Affinage

SLC22A1

Solute carrier family 22 member 1 · UniProt O15245

Length
554 aa
Mass
61.2 kDa
Annotated
2026-06-10
72 papers in source corpus 24 papers cited in narrative 23 extracted findings
Cross-family judge vs UniProt: Affinage preferred faithfulness: 6/6 claims corpus-supported (100%)

Mechanistic narrative

Synthesis pass · prose summary of the discoveries below

SLC22A1 encodes OCT1, a polyspecific, electrogenic organic cation transporter localized to the basolateral membrane of hepatocytes, where it mediates facilitated uptake of diverse organic cations into the liver and contributes to intestinal secretion (PMID:11463829, PMID:19591196). By providing the basolateral entry step, OCT1 enables vectorial transcellular cation secretion: in epithelial cells co-expressing OCT1 (basolateral) and apical efflux transporters, substrates such as berberine undergo directional transport across the cell (PMID:18157518). Its substrate range encompasses model cations (TEA, MPP+) and numerous drugs, including ranitidine and famotidine, cisplatin, the survivin suppressant YM155, sorafenib, and fluoroquinolones, with the transporter also exporting endogenous acylcarnitines from hepatocytes to the circulation (PMID:16141367, PMID:16914559, PMID:19833842, PMID:23532667, PMID:23545524, PMID:28942964). Only the full-length isoform is transport-competent, with shorter alternatively spliced variants being non-functional (PMID:11388889). Basal hepatic expression is driven by USF1/USF2 binding a core-promoter E-box and is amplified by HNF4α, glucocorticoid receptor signaling, and PPAR-α/γ agonists, while PXR activation represses OCT1 by squelching the SRC-1 coactivator from HNF4α and USF elements, and promoter DNA methylation silences OCT1 in hepatocellular carcinoma (PMID:18845576, PMID:15458920, PMID:26920453, PMID:24399729, PMID:22196450, PMID:23228442). Loss-of-function arises through two routes: coding variants that abolish transport while remaining membrane-resident (e.g., P283L, R287G) or that prevent membrane targeting (truncating R61S fs*10, C88A fs*16), with systematic variant scanning showing most human variants impair function through protein misfolding rather than disrupted substrate binding; promoter SNPs additionally alter transcription-factor binding and expression, collectively explaining inter-individual pharmacokinetic variability for OCT1 substrate drugs (PMID:14697261, PMID:23532667, PMID:37333090, PMID:30544975, PMID:39668580).

Mechanistic history

Synthesis pass · year-by-year structured walk · 13 steps
  1. 1997 Medium

    Establishing the genomic locus and exon structure of SLC22A1 anchored the gene and revealed that alternative splicing generates multiple transcripts, only one of which is functional.

    Evidence FISH chromosomal mapping to 6q26 and cDNA cloning with isoform transport assays in HEK293 cells

    PMID:11388889 PMID:9605850

    Open questions at the time
    • Physiological relevance of non-functional splice variants unresolved
    • Tissue distribution of isoforms not defined
  2. 2001 High

    In vivo knockout addressed whether OCT1 is physiologically required for hepatic cation handling, establishing it as the basolateral uptake transporter into liver and a contributor to intestinal secretion.

    Evidence Oct1 knockout mouse with TEA tissue distribution and excretion measurements across multiple cation substrates

    PMID:11463829

    Open questions at the time
    • Driving force / electrogenicity not directly measured in this study
    • Human tissue localization not yet confirmed at this point
  3. 2004 High

    Variant-specific mutagenesis resolved whether loss-of-function variants act on transport catalysis or membrane delivery, showing some abolish transport while remaining membrane-resident.

    Evidence Xenopus oocyte uptake of TEA and MPP+ with Western blot for membrane expression across coding variants

    PMID:14697261

    Open questions at the time
    • Structural basis of transport loss not defined
    • Allele frequencies and clinical impact not assessed here
  4. 2004 High

    Promoter dissection identified a transcriptional input regulating OCT1, showing PPAR-α/γ agonists upregulate the gene via a PPAR-response element and increase hepatocyte cation uptake.

    Evidence Mouse in vivo and H35 cell PPAR-agonist treatment with promoter-reporter assays and functional uptake

    PMID:15458920

    Open questions at the time
    • Shown in murine Slc22a1; human promoter element not directly tested
    • Endogenous ligand context unclear
  5. 2009 High

    Quantitative human liver analysis connected a coding variant to expression, establishing that Arg61Cys reduces OCT1 protein in vivo and confirming basolateral localization in human hepatocytes.

    Evidence Immunofluorescence and quantitative protein analysis in 150 human livers with MALDI-TOF genotyping and transport assays

    PMID:19591196

    Open questions at the time
    • Mechanism by which R61C lowers protein (folding vs. stability) not defined here
    • Substrate-specific consequences not enumerated
  6. 2008 High

    Identifying USF1/USF2 binding to a core-promoter E-box defined the basal transcriptional driver of OCT1 and its synergy with HNF4α.

