Kinetic modelling of the response of Plasmodium falciparum to chloroquine and its experimental testing in vitro: Implications for mechanism of action of and resistance to the drug
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Cited by (75)
The Plasmodium falciparum ABC transporter ABCI3 confers parasite strain-dependent pleiotropic antimalarial drug resistance
2022, Cell Chemical BiologyCitation Excerpt :In contrast, the ABCI3 CNV line had a markedly different profile against 1, suggesting a difference in this compound's cellular accumulation in the presence of three copies of ABCI3 (Figure 5B). We extrapolated the linear relationship between the inoculum size and the measured IC50 for CQ and 1 to determine the absolute IC50, which was then used to calculate the CAR as previously defined (Figure 5C) (Geary et al., 1990). CAR results predicted that CQ accumulated ∼1- to 2-fold more in 3D7-A10 and the L690I mutant compared with the CNV line with three copies of ABCI3, whereas compound 1 was predicted to accumulate ∼30-fold more in 3D7-A10 compared with the CNV line.
Scoping insight on antiviral drugs against COVID-19
2021, Arabian Journal of ChemistryRecent developments in the design and synthesis of hybrid molecules basedon aminoquinoline ring and their antiplasmodial evaluation
2009, European Journal of Medicinal ChemistryCitation Excerpt :Efflux of CQ by a plasmodial P-glycoprotein as responsible for CQ resistance has been so questioned, however other studies have been related this resistance with a diminished level of accumulation rather than a drug export mechanism. This decreased accumulation could result from a modified vacuolar pH [48,49]. Another possibility is that the decreased CQ concentration could result from the loss of an intracellular receptor [50].
Is PfCRT a channel or a carrier? Two competing models explaining chloroquine resistance in Plasmodium falciparum
2007, Trends in Parasitology
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Current address: Parasitology Research, The Upjohn Co., Kalamazoo, MI 49001, U.S.A.
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Current address: Benson Institute, Brigham Young University, Provo, UT 84602, U.S.A.