Antimicrobial effects of N-benzyloxycarbonyl-S-(2,4-dinitrophenyl) glutathione diesters against chloroquinine sensitive (NF54) and resistant (K1) strains of Plasmodium falciparum

Daunes, Sylvie; D’Silva, Claudius

doi:10.1016/j.bioorg.2018.03.008

Cited by 1 publication

(2 citation statements)

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“…Some genomes (like NF54) might include the capacity of compensatory mechanisms, including other transporters, apparently not available in the W2 clone. The question is anyway still open, as emphasysed by the in vitro observation that 3D7 is sensitive to N-Benzyloxycarbony-S-(2,4-dinitrophenyl)-glutathione diesters, a class of specific MRP inhibitor proposed as proof of concept compounds for defining MRPs as valuable antimalarial targets ( Daunes and D'Silva, 2018 ).…”

Section: Pf Mrp S —Potential Natural Roles In the Parasite Physiologymentioning

confidence: 99%

“…It is reasonable to consider that pf MRPs, with their characteristic capacity of transporting a broad range of chemical structures, and gateway localization in the plasma membrane will have an important role. In parallel, the possibility to explore these transporters as drug targets themselves is open ( Henry et al, 2008a ; Daunes and D'Silva, 2018 ). In this scenario, the blockage of liver schizont formation is particularly attractive ( Rijpma et al, 2016 ).…”

Section: Expert Opinionmentioning

confidence: 99%

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Plasmodium falciparum Multidrug Resistance Proteins (pfMRPs)

Gil

Fançony²

2021

Front. Pharmacol.

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The capacity of the lethal Plasmodium falciparum parasite to develop resistance against anti-malarial drugs represents a central challenge in the global control and elimination of malaria. Historically, the action of drug transporters is known to play a pivotal role in the capacity of the parasite to evade drug action. MRPs (Multidrug Resistance Protein) are known in many phylogenetically diverse groups to be related to drug resistance by being able to handle a large range of substrates, including important endogenous substances as glutathione and its conjugates. P. falciparum MRPs are associated with in vivo and in vitro altered drug response, and might be important factors for the development of multi-drug resistance phenotypes, a latent possibility in the present, and future, combination therapy environment. Information on P. falciparum MRPs is scattered in the literature, with no specialized review available. We herein address this issue by reviewing the present state of knowledge.

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Section: Pf Mrp S —Potential Natural Roles In the Parasite Physiologymentioning

confidence: 99%