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Plasmodium

  • Atypical Molecular Basis for Drug Resistance to Mitochondrial Function Inhibitors in <span class="named-content genus-species" id="named-content-1">Plasmodium falciparum</span>
    Mechanisms of Resistance
    Atypical Molecular Basis for Drug Resistance to Mitochondrial Function Inhibitors in Plasmodium falciparum

    The continued emergence of drug-resistant Plasmodium falciparum parasites hinders global attempts to eradicate malaria, emphasizing the need to identify new antimalarial drugs. Attractive targets for chemotherapeutic intervention are the cytochrome (cyt) bc1 complex, which is an essential component of the mitochondrial electron transport chain (...

    Heather J. Painter, Joanne M. Morrisey, Michael W. Mather, Lindsey M. Orchard, Cuyler Luck, Martin J. Smilkstein, Michael K. Riscoe, Akhil B. Vaidya, Manuel Llinás
  • Inhibition of PfMYST Histone Acetyltransferase Activity Blocks <span class="named-content genus-species" id="named-content-1">Plasmodium falciparum</span> Growth and Survival
    Mechanisms of Action: Physiological Effects
    Inhibition of PfMYST Histone Acetyltransferase Activity Blocks Plasmodium falciparum Growth and Survival

    One of the major barriers in the prevention and control of malaria programs worldwide is the growing emergence of multidrug resistance in Plasmodium parasites, and this necessitates continued efforts to discover and develop effective drug molecules targeting novel proteins essential for parasite survival. In recent years, epigenetic regulators have evolved as an attractive drug target option owing to their crucial role in...

    Utsav Sen, Akshaykumar Nayak, Juhi Khurana, Deepu Sharma, Ashish Gupta
  • Open Access
    Safety, Pharmacokinetics, and Activity of High-Dose Ivermectin and Chloroquine against the Liver Stage of <span class="named-content genus-species" id="named-content-1">Plasmodium cynomolgi</span> Infection in Rhesus Macaques
    Pharmacology
    Safety, Pharmacokinetics, and Activity of High-Dose Ivermectin and Chloroquine against the Liver Stage of Plasmodium cynomolgi Infection in Rhesus Macaques

    Previously, ivermectin (1 to 10 mg/kg of body weight) was shown to inhibit the liver-stage development of Plasmodium berghei in orally dosed mice. Here, ivermectin showed inhibition of the in vitro development of Plasmodium cynomolgi schizonts (50% inhibitory concentration [IC50...

    Pattaraporn Vanachayangkul, Rawiwan Im-erbsin, Anchalee Tungtaeng, Chanikarn Kodchakorn, Alison Roth, John Adams, Chaiyaporn Chaisatit, Piyaporn Saingam, Richard J. Sciotti, Gregory A. Reichard, Christina K. Nolan, Brandon S. Pybus, Chad C. Black, Luis A. Lugo-Roman, Matthew D. Wegner, Philip L. Smith, Mariusz Wojnarski, Brian A. Vesely, Kevin C. Kobylinski
  • Evaluation of 4-Amino 2-Anilinoquinazolines against <em>Plasmodium</em> and Other Apicomplexan Parasites <em>In Vitro</em> and in a <em>P. falciparum</em> Humanized NOD-<em>scid</em> IL2Rγ<sup>null</sup> Mouse Model of Malaria
    Experimental Therapeutics
    Evaluation of 4-Amino 2-Anilinoquinazolines against Plasmodium and Other Apicomplexan Parasites In Vitro and in a P. falciparum Humanized NOD-scid IL2Rγnull Mouse Model of Malaria

    A series of 4-amino 2-anilinoquinazolines optimized for activity against the most lethal malaria parasite of humans, Plasmodium falciparum, was evaluated for activity against other human Plasmodium parasites and related apicomplexans that infect humans and animals. Four of the most promising compounds from the 4-amino 2-anilinoquinazoline series were equally...

    Paul R. Gilson, William Nguyen, William A. Poole, Jose E. Teixeira, Jennifer K. Thompson, Kaiyuan Guo, Rebecca J. Stewart, Trent D. Ashton, Karen L. White, Laura M. Sanz, Francisco-Javier Gamo, Susan A. Charman, Sergio Wittlin, James Duffy, Christopher J. Tonkin, Wai-Hong Tham, Brendan S. Crabb, Brian M. Cooke, Christopher D. Huston, Alan F. Cowman, Brad E. Sleebs
  • Experimental Therapeutics
    Identification of Hsp90 Inhibitors with Anti-Plasmodium Activity
    Dora Posfai, Amber L. Eubanks, Allison I. Keim, Kuan-Yi Lu, Grace Z. Wang, Philip F. Hughes, Nobutaka Kato, Timothy A. Haystead, Emily R. Derbyshire
  • Experimental Therapeutics
    Characterization of Plasmodium Atg3-Atg8 Interaction Inhibitors Identifies Novel Alternative Mechanisms of Action in Toxoplasma gondii
    Joseph M. Varberg, Kaice A. LaFavers, Gustavo Arrizabalaga, William J. Sullivan
  • Open Access
    Susceptibility
    Screening the Medicines for Malaria Venture Pathogen Box across Multiple Pathogens Reclassifies Starting Points for Open-Source Drug Discovery
    Sandra Duffy, Melissa L. Sykes, Amy J. Jones, Todd B. Shelper, Moana Simpson, Rebecca Lang, Sally-Ann Poulsen, Brad E. Sleebs, Vicky M. Avery
  • Pharmacology
    High Accumulation and In Vivo Recycling of the New Antimalarial Albitiazolium Lead to Rapid Parasite Death
    Sharon Wein, Nicolas Taudon, Marjorie Maynadier, Christophe Tran Van Ba, Delphine Margout, Yann Bordat, Laurent Fraisse, Kai Wengelnik, Rachel Cerdan, Françoise Bressolle-Gomeni, Henri J. Vial
  • Open Access
    Experimental Therapeutics
    Inhibition of Plasmodium Liver Infection by Ivermectin
    António M. Mendes, Inês S. Albuquerque, Marta Machado, Joana Pissarra, Patrícia Meireles, Miguel Prudêncio
  • Experimental Therapeutics
    In Vitro and In Vivo Properties of Ellagic Acid in Malaria Treatment
    Patrice Njomnang Soh, Benoît Witkowski, David Olagnier, Marie-Laure Nicolau, Maria-Concepcion Garcia-Alvarez, Antoine Berry, Françoise Benoit-Vical

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