Affinage

SLCO1B1

Solute carrier organic anion transporter family member 1B1 · UniProt Q9Y6L6

Length
691 aa
Mass
76.4 kDa
Annotated
2026-06-10
100 papers in source corpus 28 papers cited in narrative 28 extracted findings
Cross-family judge vs UniProt: Affinage preferred faithfulness: 5/5 claims corpus-supported (100%)

Mechanistic narrative

Synthesis pass · prose summary of the discoveries below

SLCO1B1 encodes OATP1B1, a sodium-independent organic anion uptake transporter localized to the basolateral (sinusoidal) membrane of human hepatocytes that mediates hepatic clearance of bile acid conjugates, drugs, and their metabolites (PMID:12695556, PMID:12196548). It transports a broad range of organic anions and pharmaceuticals, including sulfobromophthalein, bilirubin conjugates, statins (pravastatin), rifampin, enalapril, maraviroc, docetaxel, and glucuronide metabolites of sorafenib and gemfibrozil (PMID:11134001, PMID:11748225, PMID:12490595, PMID:16627748), with in vivo knockout and liver-specific humanized mouse models confirming its dominant role in hepatic uptake and systemic clearance of statins and chemotherapeutics (PMID:24194513, PMID:24825069, PMID:23340295). OATP1B1 achieves vectorial hepatobiliary transport by working in series with the canalicular efflux pump MRP2, as reconstituted in double-transfected polarized monolayers for estradiol glucuronide, pravastatin, rifampin, and enalapril (PMID:11748225, PMID:15652233, PMID:16627748). Its liver-restricted expression is driven by HNF1α binding to the minimal promoter (PMID:11483603) and is further controlled by direct transcriptional regulation through FXR and LXRα response elements (PMID:20827719, PMID:32292349), while post-translationally its activity depends on LYN/Src-family tyrosine kinase phosphorylation at Tyr645, the site through which tyrosine kinase inhibitors noncompetitively suppress transport (PMID:33664059). Common and rare missense variants modulate function through distinct mechanisms: L193R causes intracellular retention and abolishes maturation, the *15 haplotype (N130D+V174A) reduces normalized Vmax to under 30% of wild-type while remaining surface-localized, and folding/expression effects across the variant landscape reduce protein abundance — changes that lower hepatic clearance and increase systemic drug exposure in vivo (PMID:12196548, PMID:15564882, PMID:33658230, PMID:12811365).

Mechanistic history

Synthesis pass · year-by-year structured walk · 12 steps
  1. 2000 High

    Established OATP1B1 as a high-affinity hepatic uptake transporter for endogenous organic anions, defining its substrate class biochemically.

    Evidence Radiolabeled uptake kinetics for bilirubin conjugates and sulfobromophthalein in stably transfected HEK293 cells

    PMID:11134001

    Open questions at the time
    • Bilirubin transport role was later challenged
    • Did not address membrane polarity or in vivo relevance
  2. 2001 High

    Resolved where the transporter acts and why it is liver-specific, anchoring OATP1B1 to the sinusoidal membrane and identifying HNF1α as the driver of its tissue-restricted expression.

    Evidence Immunolocalization in human liver plus DNase footprinting, EMSA, and reporter assays in hepatic cell lines

    PMID:11483603

    Open questions at the time
    • Did not address additional transcriptional regulators identified later
    • No post-translational regulation examined
  3. 2001 High

    Demonstrated that OATP1B1 functions as the uptake arm of a coupled vectorial transport system, working with MRP2 to move organic anions basal-to-apical across hepatocytes.

    Evidence Directional flux assays in OATP1B1/MRP2 double-transfected MDCK II monolayers

    PMID:11748225

    Open questions at the time
    • Reconstituted in heterologous epithelium, not native hepatocytes
    • Stoichiometry of coupling not defined
  4. 2002 High

    Distinguished folding/trafficking defects from intrinsic activity defects among variants, showing L193R is retained intracellularly while *15 (N130D+V174A) is surface-localized but functionally impaired.

    Evidence Site-directed mutagenesis, immunofluorescence localization, and uptake kinetics with protein normalization in MDCK II and HEK293 cells

    PMID:12130747 PMID:12196548 PMID:15564882

    Open questions at the time
    • Mechanism by which V174A lowers turnover not resolved at structural level
    • Single-variant heterologous systems
  5. 2003 Medium

    Extended the substrate range to clinically important drugs and linked variant transport defects to altered drug disposition in humans, establishing pharmacogenetic relevance.

    Evidence Rifampin uptake and PXR transactivation assays in HeLa cells; pravastatin pharmacokinetic study in genotyped volunteers

    PMID:12490595 PMID:12811365

    Open questions at the time
    • Clinical PK study was modest in size, single lab
    • In vivo causality not isolated from other clearance routes
  6. 2003 Medium

    Challenged the bilirubin-transporter assignment, with replicated negative uptake data questioning whether OATP1B1 is sufficient for bilirubin transport.

    Evidence Inducible stable transfection and bilirubin/BSP uptake assays in two cell lines

    PMID:12670950

    Open questions at the time
    • Discrepancy with earlier positive bilirubin findings unresolved
    • Possible differences in substrate presentation or cofactors not examined
  7. 2004 High

    Defined the mechanistic basis of a clinical drug-drug interaction, showing a glucuronide metabolite inhibits OATP1B1-mediated statin uptake.

