In fact, rifamycin SV has been shown to inhibit OaTp1B1, OATP1B3
, nTcP [16,28], and the ATP-dependent bile salt export pump (BSEP) [29,30].
Lin, "Evaluating the in vitro inhibition of UGT1A1, OATP1B1, OATP1B3
, MRP2, and BSEP in predicting drug-induced hyperbilirubinemia," Molecular Pharmaceutics, vol.
The individual OATP1B1, OATP1B3
, and OATP2B1 expressing HEK cells were grown using PDL-coated flasks for better cell adhesion and growth.
OATP Signature sequence OATP1A2 D T R W V G A OATP1B1 D S R [W.bar] V G A OATP1B3
D S R W V G A OATP1C1 D P Q W V G A OATP2A1 D P R W I G A OATP2B1 D P R W V G A OATP3A1 D P R W I G A OATP4A1 S P L W V G A OATP4C1 D P R W L G A OATP5A1 D P R F I G N OATP6A1 S P E W L W T OATP Signature sequence OATP1A2 W W F G F L OATP1B1 [W.bar] [W.bar] L [N.bar] F L OATP1B3
W W L G F L OATP1C1 W W L G Y L OATP2A1 W W L G L L OATP2B1 W W L G F L OATP3A1 W W G G F L OATP4A1 W W V G F L OATP4C1 W W I G F L OATP5A1 W W S G F L OATP6A1 W W I N F L
Involvement of mitogen-activated protein kinase signaling pathways in microcystin-LR-induced apoptosis after its selective uptake mediated by OATP1B1 and OATP1B3
. Toxicol Sci 97(2):407-416.
We detected an increase in the mRNA expression of OATP3A1 in HCC clinical samples and a decrease in the expression of OATP1B3
and OATP2B1 compared with levels in normal liver tissue (Figure 6(b)).
The best characterized family is the OATP1 family with three transporters OATP1A2, OaTp1B1, and OATP1B3
that transport a number of typical OATP substrates including steroid hormone conjugates, thyroid hormones, prostaglandins, bile acids, and various drugs, for example, statins, antibiotics, and a number of anticancer drugs (for a review see ).
OBJECTIVE: We examined the contribution of the transcription factor p53, as well as that of the hepatic uptake transporter for microcystin-LR, organic anion transporting polypeptide 1B3 (OATP1B3
), to the cellular response to microcystin-LR exposure.
These agents may fall into the category of inhibitory or competitive OATP1B3
substrates, which may inhibit uptake of the toxin.
Transporters such as OATP1B1 (encoded by SLCO1B1) and OATP1B3
(SLCO1B3) can facilitate drug entry into the hepatocytes and, therefore, promote drug metabolism.
Kawai et al., "OATP1B1, OATP1B3
, and Mrp2 are involved in hepatobiliary transport of olmesartan, a novel angiotensin II blocker," Drug Metabolism and Disposition, vol.
Mano, "Preference of conjugated bile acids over unconjugated bile acids as substrates for OATP1B1 and OATP1B3
," PLoS ONE, vol.