Table 1.
Cellular p53 Status, P-gp Expression, MRP1 Expression, BCRP1 Expression, and Tumor Cell Sensitivity to Saquinavir and Saq-NO.
| Cell Line | p53 Status* | P-gp† | MRP1‡ | BCRP1§ | Saquinavir IC50 (µM) | Saq-NO IC50 (µM) |
| UKF-NB-3 | WT | - | - | - | 23.2 ± 6.7 | 9.40 ± 2.0¶ |
| UKF-NB-3rVCR10 | mut (C135F) | + | - | - | 18.9 ± 4.5 | 6.6 ± 1.5¶ |
| UKF-NB-3MDR1 | WT | + | - | - | 27.8 ± 5.3 | 13.5 ± 2.3¶ |
| UKF-NB-3LeGO-Cer2# | WT | - | - | - | 21.0 ± 1.4 | 10.3 ± 2.4¶ |
| UKF-NB-3BCRP1 | WT | - | - | + | 27.5 ± 5.0 | 11.5 ± 1.2¶ |
| UKF-NB-3LeGO-iG2** | WT | - | - | - | 20.4 ± 3.6 | 10.1 ± 0.9¶ |
| UKF-NB-3p53-shRNA | depl. | - | - | - | 20.2 ± 4.3 | 9.7 ± 1.3¶ |
| UKF-NB-3scr-shRNA†† | WT | - | - | - | 21.3 ± 2.1 | 9.3 ± 1.7¶ |
| Rh30 | mut (R273C) | - | - | - | 18.7 ± 3.0 | 8.4 ± 3.8¶ |
| Rh30rVCR10 | mut (R273C) | + | - | - | 26.7 ± 3.5 | 12.7 ± 1.9¶ |
| PC-3 | del. | - | - | - | 14.3 ± 2.0 | 5.6 ± 0.7¶ |
| PC-3rVCR20 | del. | - | + | - | 16.1 ± 1.9 | 7.5 ± 0.8¶ |
Values are mean ± SD from three independent experiments.
*
p53 status: WT = wild-type p53, mut = mutated p53, depl. = shRNA-induced p53 depletion, del. = deleted.
†
P-gp expression: + = overexpression, - = no overexpression.
‡
MRP1 expression: + = overexpression, - = no overexpression.
§
BCRP1 expression: + = overexpression, - = no overexpression.
¶
P < .05 relative to saquinavir.
#
Control vector for MDR1 expressing only Cerulean.
**
Control vector for BCRP1 expressing only eGFP.
††
Control vector for p53-shRNA expressing scrambled shRNA.