Gene | Description | HepaRG (DMSO−) | HepaRG-CAR (DMSO−) | HepaRG (DMSO+) | HepaRG-CAR (DMSO+) |
---|---|---|---|---|---|
Transcription factor | |||||
CAR (6) | Constitutive androstane receptor | 5.3 (±2.7) | 108 (±25)*** | 15 (±14)****** | 208 (±26)***,******,### |
PXR (6) | Pregnane X receptor | 20 (±10) | 18 (±11) | 37 (±23)*,***** | 25 (±16) |
AHR (4) | Aryl hydrocarbon receptor | 161 (±37) | 133 (±23) | 287 (±112)*,***** | 308 (±123)**,****** |
HNF4α (3) | Hepatocyte nuclear factor 4 α | 176 (±70) | 140 (±76) | 172 (±62) | 209 (±80) |
FXR (3) | Farnesoid X receptor | 123 (±27) | 89 (±5.0)* | 88 (±10)** | 94 (±21)* |
Phase 1 drug metabolism | |||||
CYP1A2 (5) | Cytochrome P450 1A2 | 0.04 (±0.02) | 0.04 (±0.05) | 0.59 (±0.35)***, ****** | 0.51 (±0.43)**,***** |
CYP2A6 (2) | Cytochrome P450 2A6 | 4.5 (±1.7) | 10 (±4.3) | 5.9 (±2.1) | 7.1 (±2.5) |
CYP2B6 (5) | Cytochrome P450 2B6 | 2.5 (±1.3) | 136 (±93) | 33 (±20) | 874 (±548)***,******,### |
CYP2C8 (2) | Cytochrome P450 2C8 | 12 (±0.9) | 22 (±1.2)*** | 9.8 (±2.9)****** | 28 (±2.7)***,****,### |
CYP2C9 (3) | Cytochrome P450 2C9 | 8.9 (±2.3) | 18 (±8.9) | 35 (±10)*** | 80 (±19)***,### |
CYP2C19 (1) | Cytochrome P450 2C19 | 21 (±1.6) | 46 (±6.2)** | 32 (±5.4) | 96 (±9.1)***,*****,### |
CYP2D6 (2) | Cytochrome P450 2D6 | 1.9 (±0.3) | 1.8 (±0.3) | 4.4 (±3.3) | 4.3 (±3.4) |
CYP2E1 (3) | Cytochrome P450 2E1 | 0.12 (±0.04) | 0.06 (±0.03) | 0.83 (±0.31) ***,****** | 0.09 (±0.02)### |
CYP3A4 (5) | Cytochrome P450 3A4 | 3.7 (±4.4) | 16 (±24) | 58 (±46) | 160 (±101) ***,******,### |
AOX1 (4) | Aldehyde oxidase 1 | 63 (±13) | 58 (±8.0) | 111 (±15)***,****** | 128 (±28) ***,****** |
POR (6) | Cytochrome P450 reductase | 54 (±13) | 78 (±17) | 81 (±23)* | 180 (±38) ***,******,### |
Phase 2 drug metabolism | |||||
UGT1A1 (3) | Uridine diphosphate glucuronosyltransferase 1 family. polypeptide A1 | 37 (±14) | 135 (±76) | 259 (±135) | 1595 (±866) ***,******,### |
Membrane transporter | |||||
NTCP (4) | Na+-taurocholate cotransporting polypeptide | 6.6 (±3.0) | 5.5 (±3.4) | 12 (±5.4)**** | 13 (±7.2)*,***** |
OATP1B1 (3) | Organic anion-transporting polypeptide 1B1 | 5.3 (±1.9) | 4.0 (±2.1) | 4.8 (±1.9) | 4.7 (±3.0) |
OATP2B1 (2) | Organic anion-transporting polypeptide 2B1 | 83 (±15) | 71 (±10) | 59 (±13)* | 65 (±14) |
MRP2 (2) | Multidrug resistance-associated protein 2 | 77 (±21) | 117 (±42) | 145 (±61)* | 216 (±34)***,*****,# |
MRP3 (1) | Multidrug resistance-associated protein 3 | 335 (±54) | 328 (±58) | 323 (±56) | 268 (±33) |
Blood protein | |||||
ALB (1) | Albumin | 47 (±6.7) | 63 (±8.2) | 41 (±7.7)**** | 31 (±2.9)***** |
Nitrogen metabolism | |||||
ARG1 (1) | Arginase 1 | 4.9 (±0.4) | 4.4 (±1.0) | 4.9 (±0.9) | 0.8 (±0.0) ***,******,### |
ARG2 (1) | Arginase 2 | 385 (±79) | 172 (±26)* | 654 (±62)**,****** | 495 (±90)***** |
CPS1 (1) | Carbamoyl-phosphate synthase 1 | 9.0 (±0.9) | 11 (±0.7)** | 2.7 (±0.4) ***,****** | 0.7 (±0.1)***,******,# |
Heme synthesis | |||||
ALAS1 (2) | 5′-Aminolevulinate synthase 1 | 23 (±5.0) | 34 (±5.9)* | 30 (±4.2) | 73 (±7.8)***,******,### |
↵* P < 0.05; **P < 0.01; ***P < 0.001 versus HepaRG (DMSO−); ****P < 0.05; *****P < 0.01; ******P < 0.001 versus HepaRG-CAR (DMSO−); #P < 0.05; ##P < 0.01; ###P < 0.001 versus HepaRG (DMSO+).