In vitro cell uptake and membrane vesicle efflux assays using [[sup.3]H] LCATD demonstrated that this amphiphilic molecule can hardly penetrate the cell membrane by passive diffusion, whereas it is quickly taken up by cells expressing the OATP1B1
, NTCP transporters, and effluxed by means of BSEP .
has about fourteen known mutations that have been found to exist within individual populations of people from either European, African, or Asian descent .
The individual OATP1B1
, OATP1B3, and OATP2B1 expressing HEK cells were grown using PDL-coated flasks for better cell adhesion and growth.
has been previously predicted by topology prediction analyses to contain 12 transmembrane domains (TMs) and intracellular amino (N) and carboxyl (C) termini [2, 14].
In the human, mouse, and rat, 36 different OATPs/Oatps have been found (Hagenbuch 2007; Hagenbuch and Meier 2004); these can be expressed either ubiquitously (e.g., OATP1A2) or with tissue/organ-specific expression (e.g., OATP1B1
and 1B3 in the liver) (Hagenbuch and Meier 2004).
Background & objectives: Organic anion transport protein 1B1 (OATP1B1
) is a major transporter protein for bile salt uptake in the enterohepatic circulation of bile salts.
Linking organic anion transporting polypeptide 1B1 and 1B3 (OATP1B1
and OATP1B3) interaction profiles to hepatotoxicity--The hyperbilirubinemia use case.
Transporters such as OATP1B1
(encoded by SLCO1B1) and OATP1B3 (SLCO1B3) can facilitate drug entry into the hepatocytes and, therefore, promote drug metabolism.
Using fibrates with statins is beneficial for some patients; however, gemfibrozil significantly interacts with statins by inhibiting CYP2C8 and organic anion transporting polypeptide 1B1 (OATP1B1
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).
polymorphism is a major determinant of serum bilirubin level but not associated with rifampicin-mediated bilirubin elevation.