamycin and Saliniketals A and B
Published in Journal of the American Chemical Society (08-06-2016)“…We describe the isolation, structure elucidation, and total synthesis of the novel marine natural product rifsaliniketal and the total synthesis of the…”
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Inhibition of Influenza A Virus Infection in Vitro by Saliphenylhalamide-Loaded Porous Silicon Nanoparticles
Published in ACS nano (27-08-2013)“…Influenza A viruses (IAVs) cause recurrent epidemics in humans, with serious threat of lethal worldwide pandemics. The occurrence of antiviral-resistant virus…”
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Au(I)- and Pt(II)-Catalyzed Cycloetherification of ω-Hydroxy Propargylic Esters
Published in Organic letters (19-06-2008)“…Depending on the nature of the metal catalyst, ω-hydroxy propargylic acetates choose between alternative cycloetherification manifolds to produce…”
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Cholesterol and 25-Hydroxycholesterol Inhibit Activation of SREBPs by Different Mechanisms, Both Involving SCAP and Insigs
Published in The Journal of biological chemistry (10-12-2004)“…The current paper demonstrates that cholesterol and its hydroxylated derivative, 25-hydroxycholesterol (25-HC), inhibit cholesterol synthesis by two different…”
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Biomarker Accessible and Chemically Addressable Mechanistic Subtypes of BRAF Melanoma
Published in Cancer discovery (01-08-2017)“…Genomic diversity among melanoma tumors limits durable control with conventional and targeted therapies. Nevertheless, pathologic activation of the ERK1/2…”
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Structural insights for selective disruption of Beclin 1 binding to Bcl-2
Published in Communications biology (24-10-2023)“…Stimulation of autophagy could provide powerful therapies for multiple diseases, including cancer and neurodegeneration. An attractive drug target for this…”
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Inhibition of iron uptake is responsible for differential sensitivity to V-ATPase inhibitors in several cancer cell lines
Published in PloS one (16-07-2010)“…Many cell lines derived from tumors as well as transformed cell lines are far more sensitive to V-ATPase inhibitors than normal counterparts. The molecular…”
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Lessons and revelations from biomimetic syntheses
Published in Nature chemical biology (15-11-2011)Get full text
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Disruption of the vacuolar-type H+-ATPase complex in liver causes MTORC1-independent accumulation of autophagic vacuoles and lysosomes
Published in Autophagy (03-04-2017)“…The vacuolar-type H + -translocating ATPase (v-H + -ATPase) has been implicated in the amino acid-dependent activation of the mechanistic target of rapamycin…”
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