    Evidence Promoter deletion, luciferase reporters, EMSA, and E-box mutagenesis in Huh7 and HepG2 cells

    PMID:18845576

    Open questions at the time
    • Genetic variation in the E-box not yet examined
    • Chromatin-level regulation not addressed
  7. 2013 High

    Mechanistic regulation studies established a bidirectional transcriptional network: GR/HNF4α and C/EBPβ/PGC1α upregulate OCT1 while PXR represses it by coactivator squelching, and promoter methylation silences it in HCC.

    Evidence Primary human hepatocytes and cell lines with reporter assays, ChIP, siRNA, SRC-1 rescue, demethylation rescue, and transport assays

    PMID:22196450 PMID:24399729 PMID:26920453

    Open questions at the time
    • Quantitative integration of competing inputs in vivo not resolved
    • Methylation triggers in HCC undefined
  8. 2013 High

    Substrate and inhibitor profiling expanded OCT1's pharmacological scope, establishing it as the hepatic sinusoidal uptake step for sorafenib, fluoroquinolones, rilpivirine, and additional drugs, and defining truncating variants that prevent membrane targeting.

    Evidence Heterologous expression (oocytes, HEK293, KCL22) with uptake, inhibition kinetics, HPLC-MS/MS, and membrane localization across substrates and variants

    PMID:16141367 PMID:16914559 PMID:19833842 PMID:23532667 PMID:23545524 PMID:24002095

    Open questions at the time
    • Relative in vivo contribution versus other OCTs/MATEs not quantified for all substrates
    • Substrate recognition determinants not structurally mapped
  9. 2017 High

    Metabolomic and genetic analysis identified an endogenous physiological role, showing OCT1 effluxes acylcarnitines from liver to circulation and that human variants impair this activity.

    Evidence Slc22a1 knockout mice, gain-of-function cells, isotope tracing, targeted metabolomics, and human variant validation

    PMID:28942964

    Open questions at the time
    • Direction (efflux) mechanism relative to cation uptake not reconciled
    • Clinical metabolic consequences in humans not established
  10. 2018 Medium

    Promoter SNP characterization linked regulatory variation to function, showing -201C>G abolishes USF-dependent promoter activity while -1795G>A has no native effect.

    Evidence EMSA, luciferase reporters in HepG2/Hep3B/Huh7, and pharmacokinetic study of OCT1 substrates in volunteers

    PMID:30544975

    Open questions at the time
    • In vivo expression impact of -201C>G not directly measured
    • Population frequency and clinical penetrance unclear
  11. 2023 Medium

    Systematic variant scanning resolved the dominant molecular mechanism of loss-of-function, showing most variants act through protein misfolding and identifying the N-terminal folding determinant region.

    Evidence Comprehensive single-variant mutagenesis with uptake assays, molecular dynamics, and population database mining (preprint)

    PMID:37333090

    Open questions at the time
    • Preprint not yet peer-reviewed
    • No experimental structure underpinning the folding model
    • Folding chaperone partners unidentified
  12. 2024 Medium

    Physiological-model and clinical studies refined OCT1 kinetics and regulation, showing stable activity under nuclear-receptor activation in human hepatocyte spheroids and confirming a coding variant reduces hepatic uptake of proguanil clinically.

    Evidence 3D primary human hepatocyte spheroid ASP+ kinetics with inhibitor and nuclear-receptor exposure, plus a clinical PK study with population modeling

    PMID:39068198 PMID:39668580

    Open questions at the time
    • Discrepancy with PXR repression seen in 2D hepatocytes not reconciled
    • Small clinical cohort for proguanil variant
  13. 2025 Low

    An overexpression study proposed a non-transport role, linking SLC22A1 to suppression of hepatitis B antigens via JAK/STAT signaling.

    Evidence SLC22A1 overexpression in HepG2.2.15 cells with antigen ELISA, RNA-seq, and IHC

    PMID:40036258

    Open questions at the time
    • Mechanism connecting a transporter to JAK/STAT not reconstituted
    • Single overexpression system without loss-of-function confirmation
    • Whether effect depends on transport activity unknown

Open questions

Synthesis pass · forward-looking unresolved questions
  • How OCT1's transport mechanism (substrate recognition, electrogenicity, and direction-switching between cation uptake and acylcarnitine efflux) is structurally encoded remains unresolved.
  • No experimentally determined structure in the corpus
  • Conformational cycle and ion-coupling not defined
  • Structural basis for polyspecificity unknown

Mechanism profile

Synthesis pass · controlled-vocabulary classification · explore literature graph →
Molecular activity
GO:0005215 transporter activity 11 GO:0140104 molecular carrier activity 1
Localization
GO:0005886 plasma membrane 4
Pathway
R-HSA-74160 Gene expression (Transcription) 6 R-HSA-9748784 Drug ADME 5 R-HSA-382551 Transport of small molecules 3
Partners
HNF4AUSF1USF2

