Development of novel drugs for human African trypanosomiasis

Nifurtimox Activation by Trypanosomal Type I Nitroreductases Generates Cytotoxic Nitrile Metabolites

(2011) Belinda S. Hall et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Discovery of Novel Orally Bioavailable Oxaborole 6-Carboxamides That Demonstrate Cure in a Murine Model of Late-Stage Central Nervous System African Trypanosomiasis

(2010) B. Nare et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Cross-Resistance to Nitro Drugs and Implications for Treatment of Human African Trypanosomiasis

(2010) A. Y. Sokolova et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

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

(2010) Deuan C. Jones et al.   BIOCHEMICAL PHARMACOLOGY

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

(2010) Nina Klee et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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

(2010) Michael P Barrett   CURRENT OPINION IN INFECTIOUS DISEASES

Discovery of Potent and Selective Inhibitors ofTrypanosoma bruceiOrnithine Decarboxylase

(2010) David C. Smithson et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Nuclear DBF-2-related Kinases Are Essential Regulators of Cytokinesis in Bloodstream StageTrypanosoma brucei

(2010) Jiangtao Ma et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Aryl Phosphoramidates of 5-Phospho Erythronohydroxamic Acid, A New Class of Potent Trypanocidal Compounds

(2010) Gian Filippo Ruda et al.   JOURNAL OF MEDICINAL CHEMISTRY

Lipid metabolism in Trypanosoma brucei

(2010) Terry K. Smith et al.   MOLECULAR AND BIOCHEMICAL PARASITOLOGY

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

(2010) Nicola Baker et al.   MOLECULAR AND BIOCHEMICAL PARASITOLOGY

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

(2010) Gabriela Schumann Burkard et al.   MOLECULAR AND BIOCHEMICAL PARASITOLOGY

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

(2010) Natasha Sienkiewicz et al.   MOLECULAR MICROBIOLOGY

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

(2010) Benoit Vanhollebeke et al.   MOLECULAR MICROBIOLOGY

N-myristoyltransferase inhibitors as new leads to treat sleeping sickness

(2010) Julie A. Frearson et al.   NATURE

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

(2010) R. Kieft et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Discovery of Novel Benzoxaborole-Based Potent Antitrypanosomal Agents

(2010) Dazhong Ding et al.   ACS Medicinal Chemistry Letters

Controlling Sleeping Sickness—“When Will They Ever Learn?”

(2010) David Molyneux et al.   PLoS Neglected Tropical Diseases

A Target-Based High Throughput Screen Yields Trypanosoma brucei Hexokinase Small Molecule Inhibitors with Antiparasitic Activity

(2010) Elizabeth R. Sharlow et al.   PLoS Neglected Tropical Diseases

Fexinidazole – A New Oral Nitroimidazole Drug Candidate Entering Clinical Development for the Treatment of Sleeping Sickness

(2010) Els Torreele et al.   PLoS Neglected Tropical Diseases

A Molecular Mechanism for Eflornithine Resistance in African Trypanosomes

(2010) Isabel M. Vincent et al.   PLoS Pathogens

New Treatment Option for Second-Stage African Sleeping Sickness: In Vitro and In Vivo Efficacy of Aza Analogs of DB289

(2009) T. Wenzler et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Novel S-Adenosylmethionine Decarboxylase Inhibitors for the Treatment of Human African Trypanosomiasis

(2009) R. H. Barker et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Post-translational import of protein into the endoplasmic reticulum of a trypanosome: anin vitrosystem for discovery of anti-trypanosomal chemical entities

(2009) Bhargavi Patham et al.   BIOCHEMICAL JOURNAL

Targeted delivery of compounds to Trypanosoma brucei using the melamine motif

(2009) Constance Chollet et al.   BIOORGANIC & MEDICINAL CHEMISTRY

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

(2009) Liam J. Morrison et al.   CELLULAR MICROBIOLOGY

Investigation of Trypanothione Reductase as a Drug Target inTrypanosoma brucei

(2009) Daniel Spinks et al.   ChemMedChem

RNA Interference-Mediated Silencing of Ornithine Decarboxylase and Spermidine Synthase Genes inTrypanosoma bruceiProvides Insight into Regulation of Polyamine Biosynthesis

(2009) Yanjing Xiao et al.   EUKARYOTIC CELL

Chemical Validation of Trypanothione Synthetase

(2009) Leah S. Torrie et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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

(2009) L. Sanderson et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

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

(2009) Gerardo Priotto et al.   LANCET

Human African trypanosomiasis

(2009) Reto Brun et al.   LANCET

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

(2009) Helen P. Price et al.   MOLECULAR AND BIOCHEMICAL PARASITOLOGY

Controlling sleeping sickness – a review

(2009) S. C. WELBURN et al.   PARASITOLOGY

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

(2008) R. E. Mdachi et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Glycogen Synthase Kinase 3 Is a Potential Drug Target for African Trypanosomiasis Therapy

(2008) K. K. Ojo et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Validation of spermidine synthase as a drug target in African trypanosomes

(2008) Martin C. Taylor et al.   BIOCHEMICAL JOURNAL

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

(2008) Matthew W. Nowicki et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Development of protease inhibitors for protozoan infections

(2008) James H McKerrow et al.   CURRENT OPINION IN INFECTIOUS DISEASES

Transport of Dicationic Drugs Pentamidine and Furamidine by Human Organic Cation Transporters

(2008) X. Ming et al.   DRUG METABOLISM AND DISPOSITION

Kinetoplastids: related protozoan pathogens, different diseases

(2008) Ken Stuart et al.   JOURNAL OF CLINICAL INVESTIGATION

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

(2008) Tracy L. Arakaki et al.   MOLECULAR MICROBIOLOGY

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

(2008) Fernán Agüero et al.   NATURE REVIEWS DRUG DISCOVERY

The history of African trypanosomiasis

(2008) Dietmar Steverding   Parasites & Vectors

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

(2008) R. E. Amaro et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

(2008) Shane R. Wilkinson et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Eliminating Human African Trypanosomiasis: Where Do We Stand and What Comes Next?

(2008) Pere P Simarro et al.   PLOS MEDICINE

The Natural Progression of Gambiense Sleeping Sickness: What Is the Evidence?

(2008) Francesco Checchi et al.   PLoS Neglected Tropical Diseases