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A novel multiple-stage antimalarial agent that inhibits protein synthesis
There is an urgent need for new drugs to treat malaria, with broad therapeutic potential and novel modes of action, to widen the scope of treatment and to overcome emerging drug resistance. Here weExpand
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Development of a Novel Lead that Targets M. tuberculosis Polyketide Synthase 13
Summary Widespread resistance to first-line TB drugs is a major problem that will likely only be resolved through the development of new drugs with novel mechanisms of action. We have usedExpand
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Identification of Morpholino Thiophenes as Novel Mycobacterium tuberculosis Inhibitors, Targeting QcrB
With the emergence of multidrug-resistant strains of Mycobacterium tuberculosis there is a pressing need for new oral drugs with novel mechanisms of action. Herein, we describe the identification ofExpand
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Discovery of β2 Adrenergic Receptor Ligands Using Biosensor Fragment Screening of Tagged Wild-Type Receptor
G-protein coupled receptors (GPCRs) are the primary target class of currently marketed drugs, accounting for about a quarter of all drug targets of approved medicines. However, almost all theExpand
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Discovery of a Quinoline-4-carboxamide Derivative with a Novel Mechanism of Action, Multistage Antimalarial Activity, and Potent in Vivo Efficacy
The antiplasmodial activity, DMPK properties, and efficacy of a series of quinoline-4-carboxamides are described. This series was identified from a phenotypic screen against the blood stage ofExpand
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Preclinical candidate for the treatment of visceral leishmaniasis that acts through proteasome inhibition
Significance Safer and more effective oral drugs are urgently required to treat visceral leishmaniasis (VL), a neglected parasitic disease that kills 20,000–40,000 people each year in parts of Asia,Expand
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Lysyl-tRNA synthetase as a drug target in malaria and cryptosporidiosis
Significance Malaria and cryptosporidiosis are major burdens to both global health and economic development in many countries. Malaria caused >400,000 deaths in 2017, and cryptosporidiosis isExpand
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Effect of immunization on herpes simplex virus type 1 latent infection in the trigeminal ganglion
Purpose. To quantify and characterize immune protection from herpes simplex virus (HSV) latent infection in mice following corneal challenge. Methods. Mice immunized or mock-immunized and boosted inExpand
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Re-evaluating pretomanid analogues for Chagas disease: Hit-to-lead studies reveal both in vitro and in vivo trypanocidal efficacy.
Phenotypic screening of a 900 compound library of antitubercular nitroimidazole derivatives related to pretomanid against the protozoan parasite Trypanosoma cruzi (the causative agent for ChagasExpand
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Identification of Trypanocidal Activity for Known Clinical Compounds Using a New Trypanosoma cruzi Hit-Discovery Screening Cascade
Chagas disease is a significant health problem in Latin America and the available treatments have significant issues in terms of toxicity and efficacy. There is thus an urgent need to develop newExpand
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