Table 3.
OATPs Expression Patterns in Endocrine Tissue and Their Known Conjugated Steroid Substrates
| Influx Transporter Expressed in Cell Lines and Tissue (Ref.) | Substrate | Km Values, μm | Refs. |
|---|---|---|---|
| OATP1A2 | |||
| Breast (145, 161, 167) | DHEA-3-sulfate | 7 | 173, 175 |
| Prostate (179) | E2-17β-glucuronide | 424 | |
| Placenta (422, 423) | E1-3-sulfate | 16 | 167, 173, 425 |
| OATP1B1 | |||
| Breast (161) | DHEA-3-sulfate | 22 | 154, 162, 173, 298 |
| Prostate (168) | E2-17β-glucuronide | 4–24 | 162, 164, 298 |
| Ovary (426) | E1-3-sulfate | 0.09–45 | 162, 163, 173, 298 |
| OATP1B3 | |||
| Breast (156, 161) | DHEA-3-sulfate | 162, 164, 165, 173, 298 | |
| Prostate (157, 168) | E2-17β-glucuronide | 5–25 | 162, 164, 298 |
| Placenta (423) | E1-3-sulfate | 137, 165, 171, 298 | |
| Ovary (426) | |||
| Intestine (155, 168) | |||
| OATP1C1 | |||
| Testes (166) | E2-17β-glucuronide | 166 | |
| Placenta (427) | E1-3-sulfate | 166 | |
| T4 sulfate | 428 | ||
| OATP2B1 | |||
| Breast (161, 166, 429) | DHEA-3-sulfate | 9 | 166 |
| Placenta (181, 430) | E1-3-sulfate | 1.56–21 | 137, 138, 163, 166, 172, 173 |
| Intestine (138) | Pregnenolone sulfate | 172 | |
| OATP3A1 | |||
| Breast (161) | E2-17β-glucuronide | 160 | |
| E1-3-sulfate | 160 |
Only six of the 11 OATPs are included because the remaining OATPs have not shown sulfated steroid transport.