The influence of ABCG2 polymorphism on erlotinib efflux in the K562 cell line.

ABSTRACT: Single nucleotide polymorphisms (SNPs) in the gene for multidrug resistance protein ABCG2, an erlotinib transporter, is a possible contributor to the interindividual variation observed in erlotinib pharmacokinetics and toxicity. Therefore, the aim was to study erlotinib efflux by ABCG2 wild-type (wt) and ABCG2 polymorphic variants in the K562 cell line. The chronic myeloid leukemia K562 cell line, neither expressing EGFR nor ABCG2, was transduced with vectors containing the ABCG2 wt, the SNPs: 34 G > A and 421 C > A, or with empty vector (K562/ve). ABCG2-expressing cells were enriched using magnetic sorting and the expression was verified using flow cytometry. Intracellular erlotinib concentrations were analyzed by LC-MS/MS after incubation with 1 µmol/L erlotinib for 60 minutes. All recom

SUBMITTER: Svedberg A 

PROVIDER: S-EPMC7138917 | biostudies-literature | 2020 Apr

REPOSITORIES: biostudies-literature