    Evidence Cerivastatin uptake inhibition by gemfibrozil and its glucuronide in OATP2-expressing cells, with parallel CYP2C8 inhibition

    PMID:15194707

    Open questions at the time
    • Relative contribution of transport vs metabolism inhibition in vivo not partitioned in this study
  8. 2010 High

    Expanded transcriptional control beyond HNF1α, identifying FXR and LXRα as direct nuclear-receptor regulators of OATP1B1 expression.

    Evidence Promoter reporter assays, ChIP, siRNA, and ligand treatment of primary human hepatocytes

    PMID:20827719

    Open questions at the time
    • Interplay between HNF1α and nuclear-receptor inputs not integrated
    • Physiological stimuli driving these receptors in vivo not defined here
  9. 2013 High

    Provided in vivo proof that OATP1B1 governs hepatic uptake and systemic clearance of statins and drug glucuronides, moving beyond cell-based inference.

    Evidence Oatp1a/1b-knockout and liver-specific OATP1B1-humanized mice with statin and sorafenib-glucuronide pharmacokinetics

    PMID:23340295 PMID:24194513

    Open questions at the time
    • Mouse humanization is partial; quantitative scaling to human uncertain
    • Contribution of other OATP isoforms not fully separated
  10. 2017 High

    Identified post-translational kinase control of transporter activity, mapping LYN-mediated phosphorylation at Tyr645 as a regulatory node exploited by tyrosine kinase inhibitors.

    Evidence Phosphoproteomics, siRNA kinome screen, mutagenesis, and in vivo rosuvastatin PK with nilotinib

    PMID:33664059

    Open questions at the time
    • Upstream signals activating LYN toward OATP1B1 unknown
    • How Y645 phosphorylation alters transport mechanistically not resolved
  11. 2020 Medium

    Revealed that OATP1B1 hetero-oligomerizes with OATP1B3, modulating membrane expression and turnover and complicating single-transporter functional estimates.

    Evidence Co-immunoprecipitation, proximity ligation assay in cells and human liver, and uptake assays

    PMID:32482756

    Open questions at the time
    • Functional impact on OATP1B1 substrates specifically not quantified
    • Stoichiometry and physiological extent of oligomerization unclear
  12. 2022 Medium

    Systematically separated folding/expression effects from intrinsic activity effects across rare variants, refining the genotype-to-function map.

    Evidence Deep mutational scanning and variant uptake assays with QTAP proteomics in HEK293 cells

    PMID:33658230 PMID:35752377

    Open questions at the time
    • High-throughput membrane-protein assays carry expression-system caveats
    • Clinical translation of many rare variants untested

Open questions

Synthesis pass · forward-looking unresolved questions
  • How transcriptional (HNF1α/FXR/LXRα), post-translational (LYN/Y645), and oligomerization inputs are integrated to set hepatic OATP1B1 transport capacity in vivo remains unresolved.
  • No unified regulatory model connecting transcription, phosphorylation, and oligomerization
  • Structural basis of substrate recognition and transport cycle not established in the corpus

Mechanism profile

Synthesis pass · controlled-vocabulary classification · explore literature graph →
Molecular activity
GO:0005215 transporter activity 7
Localization
GO:0005886 plasma membrane 4
Pathway
R-HSA-382551 Transport of small molecules 3 R-HSA-9748784 Drug ADME 3
Partners
ABCC2LYNMRP2SLCO1B3

