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• W1567682956 startingPage "992" @default.
• W1567682956 abstract "We demonstrate the effects on membrane of the tubulin‐binding chemotherapy drugs: thiocolchicoside and taxol. Electrophysiology recordings across lipid membranes in aqueous phases containing drugs were used to investigate the drug effects on membrane conductance. Molecular dynamics simulation of the chemotherapy drug–lipid complexes was used to elucidate the mechanism at an atomistic level. Both drugs are observed to induce stable ion‐flowing pores across membranes. Discrete pore current–time plots exhibit triangular conductance events in contrast to rectangular ones found for ion channels. Molecular dynamics simulations indicate that drugs and lipids experience electrostatic and van der Waals interactions for short periods of time when found within each other’s proximity. The energies from these two interactions are found to be similar to the energies derived theoretically using the screened Coulomb and the van der Waals interactions between peptides and lipids due to mainly their charge properties while forming peptide‐induced ion channels in lipid bilayers. Experimental and in silico studies together suggest that the chemotherapy drugs induce ion pores inside lipid membranes due to drug–lipid physical interactions. The findings reveal cytotoxic effects of drugs on the cell membrane, which may aid in novel drug development for treatment of cancer and other diseases." @default.
• W1567682956 created "2016-06-24" @default.
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• W1567682956 date "2012-10-25" @default.
• W1567682956 modified "2023-10-16" @default.
• W1567682956 title "Chemotherapy Drugs Form Ion Pores in Membranes Due to Physical Interactions with Lipids" @default.
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• W1567682956 doi "https://doi.org/10.1111/cbdd.12060" @default.
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• W1567682956 hasPublicationYear "2012" @default.
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