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Solute carrier organic anion transporter family, member 1B3

This gene encodes a liver-specific member of the organic anion transporter family. The encoded protein is a transmembrane receptor that mediates the sodium-independent uptake of endogenous and xenobiotic compounds and plays a critical role in bile acid and bilirubin transport. Mutations in this gene are a cause of Rotor type hyperbilirubinemia. [provided by RefSeq, Feb 2012] (from NCBI)
Top mentioned proteins: OATP1B1, OATP, ACID, CAN, HAD
Papers on OATP1B3
Novel No-Wash Luminogenic Probes for the Detection of Transporter Uptake Activity.
Cali et al., San Luis Obispo, United States. In Bioconjug Chem, Feb 2016
Six probes were tested with OATP1B1*1a and OATP1B3 overexpressing HEK293 cells, and all compounds showed up to 10.2-fold enhancement in uptake when compared to control cells.
Investigation of Fluorescein Derivatives as Substrates of Organic Anion Transporting Polypeptide (OATP) 1B1 To Develop Sensitive Fluorescence-Based OATP1B1 Inhibition Assays.
Sugiyama et al., Tsukuba, Japan. In Mol Pharm, Feb 2016
For establishing a highly sensitive, high-throughput fluorescence-based OATP1B1 inhibition assay system, the present study focused on fluorescein (FL) and its derivatives and evaluated their uptake via OATP1B1 as well as OATP1B3 and OATP2B1 using the transporter-expressing human embryonic kidney 293 cells.
The non-metabolized β-blocker nadolol is a substrate of OCT1, OCT2, MATE1, MATE2-K and P-glycoprotein, but not of OATP1B1 and OATP1B3.
Fromm et al., In Mol Pharm, Jan 2016
We therefore investigated nadolol as a potential substrate of the hepatic uptake transporters OATP1B1, OATP1B3, and OCT1 and of the renal transporters OCT2, MATE1, and MATE2-K expressed in HEK cells.
Evaluation of Ketoconazole and its Alternative Clinical CYP3A4/5 Inhibitors as Inhibitors of Drug Transporters: The In Vitro Effects of Ketoconazole, Ritonavir, Clarithromycin and Itraconazole on 13 Clinically-Relevant Drug Transporters.
Buckley et al., In Drug Metab Dispos, Jan 2016
In this study, the inhibitory effects of ketoconazole, clarithromycin, ritonavir and itraconazole (and its CYP3A4-inhibitory metabolites, hydroxy-, keto- and N-desalkyl itraconazole) towards 13 drug transporters (OATP1B1, OATP1B3, OAT1, OAT3, OCT1, OCT2, MATE1, MATE2-K, P-gp, BCRP, MRP2, MRP3 and BSEP) were systematically assessed in transporter-expressing HEK-293 cell lines or membrane vesicles.
Alteration of the intravenous and oral pharmacokinetics of valsartan via the concurrent use of gemfibrozil in rats.
Han et al., Seoul, South Korea. In Biopharm Drug Dispos, Jan 2016
The cellular uptake of valsartan and gemfibrozil was also investigated by using cells overexpressing OATP1B1 or OATP1B3.
Pharmacogenetic analysis of advanced non-small-cell lung cancer patients treated with first-line paclitaxel and carboplatin chemotherapy.
Cho et al., Pusan, South Korea. In Pharmacogenet Genomics, Jan 2016
RESULTS: Patients with the c.334 T>G and c.699 G>A homozygous variant in SLCO1B3 showed a higher incidence of grade 3/4 anemia (P=0.002).
Gene replacement therapy for genetic hepatocellular jaundice.
Bosma et al., Amsterdam, Netherlands. In Clin Rev Allergy Immunol, Jun 2015
In patients with Rotor syndrome, bilirubin (re)uptake is impaired due to the deficiency of two basolateral/sinusoidal hepatocellular membrane proteins, organic anion-transporting polypeptide 1B1 (OATP1B1) and OATP1B3.
Organic anion transporting polypeptide (OATP)1B1 and OATP1B3 as important regulators of the pharmacokinetics of substrate drugs.
Maeda, Tokyo, Japan. In Biol Pharm Bull, 2014
Because of their broad substrate specificities, once the functions of OATP1B1 or OATP1B3 are altered by several kinds of special occasions such as drug-drug interactions (DDI) and genetic polymorphisms of transporter genes, the hepatic clearance of many kinds of structurally-unrelated drugs is expected to be changed.
Cancer-type Organic Anion Transporting Polypeptide 1B3: Current Knowledge of the Gene Structure, Expression Profile, Functional Implications and Future Perspectives.
