Search Results - "Ward, Stephen A"
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Artemisinin activity-based probes identify multiple molecular targets within the asexual stage of the malaria parasites Plasmodium falciparum 3D7
Published in Proceedings of the National Academy of Sciences - PNAS (23-02-2016)“…The artemisinin (ART)-based antimalarials have contributed significantly to reducing global malaria deaths over the past decade, but we still do not know how…”
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The molecular mechanism of action of artemisinin--the debate continues
Published in Molecules (12-03-2010)“…Despite international efforts to 'roll back malaria' the 2008 World Malaria Report revealed the disease still affects approximately 3 billion people in 109…”
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Antimalarial activity of primaquine operates via a two-step biochemical relay
Published in Nature communications (19-07-2019)“…Primaquine (PQ) is an essential antimalarial drug but despite being developed over 70 years ago, its mode of action is unclear. Here, we demonstrate that…”
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Anti-Wolbachia drug discovery and development: safe macrofilaricides for onchocerciasis and lymphatic filariasis
Published in Parasitology (01-01-2014)“…Anti-Wolbachia therapy delivers safe macrofilaricidal activity with superior therapeutic outcomes compared to all standard anti-filarial treatments, with the…”
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Rapid kill of malaria parasites by artemisinin and semi-synthetic endoperoxides involves ROS-dependent depolarization of the membrane potential
Published in Journal of antimicrobial chemotherapy (01-04-2014)“…Objectives Artemisinin and artemisinin semi-synthetic derivatives (collectively known as endoperoxides) are first-line antimalarials for the treatment of…”
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Antimalarial 4(1H)-pyridones bind to the Qi site of cytochrome bc1
Published in Proceedings of the National Academy of Sciences - PNAS (20-01-2015)“…Cytochrome bc1 is a proven drug target in the prevention and treatment of malaria. The rise in drug-resistant strains of Plasmodium falciparum, the organism…”
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M1 macrophage features in severe Plasmodium falciparum malaria patients with pulmonary oedema
Published in Malaria journal (15-05-2020)“…Pulmonary oedema (PE) is a serious complication of Plasmodium falciparum malaria which can lead to acute lung injury in severe cases. Lung macrophages are…”
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Industrial scale high-throughput screening delivers multiple fast acting macrofilaricides
Published in Nature communications (02-01-2019)“…Nematodes causing lymphatic filariasis and onchocerciasis rely on their bacterial endosymbiont, Wolbachia , for survival and fecundity, making Wolbachia a…”
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Generation of quinolone antimalarials targeting the Plasmodium falciparum mitochondrial respiratory chain for the treatment and prophylaxis of malaria
Published in Proceedings of the National Academy of Sciences - PNAS (22-05-2012)“…There is an urgent need for new antimalarial drugs with novel mechanisms of action to deliver effective control and eradication programs. Parasite resistance…”
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Short-Course, High-Dose Rifampicin Achieves Wolbachia Depletion Predictive of Curative Outcomes in Preclinical Models of Lymphatic Filariasis and Onchocerciasis
Published in Scientific reports (16-03-2017)“…Lymphatic filariasis (LF) and onchocerciasis are priority neglected tropical diseases targeted for elimination. The only safe drug treatment with substantial…”
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Pharmacokinetic-Pharmacodynamic modelling of intracellular Mycobacterium tuberculosis growth and kill rates is predictive of clinical treatment duration
Published in Scientific reports (29-03-2017)“…Tuberculosis (TB) treatment is long and complex, typically involving a combination of drugs taken for 6 months. Improved drug regimens to shorten and simplify…”
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Identification of a 1,2,4,5-Tetraoxane Antimalarial Drug-Development Candidate (RKA 182) with Superior Properties to the Semisynthetic Artemisinins
Published in Angewandte Chemie (International ed.) (02-08-2010)“…Fighting drug resistence: From a library of over 150 1,2,4,5‐tetraoxanes, the candidate RKA 182 was selected for preclinical development as an antimalarial…”
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Cytochrome b Mutation Y268S Conferring Atovaquone Resistance Phenotype in Malaria Parasite Results in Reduced Parasite bc1 Catalytic Turnover and Protein Expression
Published in The Journal of biological chemistry (23-03-2012)“…Atovaquone is an anti-malarial drug used in combination with proguanil (e.g. MalaroneTM) for the curative and prophylactic treatment of malaria. Atovaquone, a…”
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Identification, Design and Biological Evaluation of Bisaryl Quinolones Targeting Plasmodium falciparum Type II NADH:Quinone Oxidoreductase (PfNDH2)
Published in Journal of medicinal chemistry (08-03-2012)“…A program was undertaken to identify hit compounds against NADH:ubiquinone oxidoreductase (PfNDH2), a dehydrogenase of the mitochondrial electron transport…”
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In vivo kinetics of Wolbachia depletion by ABBV-4083 in L. sigmodontis adult worms and microfilariae
Published in PLoS neglected tropical diseases (01-08-2019)“…Depletion of Wolbachia endosymbionts of human pathogenic filariae using 4-6 weeks of doxycycline treatment can lead to permanent sterilization and adult…”
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Discovery of ABBV-4083, a novel analog of Tylosin A that has potent anti-Wolbachia and anti-filarial activity
Published in PLoS neglected tropical diseases (01-02-2019)“…There is a significant need for improved treatments for onchocerciasis and lymphatic filariasis, diseases caused by filarial worm infection. In particular, an…”
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Antimalarial drugs and pregnancy: safety, pharmacokinetics, and pharmacovigilance
Published in The Lancet infectious diseases (01-02-2007)“…Summary Before a recommendation for antimalarial drug use in pregnancy is made, it is essential that we understand the potential risks involved and have…”
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Short-course, oral flubendazole does not mediate significant efficacy against Onchocerca adult male worms or Brugia microfilariae in murine infection models
Published in PLoS neglected tropical diseases (01-01-2019)“…The Onchocerca ochengi adult implant and Brugia malayi microfilariemic Severe-Combined Immunodeficient (SCID) mouse models are validated screens to measure…”
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Targeting the Ubiquinol-Reduction (Qi) Site of the Mitochondrial Cytochrome bc1 Complex for the Development of Next Generation Quinolone Antimalarials
Published in Biology (Basel, Switzerland) (25-07-2022)“…Antimalarials targeting the ubiquinol-oxidation (Qo) site of the Plasmodium falciparum bc1 complex, such as atovaquone, have become less effective due to the…”
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Pharmacokinetics of Rifampin in Peruvian Tuberculosis Patients with and without Comorbid Diabetes or HIV
Published in Antimicrobial Agents and Chemotherapy (01-05-2012)“…For drug-compliant patients, poor responses to tuberculosis (TB) treatment might be attributable to subtherapeutic drug concentrations. An impaired absorption…”
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