Evidence

Reading pass · 28 per-paper findings extracted from the source corpus
Year Finding Method Journal Conf PMIDs
2000 OATP1B1 (SLC21A6) mediates high-affinity hepatic uptake of bilirubin and its glucuronate conjugates; HEK293 cells stably expressing recombinant OATP1B1 showed uptake of monoglucuronosyl bilirubin, bisglucuronosyl bilirubin, and sulfobromophthalein with Km values of 0.10, 0.28, and 0.14 µM respectively; transport of unconjugated bilirubin from albumin was also demonstrated and was not mediated by OATP8. Stable transfection of HEK293 cells with recombinant OATP1B1; radiolabeled substrate uptake assays; kinetic analysis The Journal of biological chemistry High 11134001
2001 OATP1B1 (SLC21A6) is localized to the basolateral (sinusoidal) membrane of human hepatocytes and its liver-specific expression is driven by the hepatocyte nuclear factor 1 alpha (HNF1α) binding to a functional element in the minimal promoter; mutation of the HNF1 site abolished promoter function. DNase I footprint analysis, electrophoretic mobility shift assay (EMSA), reporter gene assays with HNF1α co-expression in HepG2, Huh7, and HeLa cells; promoter deletion constructs The Journal of biological chemistry High 11483603
2001 OATP1B1 and MRP2 together mediate vectorial (basolateral-to-apical) transcellular transport of organic anions including 17β-estradiol 17β-D-glucuronide, pravastatin, and leukotriene C4 across a double-transfected MDCK II cell monolayer; Km values for E2-17βG and pravastatin for basal-to-apical flux were 27.9 and 24.3 µM respectively. Double-transfected MDCK II cell monolayer expressing OATP1B1 (basal) and MRP2 (apical); directional flux assays with radiolabeled substrates The Journal of biological chemistry High 11748225
2002 The naturally occurring OATP1B1 mutation L193R (SLC21A6) causes intracellular retention of the protein and abolishes organic anion transport; the mutation impairs protein maturation. In contrast, polymorphic variants N130D (P155T) were sorted correctly to the lateral membrane but showed altered transport for cholyltaurine and 17β-glucuronosyl estradiol. Stably transfected MDCK II cells with mutant SLC21A6 constructs; immunofluorescence microscopy for localization; radiolabeled uptake assays The Journal of biological chemistry High 12196548
2002 Functional analysis in HEK293 cells of OATP1B1 alleles showed that the OATP1B1*15 variant (N130D + V174A combined) has a normalized Vmax for estrone-3-sulfate uptake reduced to less than 30% of wild-type, while the individual *1b (N130D) and *5 (V174A) variants did not significantly alter Km or corrected Vmax. Stably transfected HEK293 cells expressing OATP1B1 alleles; radiolabeled estrone-3-sulfate uptake kinetics; Western blot normalization of Vmax The Journal of pharmacology and experimental therapeutics High 12130747
2003 OATP1B1 (OATP-C, SLC21A6) is the major hepatic uptake transporter for rifampin; HeLa cells expressing OATP-C showed greater affinity and capacity for rifampin transport than OATP8. OATP-C allelic variants had markedly decreased rifampin transport activity. OATP-C expression potentiated PXR reporter gene activity by increasing intracellular rifampin retention. Transient expression of OATP-C and OATP8 in HeLa cells; radiolabeled rifampin uptake assays; cell-based PXR transactivation reporter assay The Journal of pharmacology and experimental therapeutics High 12490595
2003 OATP1B1 (OATP-C) polymorphisms, particularly the T521C (Val174Ala) variant in the *15 allele, are associated with reduced non-renal clearance of pravastatin in vivo; subjects homozygous for *15 showed drastically reduced nonrenal clearance compared to *1b/*1b subjects. Clinical pharmacokinetic study with pravastatin as probe drug in 23 healthy volunteers genotyped for OATP-C polymorphisms; plasma/urine pharmacokinetic analysis Clinical pharmacology and therapeutics Medium 12811365
2003 OATP-C (SLC21A6) mRNA is detectable only in human liver and not in human placenta at term, while OATP-8 and OATP-A are expressed in placenta. Xenopus oocytes injected with OATP-C mRNA transported unconjugated bilirubin (UCB) with higher affinity than OATP-8; Km for UCB transport was lower for OATP-C than OATP-8. Real-time RT-PCR for tissue distribution; Xenopus laevis oocyte expression system with radiolabeled substrate transport assays; kinetic analysis The Biochemical journal Medium 12568656
2003 SLC21A6 (OATP1B1) is not sufficient for bilirubin transport: stably transfected HeLa and HEK293 cells expressing OATP2 showed substantial sulfobromophthalein uptake but no significant increase in bilirubin uptake compared to uninduced controls, challenging the proposed role of OATP1B1 as a bilirubin transporter. Inducible stable transfection of HeLa cells and HEK293 cells with OATP2; radiolabeled bilirubin and sulfobromophthalein uptake assays; immunoblot confirmation of protein expression The Journal of biological chemistry Medium 12670950
