Transporters such as OATP1B1 (encoded by SLCO1B1) and OATP1B3 (SLCO1B3
) can facilitate drug entry into the hepatocytes and, therefore, promote drug metabolism.
Unconjugated BS are transported by the multispecific ATP- and [Na.sup.+]-independent basolateral uptake transporters, organic anion-transporting polypeptide 1B1 (OATP1B1, also termed OATP-C, OATP2, SLC21A6, or LST-1, encoded by SLCO1B1), and 1B3 (OATP1B3, synonyms OATP8, SLC21A8, or LST3, encoded by SLCO1B3) [4, 7, 8].
Likewise, FXR can directly transactivate the ABCC2, ABCB4, and SLCO1B3 genes [36, 37].
Nakashima et al., "Association of genetic polymorphisms in the influx transporter SLCO1B3
and the efflux transporter ABCB1 with imatinib pharmacokinetics in patients with chronic myeloid leukemia," Therapeutic Drug Monitoring, vol.
Ostrander et al., "Expression of SLCO transport genes in castration-resistant prostate cancer and impact of genetic variation in SLCO1B3 and SLCO2B1 on prostate cancer outcomes," Cancer Epidemiology Biomarkers and Prevention, vol.
Price et al., "Effect of SLCO1B3 haplotype on testosterone transport and clinical outcome in caucasian patients with androgen-independent prostatic cancer," Clinical Cancer Research, vol.
However, the association was found in SNPs of another gene in the same gene family, SLCO1B3 (rs2117032, P = 4.7 X [10.sup.-8]).
In addition, the effects of SLCO1B1 or other transporter genes within the same chromosome location such as SLCO1B3, as well as X-linked G6PD, were confirmed.
2007), we demonstrated that transfection of OATP1B1 (SLCO1B1) or OATP1B3 (SLCO1B3) cDNA into HEK293 cells increased their sensitivity to, and their accumulation of, microcystin-LR and, consequently, induced apoptosis in those cells.
Mutations in the SLCO1B3 gene affecting the substrate specificity of the hepatocellular uptake transporter OATP1B3 (OATP8).
hepatocytes, but not OATP1B1 (SLCO1B1) or OATP1B3 (SLCO1B3
Fried et al., "The human organic anion transporting polypeptide 8 (SLCO1B3
) gene is transcriptionally repressed by hepatocyte nuclear factor 3[beta] in hepatocellular carcinoma," Journal of Hepatology, vol.