Chlorpheniramine Analogues Reverse Chloroquine Resistance in Plasmodium falciparum by Inhibiting PfCRT
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چکیده
منابع مشابه
RESISTANCE OF PLASMODIUM FALCIPARUM TO CHLOROQUINE IN SOUTH EASTERN IRAN
In vivo and in vitro assessments of the response of P. falciparum to chloroquine using WHO standard kits and techniques were carried out in I ran Shahr, Sistan and Baluchestan province of Iran in 1985. In the in vivo assessment, 24 malaria patients treated with chloroquine (25mg/kg over three days) were followed up for one to four weeks. The mean parasite clearance time was 4.3 days and in...
متن کاملChloroquine resistance in Plasmodium falciparum malaria parasites conferred by pfcrt mutations.
Plasmodium falciparum chloroquine resistance is a major cause of worldwide increases in malaria mortality and morbidity. Recent laboratory and clinical studies have associated chloroquine resistance with point mutations in the gene pfcrt. However, direct proof of a causal relationship has remained elusive and most models have posited a multigenic basis of resistance. Here, we provide conclusive...
متن کاملNew haplotypes of the Plasmodium falciparum chloroquine resistance transporter (pfcrt) gene among chloroquine-resistant parasite isolates.
Mutations in the Plasmodium falciparum chloroquine resistance transporter (pfcrt) gene were examined to assess their associations with chloroquine resistance in clinical samples from Armopa (Papua) and Papua New Guinea. In Papua, two of the five pfcrt haplotypes found were new: SVIET from Armopa and CVIKT from an isolate in Timika. There was also a strong association (P < 0.0001) between the pf...
متن کاملA critical role for PfCRT K76T in Plasmodium falciparum verapamil-reversible chloroquine resistance.
Chloroquine resistance (CQR) in Plasmodium falciparum is associated with mutations in the digestive vacuole transmembrane protein PfCRT. However, the contribution of individual pfcrt mutations has not been clarified and other genes have been postulated to play a substantial role. Using allelic exchange, we show that removal of the single PfCRT amino-acid change K76T from resistant strains leads...
متن کاملFunctional Characterization of the Plasmodium falciparum Chloroquine-Resistance Transporter (PfCRT) in Transformed Dictyostelium discoideum Vesicles
BACKGROUND Chloroquine (CQ)-resistant Plasmodium falciparum malaria has been a global health catastrophe, yet much about the CQ resistance (CQR) mechanism remains unclear. Hallmarks of the CQR phenotype include reduced accumulation of protonated CQ as a weak base in the digestive vacuole of the erythrocyte-stage parasite, and chemosensitization of CQ-resistant (but not CQ-sensitive) P. falcipar...
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ژورنال
عنوان ژورنال: ACS Medicinal Chemistry Letters
سال: 2014
ISSN: 1948-5875,1948-5875
DOI: 10.1021/ml5000228