|
ABC transporter | PPAR | PPAR Ligand | Cell line | Transporter effect | Reference |
|
ABCA1 | PPARα | Bezafibrate | Primary mouse fibroblasts | ↑ ABCA1 and LXR mRNA | [47] |
| | | THP1 human macrophages | ↑ apoA1-mediated cholesterol efflux | |
| | | WI38 human fibroblasts | | |
| | | | | |
| | | Immortalized human mesangial cells | ↑ ABCA1 and LXRα mRNA | [48] |
| | | | ↑ apoA1-mediated cholesterol efflux | |
| | | | | |
| | | Primary mouse hepatocytes | ↑ ABCA1 mRNA and protein | [49] |
| | | HepG2 human hepatoma cells | ↑ HDL synthesis | |
| | | | | |
| | Clofibrate | Primary human foreskin keratinocytes | ↑ ABCA1 mRNA | [50] |
| | | | | |
| | Fenofibrate | Primary mouse fibroblasts | ↑ ABCA1 and LXR mRNA | [47] |
| | | THP1 human macrophages | ↑ apoA1-mediated cholesterol efflux | |
| | | WI38 human fibroblasts | | |
| | | | | |
| | | BALB/3T3 mouse fibroblasts | ↑ ABCA1 mRNA and protein | [51] |
| | | RAW264.7 mouse leukemic macrophages | ↑ apoA1-mediated cholesterol efflux | |
| | | THP1 human macrophages | | |
| | | | | |
| | | Primary mouse hepatocytes | ↑ ABCA1 mRNA and protein | [49] |
| | | HepG2 human hepatoma cells | ↑ HDL synthesis | |
| | | | | |
| | Gemfibrozil | Primary mouse fibroblasts | ↑ ABCA1 and LXR mRNA | [47] |
| | | THP1 human macrophages | ↑ apoA1-mediated cholesterol efflux | |
| | | WI38 human fibroblasts | | |
| | | | | |
| | | Primary mouse hepatocytes | ↑ ABCA1 mRNA and protein | [49] |
| | | HepG2 human hepatoma cells | ↑ HDL synthesis | |
| | | | | |
| | LY518674 | Primary mouse fibroblasts | ↑ ABCA1 and LXR mRNA | [47] |
| | | THP1 human macrophages | ↑ apoA1-mediated cholesterol efflux | |
| | | WI38 human fibroblasts | | |
| | | | | |
| | | Primary mouse hepatocytes | ↑ ABCA1 mRNA and protein | [49] |
| | | HepG2 human hepatoma cells | ↑ HDL synthesis | |
| | | | | |
| | RPR-5 | Primary human macrophages | ↑ ABCA1 and LXR mRNA | [52] |
| | | | | |
| | WY14643 | Immortalized human mesangial cells | ↑ ABCA1 and LXR mRNA | [48] |
| | | | ↑ apoA1-mediated cholesterol efflux | |
| | | | | |
| | | Primary human macrophages | ↑ ABCA1 and LXR mRNA | [52] |
| | | | ↑ apoA1-mediated cholesterol efflux | |
| | | | | |
| | | THP1 human macrophages | ↑ ABCA1 mRNA | [52] |
| | | | | |
| | | BALB/3T3 mouse fibroblasts | ↑ ABCA1 mRNA and protein | [51] |
| | | RAW264.7 mouse leukemic macrophages | ↑ apoA1-mediated cholesterol efflux | |
| | | THP1 human macrophages | | |
| | | | | |
| | | Primary canine gallbladder epithelial cells | ↑ ABCA1 mRNA and protein | [53] |
| | | | | |
| PPAR | 13-HODE | RAW264.7 mouse leukemic macrophages | ↑ Abca1 and LXR protein | [54] |
| | | | ↑ cholesterol efflux | |
| | | | | |
| | c9t11-CLA | RAW264.7 mouse leukemic macrophages | ↑ Abca1 mRNA and protein | [55] |
| | | | ↑ LXR mRNA | |
| | | | ↑ HDL-mediated cholesterol efflux | |
| | | | | |
| | t10c12-CLA | RAW264.7 mouse leukemic macrophages | ↑ Abca1 mRNA and protein | [55] |
| | | | ↑ LXR mRNA | |
| | | | ↑ HDL-mediated cholesterol efflux | |
| | | | | |
| | NO-pravastatin | Primary canine gallbladder epithelial cells | ↑ ABCA1 mRNA and protein | [53] |
