Search Results - "KRAUTH‐SIEGEL, R. Luise"
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Tryparedoxin peroxidase-deficiency commits trypanosomes to ferroptosis-type cell death
Published in eLife (26-07-2018)“…Tryparedoxin peroxidases, distant relatives of glutathione peroxidase 4 in higher eukaryotes, are responsible for the detoxification of lipid-derived…”
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Targeting a Large Active Site: Structure‐Based Design of Nanomolar Inhibitors of Trypanosoma brucei Trypanothione Reductase
Published in Chemistry : a European journal (02-09-2019)“…Trypanothione reductase (TR) plays a key role in the unique redox metabolism of trypanosomatids, the causative agents of human African trypanosomiasis (HAT),…”
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Inhibitor‐Induced Dimerization of an Essential Oxidoreductase from African Trypanosomes
Published in Angewandte Chemie International Edition (11-03-2019)“…Trypanosomal and leishmanial infections claim tens of thousands of lives each year. The metabolism of these unicellular eukaryotic parasites differs from the…”
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Biological Activities of Xanthatin from Xanthium strumarium Leaves
Published in Phytotherapy research (01-12-2011)“…The objective of the present work was to evaluate the biological activities of the major bioactive compound, xanthatin, and other compounds from Xanthium…”
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In Vitro and In Silico Analysis of New n-Butyl and Isobutyl Quinoxaline-7-carboxylate 1,4-di- N -oxide Derivatives against Trypanosoma cruzi as Trypanothione Reductase Inhibitors
Published in International journal of molecular sciences (01-11-2022)“…American trypanosomiasis is a worldwide health problem that requires attention due to ineffective treatment options. We evaluated n-butyl and isobutyl…”
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A tryparedoxin-coupled biosensor reveals a mitochondrial trypanothione metabolism in trypanosomes
Published in eLife (31-01-2020)“…Trypanosomes have a trypanothione redox metabolism that provides the reducing equivalents for numerous essential processes, most being mediated by tryparedoxin…”
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Trypanothione reductase: a target protein for a combined in vitro and in silico screening approach
Published in PLoS neglected tropical diseases (04-06-2015)“…With the goal to identify novel trypanothione reductase (TR) inhibitors, we performed a combination of in vitro and in silico screening approaches. Starting…”
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Dithiol Proteins as Guardians of the Intracellular Redox Milieu in Parasites: Old and New Drug Targets in Trypanosomes and Malaria-Causing Plasmodia
Published in Angewandte Chemie International Edition (21-01-2005)“…Parasitic diseases such as sleeping sickness, Chagas' heart disease, and malaria are major health problems in poverty‐stricken areas. Antiparasitic drugs that…”
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Biological Evaluation and X‐ray Co‐crystal Structures of Cyclohexylpyrrolidine Ligands for Trypanothione Reductase, an Enzyme from the Redox Metabolism of Trypanosoma
Published in ChemMedChem (08-05-2018)“…The tropical diseases human African trypanosomiasis, Chagas disease, and the various forms of leishmaniasis are caused by parasites of the family of…”
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Lipoamide dehydrogenase is essential for both bloodstream and procyclic Trypanosoma brucei
Published in Molecular microbiology (01-08-2011)“…Summary Lipoamide dehydrogenase (LipDH) is a component of four mitochondrial multienzyme complexes. RNA interference or the deletion of both alleles in…”
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Privileged structure-guided synthesis of quinazoline derivatives as inhibitors of trypanothione reductase
Published in Bioorganic & medicinal chemistry letters (01-06-2009)“…Novel quinazoline-type compounds were designed as inhibitors of the parasite specific enzyme trypanothione reductase (TR), and their biological activities were…”
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Pentafluorosulfanyl as a Novel Building Block for Enzyme Inhibitors: Trypanothione Reductase Inhibition and Antiprotozoal Activities of Diarylamines
Published in Chembiochem : a European journal of chemical biology (05-01-2009)“…Pentafluorosulfanyl power! The SF5 group—a novel substituent with striking physicochemical properties—was used as building block for trypanothione reductase…”
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Low-molecular-mass antioxidants in parasites
Published in Antioxidants & redox signaling (15-08-2012)“…Parasitic infections continue to be a major problem for global human health. Vaccines are practically not available and chemotherapy is highly unsatisfactory…”
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Natural Sesquiterpene Lactones of the 4,15- iso -Atriplicolide Type are Inhibitors of Trypanothione Reductase
Published in Molecules (Basel, Switzerland) (16-10-2019)“…In the course of our investigations on the antitrypanosomal potential of sesquiterpene lactones (STL), we have recently reported on the exceptionally strong…”
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Synthesis, Inhibition Potency, Binding Mode, and Antiprotozoal Activities of Fluorescent Inhibitors of Trypanothione Reductase Based on Mepacrine-Conjugated Diaryl Sulfide Scaffolds
Published in ChemMedChem (07-12-2009)“…Trypanothione reductase (TR) is a flavoenzyme unique to trypanosomatid parasites and a target for lead discovery programs. Various inhibitor scaffolds have…”
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The cytosolic or the mitochondrial glutathione peroxidase‐type tryparedoxin peroxidase is sufficient to protect procyclic Trypanosoma brucei from iron‐mediated mitochondrial damage and lysis
Published in Molecular Microbiology (01-01-2016)“…Summary African trypanosomes express three virtually identical glutathione peroxidase (Px)‐type enzymes that occur in the cytosol (Px I and II) and…”
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The mitochondrial peroxiredoxin displays distinct roles in different developmental stages of African trypanosomes
Published in Redox biology (01-07-2020)“…Hydroperoxide reduction in African trypanosomes relies on 2-Cys-peroxiredoxins (Prxs) and glutathione peroxidase-type enzymes (Pxs) which both obtain their…”
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Betraying the Parasite's Redox System: Diaryl Sulfide-Based Inhibitors of Trypanothione Reductase: Subversive Substrates and Antitrypanosomal Properties
Published in ChemMedChem (10-12-2007)“…Subversive substrates. Replacing the 3,4‐dichlorophenyl entity of diphenyl sulfide‐based trypanothione reductase (TR) inhibitors for a nitrofuran moiety led to…”
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An essential thioredoxin-type protein of Trypanosoma brucei acts as redox-regulated mitochondrial chaperone
Published in PLoS pathogens (26-09-2019)“…Most known thioredoxin-type proteins (Trx) participate in redox pathways, using two highly conserved cysteine residues to catalyze thiol-disulfide exchange…”
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The Dithiol Glutaredoxins of African Trypanosomes Have Distinct Roles and Are Closely Linked to the Unique Trypanothione Metabolism
Published in The Journal of biological chemistry (05-11-2010)“…Trypanosoma brucei, the causative agent of African sleeping sickness, possesses two dithiol glutaredoxins (Grx1 and Grx2). Grx1 occurs in the cytosol and…”
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