Trypanocidal drugs: mechanisms, resistance and new targets

Eflornithine is a cost-effective alternative to melarsoprol for the treatment of second-stage human West African trypanosomiasis in Caxito, Angola

(2010) J. Robays et al.   TROPICAL MEDICINE & INTERNATIONAL HEALTH

Characterization of a gene encoding alcohol dehydrogenase in benznidazole-susceptible and -resistant populations of Trypanosoma cruzi

(2009) Fernanda M.F. Campos et al.   ACTA TROPICA

Trypanothione Reductase High-Throughput Screening Campaign Identifies Novel Classes of Inhibitors with Antiparasitic Activity

(2009) G. A. Holloway 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

Trypanocidal Activity of 8-Methyl-5'- Adenosine (Genz-644131), an Adenosylmethionine Decarboxylase Inhibitor

(2009) C. J. Bacchi et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

SAR studies on azasterols as potential anti-trypanosomal and anti-leishmanial agents

(2009) Federica Gigante et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Targeted delivery of compounds to Trypanosoma brucei using the melamine motif

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

Discovery of new S-adenosylmethionine decarboxylase inhibitors for the treatment of Human African Trypanosomiasis (HAT)

(2009) Bradford Hirth et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Privileged structure-guided synthesis of quinazoline derivatives as inhibitors of trypanothione reductase

(2009) Andrea Cavalli et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis and Evaluation of 1-(1-(Benzo[b]thiophen-2-yl)cyclohexyl)piperidine (BTCP) Analogues as Inhibitors of Trypanothione Reductase

(2009) Stephen Patterson et al.   ChemMedChem

Improved Tricyclic Inhibitors of Trypanothione Reductase by Screening and Chemical Synthesis

(2009) John L. Richardson 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

Vinyl Sulfones as Antiparasitic Agents and a Structural Basis for Drug Design

(2009) Iain D. Kerr et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Indomethacin Amides as a Novel Molecular Scaffold for TargetingTrypanosoma cruziSterol 14α-Demethylase

(2009) Mary E. Konkle et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structurally Simple Inhibitors of Lanosterol 14α-Demethylase Are Efficacious In a Rodent Model of Acute Chagas Disease

(2009) Praveen Kumar Suryadevara et al.   JOURNAL OF MEDICINAL CHEMISTRY

Rational Modification of a Candidate Cancer Drug for Use Against Chagas Disease

(2009) James M. Kraus et al.   JOURNAL OF MEDICINAL 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

Chagasic encephalitis in HIV patients: common presentation of an evolving epidemiological and clinical association

(2009) Carlos A DiazGranados et al.   LANCET INFECTIOUS DISEASES

Ergosterol biosynthesis and drug development for Chagas disease

(2009) Julio A Urbina   MEMORIAS DO INSTITUTO OSWALDO CRUZ

Two approaches to discovering and developing new drugs for Chagas disease

(2009) JH McKerrow et al.   MEMORIAS DO INSTITUTO OSWALDO CRUZ

Kinetoplastid papain-like cysteine peptidases

(2009) Conor R. Caffrey et al.   MOLECULAR AND BIOCHEMICAL PARASITOLOGY

The role of ATP-binding cassette (ABC) proteins in protozoan parasites

(2009) Virginie Sauvage et al.   MOLECULAR AND BIOCHEMICAL PARASITOLOGY

Comparative Molecular Docking of Antitrypanosomal Natural Products into Multiple Trypanosoma brucei Drug Targets

(2009) Ifedayo Ogungbe et al.   MOLECULES

Novel functionalized melamine-based nitroheterocycles: synthesis and activity against trypanosomatid parasites

(2009) Alessandro Baliani et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Trypanosoma cruzi CYP51 Inhibitor Derived from a Mycobacterium tuberculosis Screen Hit

(2009) Chiung-Kuang Chen et al.   PLoS Neglected Tropical Diseases

Differential gene expression in Trypanosoma cruzi populations susceptible and resistant to benznidazole

(2008) Silvane M.F. Murta et al.   ACTA TROPICA

Validation of spermidine synthase as a drug target in African trypanosomes

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

Structural and mechanistic insights into type II trypanosomatid tryparedoxin-dependent peroxidases