| | | | ↑ LXR mRNA | |
| | | | | |
| | Pravastatin | Primary canine gallbladder epithelial cells | ↑ ABCA1 mRNA and protein | [53] |
| | | | ↑ LXR mRNA | |
| | | | | |
| | Simvastatin | Primary canine gallbladder epithelial cells | ↑ ABCA1 mRNA and protein | [53] |
| | | | ↑ LXR mRNA | |
| | | | | |
| PPAR | Pioglitazone | Primary mouse fibroblasts | ↑ ABCA1 and LXR mRNA | [47] |
| | | THP1 human macrophages | ↑ apoA1-mediated cholesterol efflux | |
| | | WI38 human fibroblasts | | |
| | | | | |
| | | RAW264.7 mouse leukemic macrophages | ↑ Abca1 mRNA and protein | [56] |
| | | THP1 human macrophages | ↑ cholesterol efflux | |
| | | | | |
| | Rosiglitazone | Primary human macrophages | ↑ ABCA1 and LXR mRNA | [52] |
| | | | ↑ apoA1-mediated cholesterol efflux | |
| | | | | |
| | | THP1 human macrophages | ↑ ABCA1 mRNA | [52] |
| | | | | |
| | | | ↑ ABCA1 and LXR mRNA | [57] |
| | | | ↑ cholesterol efflux | |
| | | | | |
| | | | ↑ ABCA1 mRNA and protein | [58] |
| | | | | |
| | | | ↑ ABCA1 mRNA and protein | [59] |
| | | | ↓ intracellular cholesterol | |
| | | | | |
| | Troglitazone | Primary human macrophages | ↑ ABCA1 and LXR mRNA | [52] |
| | | | | |
| | | THP1 human macrophages | ↑ ABCA1 mRNA | [52] |
| | | | | |
| | | Primary canine gallbladder epithelial cells | ↑ ABCA1 mRNA and protein | [53] |
| | | | | |
| | GW1929 | HepG2 human hepatoma cells | ↑ ABCA1, LXR, and LXR mRNA | [60] |
| | | | ↓ ABCA1 and LXR protein | |
| | | | | |
| | GW7845 | THP1 human macrophages | ↑ ABCA1 mRNA | [61] |
| | | | | |
| | Mycophenolic acid | HepG2 human hepatoma cells | ↑ ABCA1 mRNA and protein | [62] |
| | | | ↑ LXR protein | |
| | | | | |
| | Prostaglandin J2 | Immortalized human mesangial cells | ↑ ABCA1 and LXR mRNA | [48] |
| | | | ↑ apoA1-mediated cholesterol efflux | |
| | | | | |
| | | Primary human macrophages | ↑ ABCA1 and LXR mRNA | [52] |
| | | | | |
| | Telmisartan | RAW264.7 mouse leukemic macrophages | ↑ Abca1 mRNA | [63] |
| | | | ↓ macrophage proliferation | |
| | | | | |
| PPAR | GW501516 | Primary mouse fibroblasts | ↑ ABCA1 and LXR mRNA | [47] |
| | | THP1 human macrophages | ↑ apoA1-mediated cholesterol efflux | |
| | | WI38 human fibroblasts | | |
| | | | | |
| | | THP1 human macrophages | ↑ ABCA1 mRNA | [61] |
| | | 1BR3N human fibroblasts | ↑ apoA1-mediated cholesterol efflux | |
| | | | | |
| | | FHS74 human intestinal cells | ↑ ABCA1 mRNA | [61] |
| | | | | |
| | | Primary human skeletal muscle cells | ↑ ABCA1 mRNA | [64] |
| | | | | |
| | | Primary human foreskin keratinocytes | ↑ ABCA1 mRNA | [50] |
|
ABCA12 | PPAR | Ciglitazone | Primary human foreskin keratinocytes | ↑ ABCA12 mRNA and protein | [65] |
| | | | | |
| | Troglitazone | Primary human foreskin keratinocytes | ↑ ABCA12 mRNA | [65] |
| | | | | |
| | GI251929X | Primary human foreskin keratinocytes | ↑ ABCA12 mRNA | [65] |
| | | | | |
| PPAR | Ceramide | Primary human foreskin keratinocytes | ↑ ABCA12 mRNA and protein | [66] |
| | | | | |
| | GW610742 | Primary human foreskin keratinocytes | ↑ ABCA12 mRNA and protein | [65] |
