Development of novel drugs for human African trypanosomiasis (Q37894699)

24 August 2017

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title

Development of novel drugs for human African trypanosomiasis (English)

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24 August 2017

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African trypanosomiasis

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5

Michael P Barrett

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author name string

Reto Brun

1

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24 August 2017

Robert Don

2

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24 August 2017

Robert T Jacobs

3

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24 August 2017

Michael Zhuo Wang

4

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24 August 2017

Michael P Barrett

5

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24 August 2017

1 June 2011

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24 August 2017

15

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based on heuristic

inferred from page(s)

published in

Future Microbiology

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24 August 2017

6

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24 August 2017

6

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24 August 2017

677-691

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Human African trypanosomiasis

24 August 2017

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Kinetoplastids: related protozoan pathogens, different diseases

21 January 2018

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Human African trypanosomiasis: pharmacological re-engagement with a neglected disease.

21 January 2018

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The natural progression of Gambiense sleeping sickness: what is the evidence?

21 January 2018

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The trypanolytic factor of human serum: many ways to enter the parasite, a single way to kill

21 January 2018

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Mechanism of Trypanosoma brucei gambiense (group 1) resistance to human trypanosome lytic factor

21 January 2018

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Antigenic variation in the African trypanosome: molecular mechanisms and phenotypic complexity

21 January 2018

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The history of African trypanosomiasis

21 January 2018

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Human African trypanosomiasis in areas without surveillance

21 January 2018

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Nifurtimox-eflornithine combination therapy for second-stage African Trypanosoma brucei gambiense trypanosomiasis: a multicentre, randomised, phase III, non-inferiority trial

21 January 2018

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Loss of the high-affinity pentamidine transporter is responsible for high levels of cross-resistance between arsenical and diamidine drugs in African trypanosomes

21 January 2018

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A molecular mechanism for eflornithine resistance in African trypanosomes

21 January 2018

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Genome-wide RNAi screens in African trypanosomes identify the nifurtimox activator NTR and the eflornithine transporter AAT6.

21 January 2018

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Genome-wide RNAi screens in bloodstream form trypanosomes identify drug transporters.

21 January 2018

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A mechanism for cross-resistance to nifurtimox and benznidazole in trypanosomes

21 January 2018

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Nifurtimox activation by trypanosomal type I nitroreductases generates cytotoxic nitrile metabolites.

21 January 2018

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Cross-resistance to nitro drugs and implications for treatment of human African trypanosomiasis

21 January 2018

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The use of the 2 substituted 5-nitroimidazole, Fexinidazole (Hoe 239) in the treatment of chronic T. brucei infections in mice

21 January 2018

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Fexinidazole--a new oral nitroimidazole drug candidate entering clinical development for the treatment of sleeping sickness

21 January 2018

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Pharmacokinetics and metabolism of the prodrug DB289 (2,5-bis[4-(N-methoxyamidino)phenyl]furan monomaleate) in rat and monkey and its conversion to the antiprotozoal/antifungal drug DB75 (2,5-bis(4-guanylphenyl)furan dihydrochloride).

21 January 2018

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New treatment option for second-stage African sleeping sickness: in vitro and in vivo efficacy of aza analogs of DB289

21 January 2018

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Efficacy of the novel diamidine compound 2,5-Bis(4-amidinophenyl)- furan-bis-O-Methlylamidoxime (Pafuramidine, DB289) against Trypanosoma brucei rhodesiense infection in vervet monkeys after oral administration

21 January 2018

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Accumulation and intracellular distribution of antitrypanosomal diamidine compounds DB75 and DB820 in African trypanosomes

21 January 2018

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Roles for the Trypanosoma brucei P2 transporter in DB75 uptake and resistance

21 January 2018

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CYP4F enzymes are the major enzymes in human liver microsomes that catalyze the O-demethylation of the antiparasitic prodrug DB289 [2,5-bis(4-amidinophenyl)furan-bis-O-methylamidoxime].

