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Medroxyprogesterone acetate, unlike norethisterone, increases HIV-1 replication in human peripheral blood mononuclear cells and an indicator cell line, via mechanisms involving the glucocorticoid
TLDR
It is shown for the first time that MPA, unlike NET, significantly increases HIV-1 replication in peripheral blood mononuclear cells (PBMCs) and a cervical cell line model, and offers strong support for different biological mechanisms for MPA versus NET, due to their differential GR activity.
Chemical Proteomics and Super-resolution Imaging Reveal That Chloroquine Interacts with Plasmodium falciparum Multidrug Resistance-Associated Protein and Lipids.
TLDR
This work demonstrated pull-down of PfMRP1 by matrices labeled with Cinchona alkaloids quinine and quinidine, the first time that these drugs have been found to bind directly to this protein.
Shining new light on ancient drugs: preparation and subcellular localisation of novel fluorescent analogues of Cinchona alkaloids in intraerythrocytic Plasmodium falciparum.
TLDR
Quantitative analysis revealed minimal accumulation within the nucleus, rejecting the disruption of DNA replication as a possible mode of action and extensive localisation to phospholipid structures and associated organelles was observed, but the analogues did not show evidence of association with neutral lipid bodies.
Reciprocal Modulation of Antiretroviral Drug and Steroid Receptor Function In Vitro
TLDR
The ability of TDF and DPV to influence GR and PR activity suggests that their use may be associated with steroid receptor-mediated off-target effects, and raises concerns that reciprocal modulation may cause side effects in a cell- and donor-specific manner in vivo.
Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite Plasmodium falciparum and Optimization Efforts.
TLDR
A novel diazaspiro[3.4]octane series was identified from a Plasmodium falciparum whole-cell high-throughput screening campaign and led to the identification of compounds that showed low nanomolar asexual blood-stage activity together with strong gametocyte sterilizing properties that translated to transmission-blocking activity in the standard membrane feeding assay.
Quinine fever
TLDR
The tumultuous history of quinine is retrace from a medicine — used as a tool for colonialism — to a puzzling chemical target, a fluorescence standard and a key ingredient in popular drinks.
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