Ebsulfur is a benzisothiazolone cytocidal inhibitor targeting the trypanothione reductase of Trypanosoma brucei.

scientific article published on 29 July 2013

Ebsulfur is a benzisothiazolone cytocidal inhibitor targeting the trypanothione reductase of Trypanosoma brucei. is …
instance of (P31):
scholarly articleQ13442814

External links are
P356DOI10.1074/JBC.M113.495101
P932PMC publication ID3779740
P698PubMed publication ID23900839

P50authorJun LuQ55979634
Tomas N GustafssonQ58227533
Sangit KumarQ59618397
Martin E RottenbergQ61113293
P2093author name stringBirger Sjöberg
Arne Holmgren
Suman K Vodnala
Lars Engman
Anna-Lena Gustavsson
Agneta Tjernberg
Henrik A Johansson
P2860cites workTwo interacting binding sites for quinacrine derivatives in the active site of trypanothione reductase: a template for drug designQ24616801
High-resolution structures of oxidized and reduced thioredoxin reductase from Helicobacter pyloriQ27646201
Comparative structural, kinetic and inhibitor studies of Trypanosoma brucei trypanothione reductase with T. cruziQ27657406
Dihydroquinazolines as a Novel Class of Trypanosoma brucei Trypanothione Reductase Inhibitors: Discovery, Synthesis, and Characterization of their Binding Mode by Protein CrystallographyQ27671819
Trypanosomes lacking trypanothione reductase are avirulent and show increased sensitivity to oxidative stressQ28144631
Dual action of antimonial drugs on thiol redox metabolism in the human pathogen Leishmania donovaniQ28271918
Redox control in trypanosomatids, parasitic protozoa with trypanothione-based thiol metabolismQ28275518
Molecular actions of Ebselen—an antiinflammatory antioxidantQ28291545
Trypanothione: a novel bis(glutathionyl)spermidine cofactor for glutathione reductase in trypanosomatidsQ28306157
A target-based high throughput screen yields Trypanosoma brucei hexokinase small molecule inhibitors with antiparasitic activityQ28473648
Cerebral vessel laminins and IFN-gamma define Trypanosoma brucei brucei penetration of the blood-brain barrierQ28510213
Investigation of trypanothione reductase as a drug target in Trypanosoma bruceiQ30897674
Improved tricyclic inhibitors of trypanothione reductase by screening and chemical synthesisQ33474992
Trypanothione is the primary target for arsenical drugs against African trypanosomesQ33849836
Enzymes of the trypanothione metabolism as targets for antitrypanosomal drug developmentQ33960778
Metabolism and functions of trypanothione in the KinetoplastidaQ33972467
Ebselen: a substrate for human thioredoxin reductase strongly stimulating its hydroperoxide reductase activity and a superfast thioredoxin oxidantQ34065084
Esters of methanesulfonic acid as irreversible inhibitors of acetylcholinesteraseQ34254828
Parasites and the brain: neuroinvasion, immunopathogenesis and neuronal dysfunctions.Q34640320
Specific chemotherapy of Chagas disease: controversies and advancesQ35569069
Down-regulation of Leishmania donovani trypanothione reductase by heterologous expression of a trans-dominant mutant homologue: effect on parasite intracellular survivalQ36069752
Inhibition of glutathione synthesis as a chemotherapeutic strategy for trypanosomiasisQ36344549
Programmed cell death in African trypanosomes.Q36612384
Targeting Trypanothione Metabolism in Trypanosomatid Human ParasitesQ37782110
Low-molecular-mass antioxidants in parasites.Q37952777
Active site of trypanothione reductase. A target for rational drug design.Q39088644
RNA interference identifies two hydroperoxide metabolizing enzymes that are essential to the bloodstream form of the african trypanosome.Q39594334
Antiparasitic prodrug nifurtimox: revisiting its activation mechanismQ39715054
Susceptibility of methicillin-resistant Staphylococcus aureus to the selenium-containing compound 2-phenyl-1,2-benzoisoselenazol-3(2H)-one (PZ51).Q39819760
Depletion of the thioredoxin homologue tryparedoxin impairs antioxidative defence in African trypanosomesQ40220444
Flavoprotein structure and mechanism. 5. Trypanothione reductase and lipoamide dehydrogenase as targets for a structure-based drug design.Q40481216
Azaanalogues of ebselen as antimicrobial and antiviral agents: synthesis and propertiesQ40491914
Bacillus anthracis thioredoxin systems, characterization and role as electron donors for ribonucleotide reductaseQ41462921
Potent, selective, and orally available benzoisothiazolone phosphomannose isomerase inhibitors as probes for congenital disorder of glycosylation Ia.Q41879491
Disruption of the trypanothione reductase gene of Leishmania decreases its ability to survive oxidative stress in macrophages.Q42123859
Rationally designed selective inhibitors of trypanothione reductase. Phenothiazines and related tricyclics as lead structuresQ42152987
The dithiol glutaredoxins of african trypanosomes have distinct roles and are closely linked to the unique trypanothione metabolismQ42394562
Drug-resistance of Trypanosoma b. rhodesiense isolates from TanzaniaQ43947251
A novel antioxidant mechanism of ebselen involving ebselen diselenide, a substrate of mammalian thioredoxin and thioredoxin reductaseQ44102189
Substrate specificity, localization, and essential role of the glutathione peroxidase-type tryparedoxin peroxidases in Trypanosoma bruceiQ45234385
The effect of TAO expression on PCD-like phenomenon development and drug resistance in Trypanosoma bruceiQ46229139
Inhibitors of Trypanosoma cruzi trypanothione reductase revealed by virtual screening and parallel synthesisQ46610163
Inhibition of bacterial thioredoxin reductase: an antibiotic mechanism targeting bacteria lacking glutathione.Q53128898
Cerebral vessel laminins and IFN-γ define Trypanosoma brucei brucei penetration of the blood-brain barrierQ58852404
Human neutrophils lose their surface Fc gamma RIII and acquire Annexin V binding sites during apoptosis in vitroQ72386143
Inhibition of Trypanosoma cruzi trypanothione reductase by acridines: kinetic studies and structure-activity relationshipsQ73364992
Inhibition of thioredoxin reductase by a novel series of bis-1,2-benzisoselenazol-3(2H)-ones: Organoselenium compounds for cancer therapyQ84115829
P433issue38
P407language of work or nameEnglishQ1860
P921main subjectTrypanosoma bruceiQ33244
P304page(s)27456-27468
P577publication date2013-07-29
P1433published inJournal of Biological ChemistryQ867727
P1476titleEbsulfur is a benzisothiazolone cytocidal inhibitor targeting the trypanothione reductase of Trypanosoma brucei
P478volume288

