Functional activity of efflux transporters in knockdown cells
| Substrate/Transporter | Cell Clone | Papp A→B* | Papp B→A* | Efflux Ratio | Percentage of VC |
|---|---|---|---|---|---|
| Digoxin/P-gp | VC | 1.14 ± 0.07 | 20.09 ± 1.36 | 17.7 | |
| P-gp KD | 1.59 ± 0.10 | 11.78 ± 1.22 | 7.4 | 42% | |
| BCRP KD | 0.54 ± 0.04 | 9.46 ± 1.60 | 17.7 | 100% | |
| MRP2 KD | 0.89 ± 0.20 | 19.00 ± 0.29 | 21.4 | 121% | |
| E3S/BCRP | VC | 0.57 ± 0.02 | 27.17 ± 1.08 | 48.5 | |
| P-gp KD | 0.52 ± 0.04 | 22.90 ± 2.98 | 43.6 | 90% | |
| BCRP KD | 1.03 ± 0.02 | 10.50 ± 2.81 | 10.2 | 21% | |
| MRP2 KD | 0.54 ± 0.04 | 33.46 ± 1.09 | 62.2 | 128% | |
| BSP/MRP2 | VC | 0.03 ± 0.05 | 1.45 ± 0.27 | 48.3 | |
| MRP2 KD | 0.34 ± 0.12 | 0.90 ± 0.14 | 2.6 | 5% |
↵* Papp values are expressed as the means ± S.D. (×10−6, cm/s); n = 3.