2003 SLC21A6 (OATP1B1) and SLC21A8 (OATP8) are both localized to the basolateral membrane of human hepatocytes, as established by immunofluorescence microscopy and immunoprecipitation with newly generated monoclonal antibodies. Both proteins are differentially expressed in hepatocellular carcinoma. Generation and characterization of monoclonal antibodies; immunoblot, immunoprecipitation, immunofluorescence microscopy in human liver and HCC samples Laboratory investigation Medium 12695556
2004 Gemfibrozil and its glucuronide metabolite (GEM-1-O-glu) inhibit OATP1B1 (OATP2)-mediated uptake of cerivastatin with IC50 values of 72 and 24 µM respectively in OATP2-expressing cells; both also inhibited CYP2C8-mediated metabolism, with GEM-1-O-glu being the primary driver of the clinical drug-drug interaction between cerivastatin and gemfibrozil. OATP2-expressing cell uptake inhibition assays with radiolabeled cerivastatin; CYP2C8 inhibition assays in P450 expression systems The Journal of pharmacology and experimental therapeutics High 15194707
2004 Functional analysis of OATP1B1 SNP variants in stably transfected HEK293 cells showed that OATP1B1*15 (N130D + V174A) has normalized Vmax reduced to less than 30% of wild-type *1a; *1b (N130D alone) and *5 (V174A alone) show similar transport activity to wild-type. All variants are predominantly localized on the cell surface. Stably transfected HEK293 cells; uptake kinetics of radiolabeled E2-17βG; Western blot for protein expression normalization; immunofluorescence for subcellular localization Pharmacogenetics High 15564882
2004 OATP1B1 together with MRP2 mediates transcellular transport of rifampin across LLC-PK1 cell monolayers co-expressing both transporters; directional transport was demonstrated for the first time for rifampin through this transporter pair. Porcine LLC-PK1 cells stably co-expressing OATP1B1 and MRP2; directional transport assays across monolayers Biochemical pharmacology Medium 15652233
2005 Multiple naturally occurring flavonoids inhibit OATP1B1-mediated transport of DHEAS in a concentration-dependent manner in OATP1B1-expressing HeLa cells; biochanin A is among the most potent inhibitors (IC50 ~11 µM) and acts via a noncompetitive mechanism (Ki ~10 µM). Biochanin A is not itself a substrate of OATP1B1. OATP1B1-expressing HeLa cells; radiolabeled DHEAS uptake inhibition assays; kinetic analysis of inhibition mechanism Drug metabolism and disposition Medium 16081670
2006 OATP1B1 mediates hepatic uptake of enalapril with a Km of ~262 µM in HEK293 cells; double-transfected MDCK II cells expressing OATP1B1 and MRP2 showed significantly higher sinusoidal-to-canalicular vectorial flux of enalapril, demonstrating the coupled role of these two transporters in hepatic enalapril disposition. HEK293 cells transfected with OATP1B1 or OATP1B3; radiolabeled enalapril uptake kinetics; double-transfected MDCK II cells with OATP1B1 and MRP2; Transwell directional flux assays The Journal of pharmacology and experimental therapeutics High 16627748
2010 OATP1B1 transcription is under dual nuclear receptor control: LXRα and FXR directly regulate OATP1B1 gene expression. Two functional FXR response elements and one LXRα response element were identified in the OATP1B1 promoter; direct receptor-promoter binding was confirmed by chromatin immunoprecipitation. LXRα or FXR agonists induced OATP1B1 mRNA in primary human hepatocytes, whereas PXR and CAR agonists did not. Promoter deletion/reporter gene assays; chromatin immunoprecipitation (ChIP); siRNA knockdown; primary human hepatocyte treatment with nuclear receptor ligands Hepatology High 20827719
2010 Maraviroc is a substrate of OATP1B1 with a Km of 33.9 µM, as demonstrated in a Xenopus laevis oocyte expression system. The SLCO1B1 521T>C polymorphism was associated with higher maraviroc trough plasma concentrations in HIV-infected patients. Xenopus laevis oocyte heterologous expression system; LC-MS/MS quantification; clinical pharmacokinetic analysis Pharmacogenetics and genomics Medium 21217360
2010 Flavopiridol and its glucuronide metabolite are substrates of OATP1B1, as demonstrated in transiently transfected HEK-293 and MDCK-II cells. SLCO1B1 polymorphisms were associated with flavopiridol pharmacokinetics in a population pharmacokinetic model. Transient transfection of HEK-293 and MDCK-II cells with SLCO1B1; uptake assays; population pharmacokinetic modeling from clinical data PloS one Medium 21072184
