New endoperoxides highly active in vivo and in vitro against artemisinin-resistant Plasmodium falciparum

Authors: Lobo L, Cabral LIL, Sena MI, Guerreiro B, Rodrigues AS, De Andrade-Neto VF, Cristiano MLS, Nogueira F
Publication Year: 2018
Journal: Malaria Journal
Link: https://malariajournal.biomedcentral.com/articles/10.1186/s12936-018-2281-x%20

Background: The emergence and spread of Plasmodium falciparum resistance to artemisinin-based combination therapy in Southeast Asia prompted the need to develop new endoperoxide-type drugs. Methods: A chemically diverse library of endoperoxides was designed and synthesized. The compounds were screened for in vitro and in vivo anti-malarial activity using, respectively, the SYBR Green I assay and […]
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The drug transporter ABCB1 c.3435C&gt T SNP influences artemether-lumefantrine treatment outcome

Authors: Do Rosário V, Gil JP, Kiaco K, Lopes D, Rodrigues AS
Publication Year: 2017
Journal: Malaria Journal
Link: https://www.ncbi.nlm.nih.gov/pubmed/28934955

Malaria treatment performance is potentially influenced by pharmacogenetic factors. This study reports an association study between the ABCB1 c.3435C>T, CYP3A4*1B (g.-392A>G), CYP3A5*3 (g.6986A>G) SNPs and artemether + lumefantrine treatment outcome in 103 uncomplicated malaria patients from Angola. No significant associations with the CYP3A4*1B and CYP3A5*3 were observed, while a significant predominance of the ABCB1 c.3435CC genotype was […]
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Fluorimetric methods for analysis of permeability, drug transport kinetics, and inhibition of the ABCB1 membrane transporter

Authors: Amaral L, Armada A, Martins C, Molnar J, Rodrigues AS, Spengler G, Viveiros M
Publication Year: 2016
Journal: Cancer Drug Resistance
Link: https://link.springer.com/protocol/10.1007%2F978-1-4939-3347-1_7%20

The cell membrane P-glycoprotein (P-gp; MDR1, ABCB1) is an energy-dependent efflux pump that belongs to the ATP-binding cassette (ABC) family of transporters, and has been associated with drug resistance in eukaryotic cells. Multidrug resistance (MDR) is related to an increased expression and function of the ABCB1 (P-gp) efflux pump that often causes chemotherapeutic failure in […]
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New endoperoxides highly active in vivo and in vitro against artemisinin-resistant Plasmodium falciparum

The drug transporter ABCB1 c.3435C&gt T SNP influences artemether-lumefantrine treatment outcome

Fluorimetric methods for analysis of permeability, drug transport kinetics, and inhibition of the ABCB1 membrane transporter

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