Search Results - "van der Wouden, Petra"
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Proteolysis Targeting Chimera (PROTAC) for Macrophage Migration Inhibitory Factor (MIF) Has Anti‐Proliferative Activity in Lung Cancer Cells
Published in Angewandte Chemie International Edition (02-08-2021)“…Macrophage migration inhibitory factor (MIF) is involved in protein‐protein interactions that play key roles in inflammation and cancer. Current strategies to…”
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A next-generation sequencing method for gene doping detection that distinguishes low levels of plasmid DNA against a background of genomic DNA
Published in Gene therapy (01-08-2019)“…Gene doping confers health risks for athletes and is a threat to fair competition in sports. Therefore the anti-doping community has given attention on its…”
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De novo CoA biosynthesis is required to maintain DNA integrity during development of the Drosophila nervous system
Published in Human molecular genetics (01-07-2008)“…In a forward genetic screen in Drosophila melanogaster, aimed to identify genes required for normal locomotor function, we isolated dPPCS (the second enzyme of…”
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Induced protein degradation of histone deacetylases 3 (HDAC3) by proteolysis targeting chimera (PROTAC)
Published in European journal of medicinal chemistry (15-12-2020)“…Histone deacetylases (HDACs) play important roles in inflammatory diseases like asthma and chronic obstructive pulmonary disease (COPD). Unravelling of and…”
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Histone Deacetylase 3‐Directed PROTACs Have Anti‐inflammatory Potential by Blocking Polarization of M0‐like into M1‐like Macrophages
Published in Angewandte Chemie International Edition (16-10-2023)“…Abstract Macrophage polarization plays a crucial role in inflammatory processes. The histone deacetylase 3 (HDAC3) has a deacetylase‐independent function that…”
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Identification of a Bromodomain‐like Region in 15‐Lipoxygenase‐1 Explains Its Nuclear Localization
Published in Angewandte Chemie International Edition (27-09-2021)“…Lipoxygenase (LOX) activity provides oxidative lipid metabolites, which are involved in inflammatory disorders and tumorigenesis. Activity‐based probes to…”
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Light-controlled inhibition of BRAFV600E kinase
Published in European journal of medicinal chemistry (01-10-2019)“…Metastatic melanoma is amongst the most difficult types of cancer to treat, with current therapies mainly relying on the inhibition of the BRAFV600E mutant…”
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HDAC1-3 inhibitor MS-275 enhances IL10 expression in RAW264.7 macrophages and reduces cigarette smoke-induced airway inflammation in mice
Published in Scientific reports (27-03-2017)“…Chronic obstructive pulmonary disease (COPD) constitutes a major health burden. Studying underlying molecular mechanisms could lead to new therapeutic targets…”
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Thieno[2,3‑d]pyrimidine-2,4(1H,3H)‑dione Derivative Inhibits d‑Dopachrome Tautomerase Activity and Suppresses the Proliferation of Non-Small Cell Lung Cancer Cells
Published in Journal of medicinal chemistry (10-02-2022)“…The homologous cytokines macrophage migration inhibitory factor (MIF) and d-dopachrome tautomerase (d-DT or MIF2) play key roles in cancers. Molecules binding…”
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Allosteric Inhibitors of Macrophage Migration Inhibitory Factor (MIF) Interfere with Apoptosis-Inducing Factor (AIF) Co-Localization to Prevent Parthanatos
Published in Journal of medicinal chemistry (13-07-2023)“…Macrophage migration inhibitory factor (MIF) is a multifunctional cytokine and essential signaling protein associated with inflammation and cancers. One of the…”
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HDAC 3-selective inhibitor RGFP966 demonstrates anti-inflammatory properties in RAW 264.7 macrophages and mouse precision-cut lung slices by attenuating NF-κB p65 transcriptional activity
Published in Biochemical pharmacology (15-05-2016)“…[Display omitted] The increasing number of patients suffering from chronic obstructive pulmonary disease (COPD) represents a major and increasing health…”
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The synthesis of 1,2,3-triazoles as binders of D-dopachrome tautomerase (D-DT) for the development of dual-targeting inhibitors
Published in European journal of medicinal chemistry (05-10-2024)“…Despite recent advances in the treatment of cancer, the issue of therapy resistance remains one of the most significant challenges in the field. In this…”
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7‑Hydroxycoumarins Are Affinity-Based Fluorescent Probes for Competitive Binding Studies of Macrophage Migration Inhibitory Factor
Published in Journal of medicinal chemistry (22-10-2020)“…Macrophage migration inhibitory factor (MIF) is a cytokine with key roles in inflammation and cancer, which qualifies it as a potential drug target. Apart from…”
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Rational Development of a Potent 15-Lipoxygenase‑1 Inhibitor with in Vitro and ex Vivo Anti-inflammatory Properties
Published in Journal of medicinal chemistry (08-10-2015)“…Human 15-lipoxygenase-1 (h-15-LOX-1) is a mammalian lipoxygenase and plays an important role in several inflammatory lung diseases such as asthma, COPD, and…”
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4‐Iodopyrimidine Labeling Reveals Nuclear Translocation and Nuclease Activity for Both MIF and MIF2
Published in Chemistry : a European journal (03-01-2022)“…Macrophage migration inhibitory factor (MIF) and its homolog MIF2 (also known as D‐dopachrome tautomerase or DDT) play key roles in cell growth and immune…”
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Enzyme kinetics and inhibition of histone acetyltransferase KAT8
Published in European journal of medicinal chemistry (13-11-2015)“…Lysine acetyltransferase 8 (KAT8) is a histone acetyltransferase (HAT) responsible for acetylating lysine 16 on histone H4 (H4K16) and plays a role in cell…”
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Novel 15-Lipoxygenase‑1 Inhibitor Protects Macrophages from Lipopolysaccharide-Induced Cytotoxicity
Published in Journal of medicinal chemistry (09-05-2019)“…Various mechanisms for regulated cell death include the formation of oxidative mediators such as lipid peroxides and nitric oxide (NO). In this respect,…”
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Deposition Bias of Chromatin Proteins Inverts under DNA Replication Stress Conditions
Published in ACS chemical biology (19-11-2021)“…Following DNA replication, equal amounts of chromatin proteins are distributed over sister chromatids by re-deposition of parental chromatin proteins and…”
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Protocol of the Double-Click Seq Method to Evaluate the Deposition Bias of Chromatin Proteins
Published in Current protocols (01-06-2023)“…Symmetrical deposition of parental and newly synthesized chromatin proteins over both sister chromatids is important for the maintenance of epigenetic…”
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The relevance of K i calculation for bi-substrate enzymes illustrated by kinetic evaluation of a novel lysine (K) acetyltransferase 8 inhibitor
Published in European journal of medicinal chemistry (18-08-2017)“…Histone acetyltransferases (HATs) are important mediators of epigenetic post-translational modifications of histones that play important roles in health and…”
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