2013 OATP1B1 transports sorafenib-glucuronide (10.6-fold over control) in HEK293 cells stably transfected with OATP1B1; plasma levels of sorafenib-glucuronide were increased >8-fold in Oatp1b2-knockout mice. Introduction of human OATP1B1 in knockout mice partially restored clearance of sorafenib-glucuronide. Stably transfected HEK293 cells with OATP1B1; radiolabeled/LC-MS uptake assays; Oatp1b2-knockout and humanized OATP1B1-transgenic mice pharmacokinetic studies Clinical cancer research High 23340295
2013 In vivo studies using oatp1a/1b-knockout and liver-specific OATP1B1-humanized mice established that OATP1B1 mediates hepatic uptake and clearance of statins (pravastatin, atorvastatin, simvastatin); oatp1a/1b-knockout mice showed up to 115-fold increased oral drug exposure and up to 196-fold lower hepatic drug distribution, partially restored by OATP1B1 knockin. Oatp1a/1b-knockout and liver-specific OATP1B1-humanized transgenic mice; pharmacokinetic studies with IV and oral administration; quantitative proteomics Drug metabolism and disposition High 24194513
2014 OATP1B1 mediates hepatic uptake of docetaxel in vivo; liver-specific expression of OATP1B1 in Oatp1a/1b-knockout mice nearly completely rescued the increased plasma levels of docetaxel seen in knockout mice after IV administration. Oatp1a/1b-knockout mice and liver-specific OATP1B1-humanized transgenic mice; in vivo pharmacokinetic studies with docetaxel; liver-to-plasma ratio measurements International journal of cancer High 24825069
2014 OATP1B1 mediates uptake of nilotinib (Km 10.14 µM) and vandetanib (Km 2.72 µM) in CHO cells transfected with OATP1B1; canertinib, erlotinib, and pazopanib did not show substrate specificity toward OATP1B1. CHO cells transfected with OATP1B1; concentration-dependent cellular accumulation assays; Michaelis-Menten kinetic analysis Drug metabolism and drug interactions Medium 24643910
2017 OATP1B1 function is regulated by tyrosine kinase-mediated phosphorylation at tyrosine residue 645. Inhibition of OATP1B1 by tyrosine kinase inhibitors (TKIs) such as nilotinib is predominantly noncompetitive and is associated with reduced phosphorylation at Y645. The Src kinase LYN was identified as a regulator of OATP1B1 activity using a siRNA kinome screen (779 kinases). Overexpressing HEK293 cells and primary hepatocytes; TKI transport inhibition assays; LC/MS-MS phosphoproteomics; siRNA kinome screen; in vivo rosuvastatin PK with nilotinib in mice Clinical cancer research High 33664059
2017 OATP1B1 function is affected by SLCO1B1 variants altering protein folding and degradation; deep mutational scanning of 137 SLCO1B1 missense variants identified 6 variants with <25% and 12 with ~50% of wild-type protein expression, with functional validation by transporter assays. Deep mutational scanning (DMS) using landing pad cell-based system with GFP fusion and FACS; next-generation sequencing; functional transport validation assays Drug metabolism and disposition Medium 33658230
2019 Preincubation with rifampicin and dasatinib potentiates inhibitory effects on OATP1B1-mediated transport by reducing Ki values (rifampicin 3-fold, dasatinib 2.1-fold for OATP1B1), without affecting plasma membrane localization of GFP-tagged OATP1B1 in HEK293 cells, as confirmed by time-lapse confocal microscopy. HEK293 stable cell lines with GFP-OATP1B1; transport inhibition assays with preincubation; Ki determination; confocal microscopy; human sandwich-cultured hepatocytes Journal of pharmaceutical sciences Medium 28373111
2020 Coexpression of OATP1B3 with OATP1B1 in HEK293 cells increases OATP1B3 plasma membrane expression while decreasing its apparent turnover rate, suggesting hetero-oligomerization modulates OATP1B3 function; this implies that single-transporter overexpression systems may over- or underestimate OATP1B1-related function. Co-immunoprecipitation; proximity ligation assay in HEK293 cells and human liver sections; membrane expression quantification; cholecystokinin-8 uptake assays Drug metabolism and disposition Medium 32482756
2020 Berberine promotes OATP1B1 expression and rosuvastatin uptake in HepG2 cells by inducing nuclear translocation and activation of FXR and LXRα; siRNA silencing of FXR or LXRα attenuated berberine-induced OATP1B1 expression. HepG2 cell treatment with berberine; rosuvastatin uptake assay; dual-luciferase reporter assay; siRNA knockdown of FXR and LXRα; Western blot of cytoplasm/nuclear fractions Frontiers in pharmacology Medium 32292349
2022 Functional analysis of rare SLCO1B1 variants in HEK293 cells showed that R57Q impairs both DCF and rosuvastatin transport without reducing protein expression, while R253Q reduces DCF uptake and increases rosuvastatin Km. N130D and N151S do not alter activity but increase protein expression. QTAP proteomics confirmed OATP1B1 protein abundance differences among variants. HEK293 cells overexpressing SLCO1B1 variants; uptake assays with DCF and rosuvastatin; LC-MS/MS-based QTAP proteomics; pharmacokinetic simulations European journal of pharmaceutical sciences Medium 35752377