21 January 2018

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Human enteric microsomal CYP4F enzymes O-demethylate the antiparasitic prodrug pafuramidine

21 January 2018

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Transport of dicationic drugs pentamidine and furamidine by human organic cation transporters

21 January 2018

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Pentamidine movement across the murine blood-brain and blood-cerebrospinal fluid barriers: effect of trypanosome infection, combination therapy, P-glycoprotein, and multidrug resistance-associated protein

21 January 2018

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Discovery of novel benzoxaborole-based potent antitrypanosomal agents

21 January 2018

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Discovery of novel orally bioavailable oxaborole 6-carboxamides that demonstrate cure in a murine model of late-stage central nervous system african trypanosomiasis

21 January 2018

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Potential new drugs for human African trypanosomiasis: some progress at last

21 January 2018

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Target assessment for antiparasitic drug discovery

21 January 2018

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Genomic-scale prioritization of drug targets: the TDR Targets database

21 January 2018

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Design, synthesis and trypanocidal activity of lead compounds based on inhibitors of parasite glycolysis

21 January 2018

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Selective irreversible inhibition of fructose 1,6-bisphosphate aldolase from Trypanosoma brucei

21 January 2018

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A target-based high throughput screen yields Trypanosoma brucei hexokinase small molecule inhibitors with antiparasitic activity

21 January 2018

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Aryl phosphoramidates of 5-phospho erythronohydroxamic acid, a new class of potent trypanocidal compounds

21 January 2018

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Investigation of trypanothione reductase as a drug target in Trypanosoma brucei

21 January 2018

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Chemical validation of trypanothione synthetase: a potential drug target for human trypanosomiasis

21 January 2018

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Selective delivery of 2-hydroxy APA to Trypanosoma brucei using the melamine motif

21 January 2018

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Targeted delivery of compounds to Trypanosoma brucei using the melamine motif

21 January 2018

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Targeting of toxic compounds to the trypanosome's interior

21 January 2018

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Discovery of potent and selective inhibitors of Trypanosoma brucei ornithine decarboxylase

21 January 2018

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Novel S-adenosylmethionine decarboxylase inhibitors for the treatment of human African trypanosomiasis

21 January 2018

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Validation of spermidine synthase as a drug target in African trypanosomes.

21 January 2018

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RNA interference-mediated silencing of ornithine decarboxylase and spermidine synthase genes in Trypanosoma brucei provides insight into regulation of polyamine biosynthesis

21 January 2018

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Thematic review series: lipid posttranslational modifications. Fighting parasitic disease by blocking protein farnesylation

21 January 2018

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Myristoyl-CoA:protein N-myristoyltransferase depletion in trypanosomes causes avirulence and endocytic defects.

21 January 2018

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N-myristoyltransferase inhibitors as new leads to treat sleeping sickness

21 January 2018

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Discovery of drug-like inhibitors of an essential RNA-editing ligase in Trypanosoma brucei

21 January 2018

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Glycogen synthase kinase 3 is a potential drug target for African trypanosomiasis therapy

21 January 2018

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Lipid metabolism in Trypanosoma brucei

21 January 2018

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Characterization of Trypanosoma brucei dihydroorotate dehydrogenase as a possible drug target; structural, kinetic and RNAi studies

21 January 2018

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Trypanosoma brucei pteridine reductase 1 is essential for survival in vitro and for virulence in mice

21 January 2018

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Post-translational import of protein into the endoplasmic reticulum of a trypanosome: an in vitro system for discovery of anti-trypanosomal chemical entities

21 January 2018

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Nuclear DBF-2-related kinases are essential regulators of cytokinesis in bloodstream stage Trypanosoma brucei

21 January 2018

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The Trypanosoma brucei cAMP phosphodiesterases TbrPDEB1 and TbrPDEB2: flagellar enzymes that are essential for parasite virulence

21 January 2018

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Development of protease inhibitors for protozoan infections

21 January 2018

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Discovery of trypanocidal compounds by whole cell HTS of Trypanosoma brucei

21 January 2018

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Identification of a κ-opioid agonist as a potent and selective lead for drug development against human African trypanosomiasis

21 January 2018

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Controlling sleeping sickness--"when will they ever learn?".

21 January 2018

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Eliminating human African trypanosomiasis: where do we stand and what comes next?

21 January 2018

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Controlling sleeping sickness - a review

21 January 2018

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21 January 2018

Identifiers

DOI

10.2217/FMB.11.44

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24 August 2017

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