|
Pgp/MDR1/ABCB1 | PPAR | Fenofibrate | Pgp-overexpressing L-MDR1 porcine kidney epithelial cells | ↓ calcein efflux | [67] |
| | | | | |
| PPAR | Simvastatin | Pgp-overexpressing L-MDR1 porcine kidney epithelial cells | ↓ calcein efflux | [67] |
| | | | | |
| PPAR | Rosiglitazone | Doxorubicin-resistant P388 mouse leukemia cells | ↓ calcein efflux | [68] |
| | | | | |
| | Troglitazone | Doxorubicin-resistant P388 mouse leukemia cells | ↓ calcein efflux | [68] |
| | | | | |
| | | Doxorubicin-resistant K562 human leukemia cells | ↓ Pgp protein | [69] |
| | | Doxorubicin-resistant MCF7 human breast cancer cells | ↑ sensitivity to doxorubicin | |
| | | | | |
| | | Vincristine-resistant SGC7901 human gastric cancer cells | ↓ Pgp mRNA and protein | [70] |
| | | | ↓ Rh123 efflux | |
| | | | ↑ sensitivity to vincristine | |
|
MDR2/MDR3/ABCB4 | PPAR | Bezafibrate | HepG2 human hepatoma cells | ↑ MDR2/MDR3 mRNA | [71] |
| | | | ↑ MDR2/MDR3 redistribution | |
| | | | | |
| | | | ↑ MDR2/MDR3 mRNA | [72] |
| | | | ↑ MDR2/MDR3 redistribution | |
| | | | ↑ phospholipid efflux | |
| | | | | |
| | Ciprofibrate | Primary mouse hepatocytes | ↑ Mdr2 mRNA | [73] |
| | | | | |
| | WY14643 | Primary mouse hepatocytes | ↑ Mdr2 mRNA | [73] |
|
MRP2/ABCC2 | PPAR | Troglitazone | Primary rat hepatocytes | ↓ Mrp2-associated bile efflux | [74] |
|
ABCG1 | PPAR | 13-HODE | RAW264.7 mouse leukemic macrophages | ↑ Abcg1 and LXR protein | [54] |
| | | | ↑ cholesterol efflux | |
| | | | | |
| PPAR | Pioglitazone | RAW264.7 mouse leukemic macrophages | ↑ ABCG1 mRNA and protein | [56] |
| | | THP1 human macrophages | ↑ cholesterol efflux | |
| | | | | |
| | Rosiglitazone | THP1 human macrophages | ↑ ABCG1 and LXR mRNA | [57] |
| | | | ↑ cholesterol efflux | |
| | | | | |
| | Telmisartan | RAW264.7 mouse leukemic macrophages | ↑ Abcg1 mRNA | [63] |
| | | | ↓ macrophage proliferation | |
|
BCRP/ABCG2 | PPAR | Clofibrate | HCMEC/D3 human cerebral microvascular endothelial cells | ↑ BCRP mRNA and protein | [75] |
| | | | ↑ mitoxantrone efflux | |
| | | | | |
| | GW7647 | HCMEC/D3 human cerebral microvascular endothelial cells | ↑ BCRP mRNA and protein | [75] |
| | | | | |
| PPAR | Rosiglitazone | Primary human dendritic cells | ↑ BCRP mRNA and protein | [76] |
| | | | ↑ Hoescht efflux | |
| | | | ↑ mitoxantrone efflux | |
| | | | ↑ sensitivity to mitoxantrone | |
| | | | | |
| | | BCRP-overexpressing MDCKII canine kidney epithelial cells | ↓ PhA efflux | [68] |
| | | | | |
| | | HuH7 human hepatoma cells | ↑ BCRP mRNA | [68] |
| | | | | |
| | Troglitazone | Primary human dendritic cells | ↑ BCRP mRNA | [76] |
| | | | | |
| | | HuH7 human hepatoma cells | ↑ BCRP mRNA | [68] |
| | | | | |
| | | Doxorubicin-resistant K562 human leukemia cells | ↓ BCRP protein | [69] |
| | | Doxorubicin-resistant MCF7 human breast cancer cells | ↑ sensitivity to doxorubicin | |
| | | | | |
| GW7845 | | Primary human dendritic cells | ↑ BCRP mRNA | [76] |
| | | | | |
| GW9662 | | Doxorubicin-resistant MCF7 human breast cancer cells | ↓ BCRP protein | [69] |
|