Source papers

Stage 0 corpus · 100 papers · ranked by NIH iCite citations
Year Title Journal Citations PMID
2008 SLCO1B1 variants and statin-induced myopathy--a genomewide study. The New England journal of medicine 1512 18650507
2003 Polymorphisms of OATP-C (SLC21A6) and OAT3 (SLC22A8) genes: consequences for pravastatin pharmacokinetics. Clinical pharmacology and therapeutics 397 12811365
2000 Hepatic uptake of bilirubin and its conjugates by the human organic anion transporter SLC21A6. The Journal of biological chemistry 386 11134001
2004 High plasma pravastatin concentrations are associated with single nucleotide polymorphisms and haplotypes of organic anion transporting polypeptide-C (OATP-C, SLCO1B1). Pharmacogenetics 341 15226675
2004 Gemfibrozil and its glucuronide inhibit the organic anion transporting polypeptide 2 (OATP2/OATP1B1:SLC21A6)-mediated hepatic uptake and CYP2C8-mediated metabolism of cerivastatin: analysis of the mechanism of the clinically relevant drug-drug interaction between cerivastatin and gemfibrozil. The Journal of pharmacology and experimental therapeutics 295 15194707
2022 The Clinical Pharmacogenetics Implementation Consortium Guideline for SLCO1B1, ABCG2, and CYP2C9 genotypes and Statin-Associated Musculoskeletal Symptoms. Clinical pharmacology and therapeutics 266 35152405
2003 Human organic anion transporting polypeptide-C (SLC21A6) is a major determinant of rifampin-mediated pregnane X receptor activation. The Journal of pharmacology and experimental therapeutics 256 12490595
2002 Genetic polymorphisms of human organic anion transporters OATP-C (SLC21A6) and OATP-B (SLC21A9): allele frequencies in the Japanese population and functional analysis. The Journal of pharmacology and experimental therapeutics 255 12130747
2004 Evidence for inverse effects of OATP-C (SLC21A6) 5 and 1b haplotypes on pravastatin kinetics. Clinical pharmacology and therapeutics 231 15116054
2009 Genetic polymorphisms of uptake (OATP1B1, 1B3) and efflux (MRP2, BCRP) transporters: implications for inter-individual differences in the pharmacokinetics and pharmacodynamics of statins and other clinically relevant drugs. Expert opinion on drug metabolism & toxicology 160 19442037
2014 The roles of MRP2, MRP3, OATP1B1, and OATP1B3 in conjugated hyperbilirubinemia. Drug metabolism and disposition: the biological fate of chemicals 156 24459177
2001 Transcellular transport of organic anions across a double-transfected Madin-Darby canine kidney II cell monolayer expressing both human organic anion-transporting polypeptide (OATP2/SLC21A6) and Multidrug resistance-associated protein 2 (MRP2/ABCC2). The Journal of biological chemistry 147 11748225
2013 Contribution of OATP1B1 and OATP1B3 to the disposition of sorafenib and sorafenib-glucuronide. Clinical cancer research : an official journal of the American Association for Cancer Research 142 23340295
2003 Role of organic anion-transporting polypeptides, OATP-A, OATP-C and OATP-8, in the human placenta-maternal liver tandem excretory pathway for foetal bilirubin. The Biochemical journal 133 12568656
2009 The influence of SLCO1B1 (OATP1B1) gene polymorphisms on response to statin therapy. The pharmacogenomics journal 127 19884908
2010 Effects of tuberculosis, race, and human gene SLCO1B1 polymorphisms on rifampin concentrations. Antimicrobial agents and chemotherapy 126 20660695
2005 Flavonoids as a novel class of human organic anion-transporting polypeptide OATP1B1 (OATP-C) modulators. Drug metabolism and disposition: the biological fate of chemicals 124 16081670
2004 Functional analysis of single nucleotide polymorphisms of hepatic organic anion transporter OATP1B1 (OATP-C). Pharmacogenetics 124 15564882
2001 Characterization of the human OATP-C (SLC21A6) gene promoter and regulation of liver-specific OATP genes by hepatocyte nuclear factor 1 alpha. The Journal of biological chemistry 120 11483603
2013 SLCO1B1 genetic variant associated with statin-induced myopathy: a proof-of-concept study using the clinical practice research datalink. Clinical pharmacology and therapeutics 110 23942138
2002 A naturally occurring mutation in the SLC21A6 gene causing impaired membrane localization of the hepatocyte uptake transporter. The Journal of biological chemistry 108 12196548
2003 Detection of the human organic anion transporters SLC21A6 (OATP2) and SLC21A8 (OATP8) in liver and hepatocellular carcinoma. Laboratory investigation; a journal of technical methods and pathology 102 12695556
2004 Effect of genetic polymorphism of OATP-C (SLCO1B1) on lipid-lowering response to HMG-CoA reductase inhibitors. Drug metabolism and pharmacokinetics 97 15548849
2003 Semi quantitative expression analysis of MDR3, FIC1, BSEP, OATP-A, OATP-C,OATP-D, OATP-E and NTCP gene transcripts in 1st and 3rd trimester human placenta. Placenta 80 12495658
2013 Utility of Oatp1a/1b-knockout and OATP1B1/3-humanized mice in the study of OATP-mediated pharmacokinetics and tissue distribution: case studies with pravastatin, atorvastatin, simvastatin, and carboxydichlorofluorescein. Drug metabolism and disposition: the biological fate of chemicals 77 24194513
2012 Ethnic variability in the plasma exposures of OATP1B1 substrates such as HMG-CoA reductase inhibitors: a kinetic consideration of its mechanism. Clinical pharmacology and therapeutics 76 23443754
2001 Expression of hepatic transporters OATP-C and MRP2 in primary sclerosing cholangitis. Liver 75 11454187
2017 Interindividual and interethnic variability in drug disposition: polymorphisms in organic anion transporting polypeptide 1B1 (OATP1B1; SLCO1B1). British journal of clinical pharmacology 74 27936281
2006 Vectorial transport of enalapril by Oatp1a1/Mrp2 and OATP1B1 and OATP1B3/MRP2 in rat and human livers. The Journal of pharmacology and experimental therapeutics 71 16627748
2011 The role of OATP1B1 and BCRP in pharmacokinetics and DDI of novel statins. Cardiovascular therapeutics 64 21884024
