Table 2.
Changes in transporter expression levels in various chronic disease states versus healthy subjects*
| Disease | Organ | Transporter mRNA |
Transporter Protein |
References |
|---|---|---|---|---|
| Chronic Kidney Disease | Kidney | Rat: ↑Mrp2, Mrp3, Mrp4, Oatp2, Oatp3 ↓Oatk2, Oatp1, OATP4c1, Oatp5, P-gp, Urat1, Npt1 |
Rat: ↑Mrp2, Mrp3, Mrp4, Oatp2, Oatp3 ↓Oat1, Oat2, Oat3, Oatp1, Oatp4c1, P-gp, Urat1, Npt1 |
(102) |
| Liver | Rat: ↑P-gp, Mrp2 |
Rat: ↑P-gp ↓Oatp2 |
(103) | |
| Intestine | Rat: ↓P-gp, Mrp2, Mrp3 |
(104) | ||
| Nonalcoholic Fatty Liver Disease/Nonalcoholic steatohepatitis | Liver | Human: ↓BSEP (males and females), MRP2 (females), NTCP (males and females) |
(105) | |
| Human: ↓MRP6 ↑MRP1, MRP3, MRP4, MRP5, P-gp, BCRP |
Human: ↑MRP1, MRP3, MRP4, MRP5, MRP6, P-gp, BCRP |
(57) | ||
| Human: ↔OATP1B1, OATP2B1 ↓OATP1B3 |
Human: ↔OATP1A2 ↓OATP1B3 ↑OATP1B1 |
(54) | ||
| Hepatitis C Cirrhosis | Liver | Humana: ↓NTCP, OATP1B3, OCT1, BSEP, MRP2, P-gp ↑ MATE1 ↔ OATP1B1, OATP2B1, BCRP, MRP3 |
(46) | |
| Human: ↓OCT1, OAT2, OAT7, OATP1B1, OATP1B3, OATP2B1, MATE1, MRP2, MRP3, MRP6, BCRP ↑P-gp, MRP1, MRP4, MRP5 |
Human: ↑MRP4 |
(48) | ||
| Alcoholic Cirrhosis | Liver | Humana: ↓NTCP, OATP1B1, OATP1B3, OCT1, BCRP, BSEP ↑MATE1, MRP3 ↔ OATP2B1, MATE1, MRP2, P-gp |
(46) | |
| Human: ↓OATP1B3, ↑MRP4, MRP5, BCRP, OATP2B1, MRP1, MRP3, MRP5 |
(47) | |||
| HCV Hepatocellular Carcinoma | Liver | Human cancerous tissuea: ↓NTCP, OATP1B1, OATP1B3, OATP2B1, OCT1, BSEP, MRP2, MRP3, P-gp ↔ MATE1 Human non-cancerous tissuea: ↓OATP1B1, OATP1B3, OATP2B1, OCT1, BSEP, MATE1, MRP3, P-gp ↑NTCP ↔ MRP2 |
(106) | |
| Human Immuno-Deficiency Virus | Intestine | Human: ↓MRP2, BCRP |
Human: ↓MRP2, BCRP |
(107) |
| Colon | Human: ↓P-gp, MRP4 |
Human: ↓P-gp, MRP2 |
(108) | |
| Inflammatory Bowel Disease | Colon | Human: ↓P-gp, BCRP, MRP3, MRP4, OCTN2, OSTα/β ↑OATP2B1, OATP4A1, ENT1, ENT2, CNT2, PEPT1 |
Human: ↓P-gp, BCRP ↑MRP1 |
(65,67-69) |
| Ileum | Human: ↓ASBT, BCRP, OCTN2 ↑OATP2B1, ENT1, ENT2 |
(67,68) |
↑, expression increased in disease state relative to controls; ↓, expression decreased in disease state relative to controls; mg, milligram
*
Data obtained in preclinical species were only included in cases where human data were not available
a
Data were normalized to picomole/gram of liver