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Antimalarial drug discovery: progress and approaches
Recent antimalarial drug discovery has been a race to produce new medicines that
overcome emerging drug resistance, whilst considering safety and improving dosing …
overcome emerging drug resistance, whilst considering safety and improving dosing …
[HTML][HTML] MalDA, accelerating malaria drug discovery
The Malaria Drug Accelerator (MalDA) is a consortium of 15 leading scientific laboratories.
The aim of MalDA is to improve and accelerate the early antimalarial drug discovery process …
The aim of MalDA is to improve and accelerate the early antimalarial drug discovery process …
The anticancer human mTOR inhibitor sapanisertib potently inhibits multiple Plasmodium kinases and life cycle stages
Compounds acting on multiple targets are critical to combating antimalarial drug resistance.
Here, we report that the human “mammalian target of rapamycin”(mTOR) inhibitor …
Here, we report that the human “mammalian target of rapamycin”(mTOR) inhibitor …
Towards next-generation treatment options to combat Plasmodium falciparum malaria
Malaria, which is caused by infection of red blood cells with Plasmodium parasites, can be
fatal in non-immune individuals if left untreated. The recent approval of the pre-erythrocytic …
fatal in non-immune individuals if left untreated. The recent approval of the pre-erythrocytic …
Discovery and characterization of potent, efficacious, orally available antimalarial plasmepsin X inhibitors and preclinical safety assessment of UCB7362
MA Lowe, A Cardenas, JP Valentin, Z Zhu… - Journal of medicinal …, 2022 - ACS Publications
Plasmepsin X (PMX) is an essential aspartyl protease controlling malaria parasite egress
and invasion of erythrocytes, development of functional liver merozoites (prophylactic …
and invasion of erythrocytes, development of functional liver merozoites (prophylactic …
Ca2+ signals critical for egress and gametogenesis in malaria parasites depend on a multipass membrane protein that interacts with PKG
Calcium signaling regulated by the cGMP-dependent protein kinase (PKG) controls key life
cycle transitions in the malaria parasite. However, how calcium is mobilized from …
cycle transitions in the malaria parasite. However, how calcium is mobilized from …
The antimalarial MMV688533 provides potential for single-dose cures with a high barrier to Plasmodium falciparum parasite resistance
JM Murithi, C Pascal, J Bath, X Boulenc… - Science translational …, 2021 - science.org
The emergence and spread of Plasmodium falciparum resistance to first-line antimalarials
creates an imperative to identify and develop potent preclinical candidates with distinct …
creates an imperative to identify and develop potent preclinical candidates with distinct …
Plasmodium Egress Across the Parasite Life Cycle
Human malaria, caused by infection with Plasmodium parasites, remains one of the most
important global public health problems, with the World Health Organization reporting more …
important global public health problems, with the World Health Organization reporting more …
Cytoplasmic isoleucyl tRNA synthetase as an attractive multistage antimalarial drug target
ES Istvan, F Guerra, M Abraham, KS Huang… - Science translational …, 2023 - science.org
Development of antimalarial compounds into clinical candidates remains costly and arduous
without detailed knowledge of the target. As resistance increases and treatment options at …
without detailed knowledge of the target. As resistance increases and treatment options at …
Systematic in vitro evolution in Plasmodium falciparum reveals key determinants of drug resistance
Surveillance of drug resistance and the discovery of novel targets—key objectives in the
fight against malaria—rely on identifying resistance-conferring mutations in Plasmodium …
fight against malaria—rely on identifying resistance-conferring mutations in Plasmodium …