2010 Liver X receptor α and farnesoid X receptor are major transcriptional regulators of OATP1B1. Hepatology (Baltimore, Md.) 63 20827719
2015 OATP1B1 and tumour OATP1B3 modulate exposure, toxicity, and survival after irinotecan-based chemotherapy. British journal of cancer 61 25611302
2014 Selectivity and potency of microcystin congeners against OATP1B1 and OATP1B3 expressing cancer cells. PloS one 57 24614281
2014 Association between statin-induced creatine kinase elevation and genetic polymorphisms in SLCO1B1, ABCB1 and ABCG2. European journal of clinical pharmacology 54 24595600
2022 PharmVar GeneFocus: SLCO1B1. Clinical pharmacology and therapeutics 52 35797228
2013 OATP1B1-related drug-drug and drug-gene interactions as potential risk factors for cerivastatin-induced rhabdomyolysis. Pharmacogenetics and genomics 51 23652407
2003 The human organic anion transport protein SLC21A6 is not sufficient for bilirubin transport. The Journal of biological chemistry 51 12670950
2014 Human OATP1B1, OATP1B3 and OATP1A2 can mediate the in vivo uptake and clearance of docetaxel. International journal of cancer 50 24825069
2016 CYP2C8 and SLCO1B1 Variants and Therapeutic Response to Thiazolidinediones in Patients With Type 2 Diabetes. Diabetes care 49 27271184
2015 Association Between SLCO1B1 Gene T521C Polymorphism and Statin-Related Myopathy Risk: A Meta-Analysis of Case-Control Studies. Medicine 49 26376374
2013 SLCO1B1 Polymorphisms and Statin-Induced Myopathy. PLoS currents 49 24459608
2014 Inhibition of OATP1B1 by tyrosine kinase inhibitors: in vitro-in vivo correlations. British journal of cancer 48 24398510
2011 Pharmacogenetics of OATP transporters reveals that SLCO1B1 c.388A>G variant is determinant of increased atorvastatin response. International journal of molecular sciences 48 22016628
2011 Impact of SLCO1B1 (OATP1B1) and ABCG2 (BCRP) genetic polymorphisms and inhibition on LDL-C lowering and myopathy of statins. Xenobiotica; the fate of foreign compounds in biological systems 47 21425956
2022 A comprehensive pharmacogenomic study indicates roles for SLCO1B1, ABCG2 and SLCO2B1 in rosuvastatin pharmacokinetics. British journal of clinical pharmacology 41 35942816
2021 Regulation of OATP1B1 Function by Tyrosine Kinase-mediated Phosphorylation. Clinical cancer research : an official journal of the American Association for Cancer Research 41 33664059
2018 Effects of Delivering SLCO1B1 Pharmacogenetic Information in Randomized Trial and Observational Settings. Circulation. Genomic and precision medicine 40 30354330
2010 Flavopiridol pharmacogenetics: clinical and functional evidence for the role of SLCO1B1/OATP1B1 in flavopiridol disposition. PloS one 39 21072184
2007 Pharmacogenetics of SLCO1B1: haplotypes, htSNPs and hepatic expression in three distinct Asian populations. European journal of clinical pharmacology 39 17415554
2019 Physiologically Based Pharmacokinetic Models for Prediction of Complex CYP2C8 and OATP1B1 (SLCO1B1) Drug-Drug-Gene Interactions: A Modeling Network of Gemfibrozil, Repaglinide, Pioglitazone, Rifampicin, Clarithromycin and Itraconazole. Clinical pharmacokinetics 38 31129789
2010 SLCO1B1 polymorphism and oral antidiabetic drugs. Basic & clinical pharmacology & toxicology 38 20406215
2017 Pretreatment With Rifampicin and Tyrosine Kinase Inhibitor Dasatinib Potentiates the Inhibitory Effects Toward OATP1B1- and OATP1B3-Mediated Transport. Journal of pharmaceutical sciences 37 28373111
2016 An integrated pharmacokinetic/pharmacogenomic analysis of ABCB1 and SLCO1B1 polymorphisms on edoxaban exposure. The pharmacogenomics journal 37 27897269
2020 Role of OATP1B1 and OATP1B3 in Drug-Drug Interactions Mediated by Tyrosine Kinase Inhibitors. Pharmaceutics 36 32916864
2018 Impact of SLCO1B1 Genotype on Pediatric Simvastatin Acid Pharmacokinetics. Journal of clinical pharmacology 36 29469964
2014 Role of OATP-1B1 and/or OATP-1B3 in hepatic disposition of tyrosine kinase inhibitors. Drug metabolism and drug interactions 36 24643910
2021 A systematic review and meta-analysis of genotype-based and individualized data analysis of SLCO1B1 gene and statin-induced myopathy. The pharmacogenomics journal 35 33608664
2015 SLCO1B1 polymorphism markedly affects the pharmacokinetics of lovastatin acid. Pharmacogenetics and genomics 35 26020121
2010 Maraviroc is a substrate for OATP1B1 in vitro and maraviroc plasma concentrations are influenced by SLCO1B1 521 T>C polymorphism. Pharmacogenetics and genomics 35 21217360
2019 Association of genetic polymorphisms of CYP2E1, NAT2, GST and SLCO1B1 with the risk of anti-tuberculosis drug-induced liver injury: a systematic review and meta-analysis. BMJ open 34 31375612
2011 Frequency of the SLCO1B1 388A>G and the 521T>C polymorphism in Tanzania genotyped by a new LightCycler®-based method. European journal of clinical pharmacology 32 21630030
2009 Construction of triple-transfected cells [organic anion-transporting polypeptide (OATP) 1B1/multidrug resistance-associated protein (MRP) 2/MRP3 and OATP1B1/MRP2/MRP4] for analysis of the sinusoidal function of MRP3 and MRP4. Drug metabolism and disposition: the biological fate of chemicals 31 19628752
2014 Inhibition of OATP-1B1 and OATP-1B3 by tyrosine kinase inhibitors. Drug metabolism and drug interactions 29 24807167
2004 Directional trans-epithelial transport of organic anions in porcine LLC-PK1 cells that co-express human OATP1B1 (OATP-C) and MRP2. Biochemical pharmacology 27 15652233
2012 SLCO1B1 gene variability influences lipid-lowering efficacy on simvastatin therapy in Southern Brazilians. Clinical chemistry and laboratory medicine 26 22505549
2021 SLCO1B1 Phenotype and CYP3A5 Polymorphism Significantly Affect Atorvastatin Bioavailability. Journal of personalized medicine 25 33805706
2019 Influence of OATP1B1 and BCRP polymorphisms on the pharmacokinetics and pharmacodynamics of rosuvastatin in elderly and young Korean subjects. Scientific reports 25 31857620
