Kinetics of interaction of gemcitabine with CNT1-reference and its four common protein altering variants Vaccinia-infected HeLa cells were transfected with CNT1 and its variants as described under Materials and Methods. The uptake of [3H]thymidine in the presence of increasing concentrations of gemcitabine was measured after a 4-min incubation. Data represent mean ± S.E. from at least three different experiments.
Variant
Gemcitabine IC50
μM
CNT1-reference
13.8 ± 0.60
CNT1 + 140Val
16.9 ± 1.21
CNT1-Val189Ile*
23.3 ± 1.55
CNT1-Gln237Lys
14.4 ± 0.43
CNT1-Asp521Asn
10.8 ± 1.08
↵*P < 0.05, significantly different from value obtained for CNT1-reference