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Compared to other PET tracers developed to study liver transporters which are transported quite selectively by the OATPs and MRP2 and BCRP [3,4] bile acid-based tracers such as [[sup.18]F] LCATD, [[sup.18]F]FCA and [[sup.11]C]Cholylsarcosine are generally handled by the same transporters involved in uptake and efflux of endogenous bile acids (NTCP, OATP1B1, OATP1B3, BSEP, and MRP2) [24-26], making them the best candidates to study physiology and pathophysiology of the hepatic bile acid transport in vivo [22,23,27].
In the influx transporter system, OATP1B1 and OATP1B3 have broad substrate specificity that can be used to measure activity, including rifampicin [159, 160], taurocholate , and pitavastatin .
Human OATP1B1, OATP1B3, and OATP2B1 expressing HEK293 cells were kindly provided by Dr.
Stieger, "Bosentan is a substrate of human OATP1B1 and OATP1B3: inhibition of hepatic uptake as the common mechanism of its interactions with cyclosporin A, rifampicin, and sildenafil," Drug Metabolism & Disposition, vol.
Expression of OATP1B3 determines uptake of Gd-EOB-DTPA in hepatocellular carcinoma.
Because of the structure and size of MCs, active uptake into cells occurs via organic anion-transporting polypeptides (OATP/Oatp), as confirmed for liver-specific human OATP1B1 and OATP1B3, mouse Oatp1b2 (mOatp 1b2), skate Oatp 1d1, and the more widely distributed OATP1A2 expressed, for example, at the blood--brain barrier.
Role of the liver-specific transporters OATP1B1 and OATP1B3 in governing drug elimination.
Transport of fluorescent chenodeoxycholic acid via the human organic anion transporters OATP1B1 and OATP1B3. J Lipid Res 2006; 47 : 1196-202.
Investigating the effect of statins on the regulation of the hepatic organic transporter OATP1B3. Carson-Newman University, Jefferson City, Tennessee.
To better determine the synergy between hypoxia and OATPs in HCC, we analyzed the expression levels of HIF1a and OATP1B3 in three different HCC PDX tissues from an HCC patient sample and found high expression of both proteins (Figure 6(a)).
De novo expression of OATPs, like OATP1B1 and OATP1B3, normally only expressed in liver, has been identified in a variety of cancers (breast, colon, pancreas, stomach, prostate, bone, and ovary cancer) [4-6].
The eight cell lines in the drug-transporter interactions service include P-glycoprotein (P-gp/MDR1), breast cancer resistant protein (BCRP), organic cation transporters 1& 2 (OCT1 & OCT2), organic anion transporter 3 (OAT3), organic anion transporting polypeptides 1B1 and 1B3 (OATP1B1 & OATP1B3), and multidrug resistance-associated protein 2 (MRP2).
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