OCT-1-mediated influx is a key determinant of the intracellular uptake of imatinib but not nilotinib (AMN107): reduced OCT-1 activity is the cause of low in vitro sensitivity to imatinib.

@article{White2006OCT1mediatedII,
  title={OCT-1-mediated influx is a key determinant of the intracellular uptake of imatinib but not nilotinib (AMN107): reduced OCT-1 activity is the cause of low in vitro sensitivity to imatinib.},
  author={Deborah L. White and Verity A. Saunders and Phuong Hoai Dang and Jane Engler and Andrew C W Zannettino and Antony C. Cambareri and Steven R Quinn and Paul William Manley and Timothy P Hughes},
  journal={Blood},
  year={2006},
  volume={108 2},
  pages={697-704}
}
Intrinsic sensitivity of newly diagnosed chronic myeloid leukemia (CML) patients to imatinib (IC50(imatinib)) correlates with molecular response. IC50(imatinib) is defined as the in vitro concentration of drug required to reduce phosphorylation of the adaptor protein Crkl by 50%. We now show that interpatient variability in IC50(imatinib) is mainly due to differences in the efficiency of imatinib intracellular uptake and retention (IUR). In 25 untreated CML patients, the IC50(imatinib) strongly… CONTINUE READING
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Oct-1–mediated Influx and Imatinib Response

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