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Mutations in the P. falciparum digestive vacuole transmembrane protein PfCRT and evidence for their role in chloroquine resistance.
Antimalarial drug discovery: efficacy models for compound screening
- D. Fidock, P. Rosenthal, S. Croft, R. Brun, S. Nwaka
- Biology, MedicineNature Reviews Drug Discovery
- 1 June 2004
Different in vitro and in vivo screens for antimalarial drug discovery are suggested and a streamlined process for evaluating new compounds on the path from drug discovery to development is recommended.
Malaria: progress, perils, and prospects for eradication.
Insights into parasite biology, human immunity, and vector behavior will guide efforts to translate parasite and mosquito genome sequences into novel interventions, including drugs, vaccines, and insecticides.
Transformation with human dihydrofolate reductase renders malaria parasites insensitive to WR99210 but does not affect the intrinsic activity of proguanil.
- D. Fidock, T. Wellems
- Biology, MedicineProceedings of the National Academy of Sciences…
- 30 September 1997
It is demonstrated that the only significant action of WR99210 is against parasite DHFR, and the transformation system described here has the advantage that P. falciparum drug-resistant lines are uniformly sensitive to methotrexate, which provides an approach for screening and identifying novel DHFR inhibitors that will be important in combined chemotherapeutic formulations against malaria.
Chloroquine Resistance in Plasmodium falciparum Malaria Parasites Conferred by pfcrt Mutations
It is provided conclusive evidence that mutant haplotypes of the pfcrt gene product of Asian, African, or South American origin confer chloroquine resistance with characteristic verapamil reversibility and reduced chlorquine accumulation.
K13-propeller mutations confer artemisinin resistance in Plasmodium falciparum clinical isolates
The data provide a conclusive rationale for worldwide K13-propeller sequencing to identify and eliminate artemisinin-resistant parasites and imperils efforts to reduce the global malaria burden.
Spiroindolones, a Potent Compound Class for the Treatment of Malaria
The preclinical profile for an optimized spiroindolone drug candidate, NITD609, shows pharmacokinetic properties compatible with once-daily oral dosing and has single-dose efficacy in a rodent malaria model.
pfmdr1 mutations contribute to quinine resistance and enhance mefloquine and artemisinin sensitivity in Plasmodium falciparum
The hypothesis that pfmdr1 3′ point mutations can significantly affect parasite susceptibility to a wide range of antimalarial drug susceptibility in a strain‐specific manner that depends on the parasite genetic background is supported.
Efficient site-specific integration in Plasmodium falciparum chromosomes mediated by mycobacteriophage Bxb1 integrase
An efficient, site-specific system of genetic integration into Plasmodium falciparum malaria parasite chromosomes mediated by mycobacteriophage Bxb1 integrase is reported, which illustrates the utility of Bxa1-based integrative recombination for genetic studies of intracellular eukaryotic organisms.
Evolution of a unique Plasmodium falciparum chloroquine-resistance phenotype in association with pfcrt polymorphism in Papua New Guinea and South America
- R. Mehlotra, H. Fujioka, P. Zimmerman
- BiologyProceedings of the National Academy of Sciences…
- 23 October 2001
A key role for pH-dependent changes in hematin receptor concentration in the P. falciparum CQR mechanism is suggested to have arisen through multiple evolutionary pathways associated with pfcrt K76T, and a previously undescribed C QR phenotype is found to be associated with the SVMNT haplotype from PNG and South America.