2019 Preincubation With Everolimus and Sirolimus Reduces Organic Anion-Transporting Polypeptide (OATP)1B1- and 1B3-Mediated Transport Independently of mTOR Kinase Inhibition: Implication in Assessing OATP1B1- and OATP1B3-Mediated Drug-Drug Interactions. Journal of pharmaceutical sciences 24 31047942
2016 Polymorphisms in SLCO1B1 and UGT1A1 are associated with sorafenib-induced toxicity. Pharmacogenomics 24 27533851
2016 SLCO1B1 Gene Variations Among Tanzanians, Ethiopians, and Europeans: Relevance for African and Worldwide Precision Medicine. Omics : a journal of integrative biology 24 27631193
2015 SLCO1B1 Variants and Angiotensin Converting Enzyme Inhibitor (Enalapril)-Induced Cough: a Pharmacogenetic Study. Scientific reports 24 26607661
2021 SLCO1B1: Application and Limitations of Deep Mutational Scanning for Genomic Missense Variant Function. Drug metabolism and disposition: the biological fate of chemicals 22 33658230
2018 CYP2C9 and OATP1B1 genetic polymorphisms affect the metabolism and transport of glimepiride and gliclazide. Scientific reports 22 30030468
2011 CYP3A5, ABCB1, and SLCO1B1 polymorphisms and pharmacokinetics and virologic outcome of lopinavir/ritonavir in HIV-infected children. Therapeutic drug monitoring 22 21743379
2020 Fluorescent probes for the dual investigation of MRP2 and OATP1B1 function and drug interactions. European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences 21 32473861
2017 Effect of OATP1B1 genetic polymorphism on the uptake of tamoxifen and its metabolite, endoxifen. Oncology reports 18 28627631
2015 SLCO1B1 c.388A>G Polymorphism Is Associated with HDL-C Levels in Response to Atorvastatin in Chilean Individuals. International journal of molecular sciences 18 26334272
2006 BacMam recombinant baculovirus in transporter expression: a study of BCRP and OATP1B1. Protein expression and purification 18 16481201
2022 Functional in vitro characterization of SLCO1B1 variants and simulation of the clinical pharmacokinetic impact of impaired OATP1B1 function. European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences 16 35752377
2014 Role of SLCO1B1, ABCB1, and CHRNA1 gene polymorphisms on the efficacy of rocuronium in Chinese patients. Journal of clinical pharmacology 16 25279974
2020 Effects of ABCG2 and SLCO1B1 gene variants on inflammation markers in patients with hypercholesterolemia and diabetes mellitus treated with rosuvastatin. European journal of clinical pharmacology 15 32361904
2020 Association of SLCO1B1 c.521T>C (rs4149056) with discontinuation of atorvastatin due to statin-associated muscle symptoms. Pharmacogenetics and genomics 15 32453264
2020 OATP1B3 Expression and Function is Modulated by Coexpression with OCT1, OATP1B1, and NTCP. Drug metabolism and disposition: the biological fate of chemicals 15 32482756
2017 No Effect of SLCO1B1 and CYP3A4/5 Polymorphisms on the Pharmacokinetics and Pharmacodynamics of Ticagrelor in Healthy Chinese Male Subjects. Biological & pharmaceutical bulletin 15 28049954
2015 Generation of Bayesian prediction models for OATP-mediated drug-drug interactions based on inhibition screen of OATP1B1, OATP1B1∗15 and OATP1B3. European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences 15 25603031
2014 Expression and activity of ABCG2, but not ABCB1 or OATP1B1, are associated with cholesterol levels: evidence from in vitro and in vivo experiments. Pharmacogenomics 15 25084202
2008 Genetic variations of the SLCO1B1 gene in the Chinese, Malay and Indian populations of Singapore. Drug metabolism and pharmacokinetics 15 19122343
2023 Real-world pharmacogenetics of statin intolerance: effects of SLCO1B1, ABCG2 , and CYP2C9 variants. Pharmacogenetics and genomics 14 37490620
2020 Effect of Rifampin-Mediated OATP1B1 and OATP1B3 Transporter Inhibition on the Pharmacokinetics of the P2Y12 Receptor Antagonist Selatogrel. Clinical and translational science 14 32166864
2023 A gene risk score using missense variants in SLCO1B1 is associated with earlier onset statin intolerance. European heart journal. Cardiovascular pharmacotherapy 13 37253618
2020 Berberine Promotes OATP1B1 Expression and Rosuvastatin Uptake by Inducing Nuclear Translocation of FXR and LXRα. Frontiers in pharmacology 13 32292349
2019 Combined Effects of UGT1A1 and SLCO1B1 Variants on Chinese Adult Mild Unconjugated Hyperbilirubinemia. Frontiers in genetics 13 31737051
2015 Meta-Analysis of the SLCO1B1 c.521T>C Variant Reveals Slight Influence on the Lipid-Lowering Efficacy of Statins. Annals of laboratory medicine 12 25932441
2015 Influence of SLCO1B1 polymorphism on maintenance therapy for childhood leukemia. Pediatrics international : official journal of the Japan Pediatric Society 12 25939871
2023 Mechanistic in vitro studies indicate that the clinical drug-drug interactions between protease inhibitors and rosuvastatin are driven by inhibition of intestinal BCRP and hepatic OATP1B1 with minimal contribution from OATP1B3, NTCP and OAT3. Pharmacology research & perspectives 11 36811234
2021 SLCO1B1 *15 allele is associated with methotrexate-induced nausea in pediatric patients with inflammatory bowel disease. Clinical and translational science 11 34423897
2018 Associations among regorafenib concentrations, severe adverse reactions, and ABCG2 and OATP1B1 polymorphisms. Cancer chemotherapy and pharmacology 11 30368586
2017 SLCO1A2, SLCO1B1 and SLCO2B1 polymorphisms influences chloroquine and primaquine treatment in Plasmodium vivax malaria. Pharmacogenomics 11 28975866
2013 The impact of SLCO1B1 genetic polymorphisms on neonatal hyperbilirubinemia: a systematic review with meta-analysis. Jornal de pediatria 11 23850112
2009 Organic anion transporter protein (OATP1B1) encoded by SLCO1B1 gene polymorphism (388A>G) & susceptibility in gallstone disease. The Indian journal of medical research 11 19293444

Missed literature

Know a paper Affinage missed for SLCO1B1? Flag it for the maintainers and the community.

No submissions yet.