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cites work (P2860)
Q89662547Computational approaches for drug discovery against trypanosomatid-caused diseases
Q35987945Development of ebsulfur analogues as potent antibacterials against methicillin-resistant Staphylococcus aureus
Q41479143Diglycosyl diselenides alter redox homeostasis and glucose consumption of infective African trypanosomes
Q34361091Ebselen inhibits hepatitis C virus NS3 helicase binding to nucleic acid and prevents viral replication
Q33898663Essential multimeric enzymes in kinetoplastid parasites: A host of potentially druggable protein-protein interactions
Q37390542Exploring the mode of action of ebselen in Trypanosoma brucei hexokinase inhibition
Q36059265Identification of Ebsulfur Analogues with Broad-Spectrum Antifungal Activity
Q51730944NADPH-dependent and -independent Disulfide Reductase Systems.
Q38695331Screening the Medicines for Malaria Venture Pathogen Box across Multiple Pathogens Reclassifies Starting Points for Open-Source Drug Discovery.
Q40175261Synergistic antibacterial effect of silver and ebselen against multidrug-resistant Gram-negative bacterial infections.
Q36076081The Oral Antimalarial Drug Tafenoquine Shows Activity against Trypanosoma brucei
Q33599669The establishment of in vitro culture and drug screening systems for a newly isolated strain of Trypanosoma equiperdum

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