(2008) Magnus S. Alphey et al.   BIOCHEMICAL JOURNAL

Redox control in trypanosomatids, parasitic protozoa with trypanothione-based thiol metabolism

(2008) R. Luise Krauth-Siegel et al.   BIOCHIMICA ET BIOPHYSICA ACTA-GENERAL SUBJECTS

Antiparasitic compounds that target DNA

(2008) W. David Wilson et al.   BIOCHIMIE

Synthesis of macrocyclic trypanosomal cysteine protease inhibitors

(2008) Yen Ting Chen et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of trypanocidal thiosemicarbazone inhibitors of rhodesain and TbcatB

(2008) Jeremy P. Mallari et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Pentafluorosulfanyl as a Novel Building Block for Enzyme Inhibitors: Trypanothione Reductase Inhibition and Antiprotozoal Activities of Diarylamines

(2008) Bernhard Stump et al.   CHEMBIOCHEM

Insights into the redox biology of Trypanosoma cruzi: Trypanothione metabolism and oxidant detoxification

(2008) Florencia Irigoín et al.   FREE RADICAL BIOLOGY AND MEDICINE

Structural Basis for a Distinct Catalytic Mechanism inTrypanosoma bruceiTryparedoxin Peroxidase

(2008) Johannes Melchers et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Kinetoplastids: related protozoan pathogens, different diseases

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

Development of Potent Purine-Derived Nitrile Inhibitors of the Trypanosomal Protease TbcatB

(2008) Jeremy P. Mallari et al.   JOURNAL OF MEDICINAL CHEMISTRY

Proteomic Analysis of Trypanosoma cruzi Resistance to Benznidazole

(2008) Hélida M. Andrade et al.   JOURNAL OF PROTEOME RESEARCH

Benznidazole biotransformation in rat heart microsomal fraction without observable ultrastructural alterations: comparison to Nifurtimox-induced cardiac effects

(2008) María Montalto de Mecca et al.   MEMORIAS DO INSTITUTO OSWALDO CRUZ

Multiple NADPH–cytochrome P450 reductases from Trypanosoma cruzi

(2008) Patricio Portal et al.   MOLECULAR AND BIOCHEMICAL PARASITOLOGY

Drug-induced cure drives conversion to a stable and protective CD8+ T central memory response in chronic Chagas disease

(2008) Juan M Bustamante et al.   NATURE MEDICINE

Diaryl sulfide-based inhibitors of trypanothione reductase: inhibition potency, revised binding mode and antiprotozoal activities

(2008) Bernhard Stump et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

The history of African trypanosomiasis

(2008) Dietmar Steverding   Parasites & Vectors

Molecular characterization of cytosolic and mitochondrial tryparedoxin peroxidase in Trypanosoma cruzi populations susceptible and resistant to benznidazole

(2008) Fernanda B. Nogueira et al.   PARASITOLOGY RESEARCH

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

Effectiveness of melarsoprol and eflornithine as first-line regimens for gambiense sleeping sickness in nine Médecins Sans Frontières programmes

(2008) Manica Balasegaram et al.   TRANSACTIONS OF THE ROYAL SOCIETY OF TROPICAL MEDICINE AND HYGIENE

Ever-increasing complexities of diamidine and arsenical crossresistance in African trypanosomes

(2008) Harry P. de Koning   TRENDS IN PARASITOLOGY

RNA Interference of Trypanosoma brucei Cathepsin B and L Affects Disease Progression in a Mouse Model

(2008) Maha-Hamadien Abdulla et al.   PLoS Neglected Tropical Diseases

Regulated Expression of an Essential Allosteric Activator of Polyamine Biosynthesis in African Trypanosomes

(2008) Erin K. Willert et al.   PLoS Pathogens

Heteroallyl-containing 5-nitrofuranes as new anti-Trypanosoma cruzi agents with a dual mechanism of action

(2007) Alejandra Gerpe et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Trypanosoma cruzi: Characterisation of the gene encoding tyrosine aminotransferase in benznidazole-resistant and susceptible populations

(2007) Juciane V. Rego et al.   EXPERIMENTAL PARASITOLOGY