Article
Mutant Gly482 and Thr482 ABCG2 mediate high-level resistance to lipophilic antifolates.
Cancer chemotherapy and pharmacology - 1 Dec 2006
Bram Eran, Ifergan Ilan, Shafran Assaf, Berman Bluma, Jansen Gerrit, Assaraf Yehuda G
Abstract excerpt
Cellular uptake of hydrophilic antifolates proceeds via the reduced folate carrier whereas lipophilic antifolates enter cells by diffusion. Recently we have shown that transfectant cells overexpressing the mutant G482 ABCG2 displayed 120-6,250-fold resistance to hydrophilic antifolates than untransfected cells upon 4 h drug exposure, but lost almost all their antifolate resistance upon 72 h drug exposure (Shafran...
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