Chiba et al., Chiba, Japan. In Curr Drug Metab, 2014
Human organic anion transporting polypeptide 1B3 (OATP1B3) is a hepatocyte drug transporter that facilitates uptake of various therapeutic drugs from the circulatory system.
Montelukast Disposition: No Indication of Transporter-Mediated Uptake in OATP2B1 and OATP1B1 Expressing HEK293 Cells.
Grime et al., Mölndal, Sweden. In Pharmaceutics, 2014
Montelukast is a carboxylic acid, a relatively potent inhibitor of OATP1B1, OATP1B3, and OATP2B1, and has previously been postulated to be actively transported into human hepatocytes.
Pharmacology and toxicology of mycophenolate in organ transplant recipients: an update.
Tett et al., Brisbane, Australia. In Arch Toxicol, 2014
Genetic variants within genes involved in MPA metabolism (UGT1A9, UGT1A8, UGT2B7), cellular transportation (SLCOB1, SLCO1B3, ABCC2) and targets (IMPDH) have been reported to effect MPA pharmacokinetics and/or response in some studies; however, larger studies across different ethnic groups that take into account genetic linkage and drug interactions that can alter a patient's phenotype are needed before any clinical recommendations based on patient genotype can be formulated.
Diagnosis of Pathologically Early HCC with EOB-MRI: Experiences and Current Consensus.
Morisaka et al., Japan. In Liver Cancer, 2014
Thus, the diagnostic performance of pathological analyses for early HCC cases may be dramatically improved, nearly up to that of EOB-MRI, by incorporating an OATP1B3 staining method.
Alteration in placental expression of bile acids transporters OATP1A2, OATP1B1, OATP1B3 in intrahepatic cholestasis of pregnancy.
Wang et al., Hangzhou, China. In Arch Gynecol Obstet, 2012
The expression of OATP1A2 and OATP1B3 in placenta decreased in, and may be involved in the pathophysiology of, intrahepatic cholestasis of pregnancy. OATP1B3 was localized to the vasculo-syncytial membrane of syncytiotrophoblasts.
Interaction of three regiospecific amino acid residues is required for OATP1B1 gain of OATP1B3 substrate specificity.
Kim et al., London, Canada. In Mol Pharm, 2012
Site-directed mutagenesis of three key residues in OATP1B1 transmembrane helices 1 and 10, and extracellular loop 6, to the corresponding residues in OATP1B3, resulted in a gain of CCK-8 transport by OATP1B1.
Functional consequences of genetic variations in the human organic anion transporting polypeptide 1B3 (OATP1B3) in the Korean population.
Chung et al., Seoul, South Korea. In J Pharm Sci, 2012
Thirty-six variations of OATP1B3 were identified in the Korean population, consisting of nine variations in the 5'-upstream region, ten in the exon regions, and seventeen in the intron regions.
Identification of a new organic anion transporting polypeptide 1B3 mRNA isoform primarily expressed in human cancerous tissues and cells.
Chiba et al., Chiba, Japan. In Biochem Biophys Res Commun, 2012
Isoform specific mRNA quantification showed that the Ct-OATP1B3 mRNA level was strikingly higher than that of Lt-OATP1B3 mRNA in human cancer tissues.
Complete OATP1B1 and OATP1B3 deficiency causes human Rotor syndrome by interrupting conjugated bilirubin reuptake into the liver.
Schinkel et al., Amsterdam, Netherlands. In J Clin Invest, 2012
Data show that Rotor syndrome was linked to mutations predicted to cause complete and simultaneous deficiencies of the organic anion transporting polypeptides OATP1B1 and OATP1B3.
The expression and function of organic anion transporting polypeptides in normal tissues and in cancer.
Hagenbuch et al., Kansas City, United States. In Annu Rev Pharmacol Toxicol, 2011
Among these are the multispecific OATP1A2, OATP1B1, OATP1B3, and OATP2B1.
SLCO2B1 and SLCO1B3 may determine time to progression for patients receiving androgen deprivation therapy for prostate cancer.
Kantoff et al., Boston, United States. In J Clin Oncol, 2011
Genetic variants of SLCO1B3 may function as pharmacogenomic determinants of resistance to androgen deprivation therapy in prostate cancer.
Organic anion transporting polypeptide 1B1: a genetically polymorphic transporter of major importance for hepatic drug uptake.
Neuvonen et al., Helsinki, Finland. In Pharmacol Rev, 2011
In this article, we review the current knowledge about the expression, function, substrate characteristics, and pharmacogenetics of OATP1B1 as well as its role in drug interactions, in parts comparing with those of other hepatocyte-expressed organic anion transporting polypeptides, OATP1B3 and OATP2B1.
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