Fast-killing tyrosine amide ((<em>S</em>)-SW228703) with blood- and liver-stage antimalarial activity associated with the cyclic amine resistance... (Publications)
Current malaria treatments are threatened by drug resistance, and new drugs are urgently needed. In a phenotypic screen for new antimalarials, we identified (S)-SW228703 ((S)-SW703), a tyrosine amide with [...] fast-killing mechanism of action, available for lead optimization to generate new treatments for malaria.
Molecular surveillance of the antifolateresistant mutation I164L in imported African isolates of <em>Plasmodium falciparum</em> in Europe: sentinel... (Publications)
BACKGROUND: Malaria parasites that carry the DHFR-mutation I164L are not only highly resistant to sulfadoxine-pyrimethamine but also to the new antimalarial drug chlorproguanil-dapsone. The spread of this [...] network for the surveillance of travel-associated diseases and seems to cover approximately 12% of all malaria cases imported into Europe. Within this network we screened 277 imported African isolates of P.
Activities of quinoxaline, nitroquinoxaline and [1,2,4]triazolo[4,3-a]quinoxaline analogs of MMV007204 against <em>Schistosoma mansoni</em> (Publications)
Recently, an antimalarial quinoxaline derivative (MMV007204) from the Medicines for Malaria Venture (MMV) Malaria Box demonstrated promise against Schistosoma mansoni In this study, 47 synthesized compounds
Molecular surveillance of the antifolateresistant mutation I164L in imported African isolates of <em>Plasmodium falciparum</em> in Europe: sentinel... (Publications)
BACKGROUND: Malaria parasites that carry the DHFR-mutation I164L are not only highly resistant to sulfadoxine-pyrimethamine but also to the new antimalarial drug chlorproguanil-dapsone. The spread of this [...] network for the surveillance of travel-associated diseases and seems to cover approximately 12% of all malaria cases imported into Europe. Within this network we screened 277 imported African isolates of P.
A simple and efficient tool for trapping gravid <em>Anopheles</em> at breeding sites (Publications)
BACKGROUND: No effective tool currently exists for trapping ovipositing malaria vectors. This creates a gap in our ability to investigate the behavior and ecology of gravid Anopheles. FINDINGS: Here we [...] ecology of gravid female Anophelines. It strongly implies that at least two of the major vectors of malaria in Africa land on the water surface during the oviposition process, and demonstrates that Anophelines
Fast-killing tyrosine amide ((<em>S</em>)-SW228703) with blood- and liver-stage antimalarial activity associated with the cyclic amine resistance... (Publications)
Current malaria treatments are threatened by drug resistance, and new drugs are urgently needed. In a phenotypic screen for new antimalarials, we identified (S)-SW228703 ((S)-SW703), a tyrosine amide with [...] fast-killing mechanism of action, available for lead optimization to generate new treatments for malaria.
Addressing the intracellular vestibule of the plasmodial lactate transporter PfFNT by p-substituted inhibitors amplifies in vitro activity (Publications)
Inhibition of the lactate transporter PfFNT is a valid novel mode of action against malaria parasites. Current pyridine-substituted pentafluoro-3-hydroxy-pent-2-en-1-ones act as substrate analogs with [...] metabolized, the more stable p-acetanilide cleared 99.7% of parasites at 4 × 50 mg kg(-1) in a mouse malaria model. Future stabilization of the p-substitution against metabolism may translate the gain in in
Multiplexed ddPCR-amplicon sequencing reveals isolated <em>Plasmodium falciparum</em> populations amenable to local elimination in Zanzibar, Tanzania (Publications)
Zanzibar has made significant progress toward malaria elimination, but recent stagnation requires novel approaches. We developed a highly multiplexed droplet digital PCR (ddPCR)-based amplicon sequencing [...] genetic structure across the Zanzibar archipelago and provides actionable insights for prioritizing malaria elimination efforts.
The catalytic subunit of <em>Plasmodium falciparum</em> casein kinase 2 is essential for gametocytogenesis (Publications)
pleiotropic kinase phosphorylating substrates in different cellular compartments in eukaryotes. In the malaria parasite Plasmodium falciparum, PfCK2 is vital for asexual proliferation of blood-stage parasites [...] PfCK2alpha catalytic subunit in gametocytes, the sexual forms of the parasite that are essential for malaria transmission. We show that PfCK2alpha localizes to the nucleus and cytoplasm in asexual and sexual
Structure-activity relationships and antiplasmodial potencies of novel 3,4-disubstituted 1,2,5-oxadiazoles (Publications)
The 4-substituted 3-amino-1,2,5-oxadiazole 1 from the Malaria Box Project of the Medicines for Malaria Venture foundation shows very promising selectivity and in vitro activity against Plasmodium falciparum