Evidence

Reading pass · 23 per-paper findings extracted from the source corpus
Year Finding Method Journal Conf PMIDs
2001 OCT1 (SLC22A1) is localized at the basolateral membrane of hepatocytes and mediates uptake of organic cations (TEA, metaiodobenzylguanidine, MPP+) into liver; Oct1 knockout mice show 4–6-fold reduced hepatic accumulation of TEA and ~2-fold reduced direct intestinal excretion, establishing OCT1's role in hepatic cation uptake and intestinal secretion. Oct1 knockout mouse model; intravenous TEA administration with tissue distribution and excretion measurements Molecular and cellular biology High 11463829
1997 The SLC22A1 gene (encoding OCT1) was mapped to chromosome 6q26 by fluorescence in situ hybridization. Chromosomal localization by cytogenetics/FISH Cytogenetics and cell genetics Medium 9605850
1999 The SLC22A1 gene consists of 7 exons and 6 introns and produces at least four alternatively spliced isoforms; only the full-length hOCT1 isoform mediates decynium-22-sensitive uptake of [3H]-MPP+ when stably expressed in HEK293 cells, demonstrating that shorter splice variants are non-functional. cDNA cloning, gene structure determination, stable transfection of HEK293 cells, [3H]-MPP+ uptake assay Annals of human genetics Medium 11388889
2004 SNPs P283L and R287G in SLC22A1 abolish transport of both TEA and MPP+ despite detectable plasma membrane protein expression in Xenopus oocytes, while P341L reduces TEA uptake to ~65% of wild type and F160L has no significant effect, demonstrating that specific coding variants impair OCT1 transport activity without affecting membrane targeting. Xenopus oocyte expression system with [14C]TEA and [3H]MPP+ uptake assays; Western blot for membrane expression Biochemical and biophysical research communications High 14697261
2005 Ranitidine is a substrate of hOCT1 (Km ~70 µM) and hOCT2 but not hOCT3, as determined by [3H]ranitidine uptake in cRNA-injected Xenopus oocytes; famotidine is an hOCT1 substrate (confirmed by trans-stimulation and electrophysiology) and potently inhibits hOCT3 (IC50 ~6.7 µM), while ranitidine is a weak hOCT3 inhibitor (IC50 ~290 µM). cRNA-injected Xenopus laevis oocytes; [3H]ranitidine uptake, trans-stimulation, and electrophysiology The Journal of pharmacology and experimental therapeutics High 16141367
2006 Cisplatin is a substrate of hOCT1 (and more potently hOCT2 and hMATE1), as shown by enhanced cytotoxicity and cellular accumulation in HEK293 cells transiently expressing hOCT1 and concentration-dependent inhibition of TEA uptake; carboplatin and nedaplatin are not transported by hOCT1 or related transporters. Transient transfection of HEK293 cells; cytotoxicity assay, [14C]cisplatin accumulation, TEA competition assay The Journal of pharmacology and experimental therapeutics High 16914559
2007 OCT1 (SLC22A1) localizes to the basolateral membrane of human hepatocytes and transports berberine (Km ~14.8 µM); in double-transfected MDCKII cells expressing OCT1 (basolateral) and MDR1 P-gp (apical), berberine undergoes vectorial transcellular transport, establishing OCT1 as the basolateral uptake step for vectorial cation secretion in liver. Immunofluorescence localization in human hepatocytes; stable transfection of MDCKII cells; fluorescence-based berberine uptake and transcellular transport assays; Michaelis-Menten kinetics Naunyn-Schmiedeberg's archives of pharmacology High 18157518
2008 USF1 and USF2 transcription factors bind a cognate E-box (CACGTG) element in the OCT1 core promoter region (−141/−69) and are required for basal OCT1 gene expression; HNF4α further stimulates USF-mediated transactivation of the OCT1 promoter in hepatocytes. Promoter deletion analysis, luciferase reporter gene assay, electrophoretic mobility shift assay (EMSA), site-directed mutagenesis of E-box, co-transfection of transcription factor expression vectors in Huh7 and HepG2 cells American journal of physiology. Gastrointestinal and liver physiology High 18845576
2009 OCT1 protein is localized to the basolateral membrane of human hepatocytes; the OCT1-Arg61Cys variant (rs12208357) strongly correlates with decreased OCT1 protein expression in human liver; both OCT1 and OCT3 transport metformin in transfected cells. Immunofluorescence microscopy of human liver tissue; quantitative protein expression analysis in 150 liver samples; functional transport assay in transfected cells; MALDI-TOF genotyping; multivariate analysis Hepatology (Baltimore, Md.) High 19591196
2010 YM155 is a substrate of OCT1/SLC22A1 (Km ~22.1 µM) and OCT2 but not OCT3, as shown by time- and concentration-dependent uptake in HEK293 cells expressing hOCT1 and inhibition of [3H]MPP+ uptake. Transient transfection of HEK293 cells; [14C]YM155 uptake kinetics; [3H]MPP+ inhibition assay Drug metabolism and disposition: the biological fate of chemicals Medium 19833842
2004 PPAR-α and PPAR-γ agonists transcriptionally upregulate murine Slc22a1 (Oct1) gene expression via a PPAR-response element in the Slc22a1 promoter, resulting in increased organic cation uptake in hepatocytes. Mouse in vivo treatment and H35 cell treatment with PPAR agonists; Slc22a1 promoter cloning; chimeric promoter-reporter luciferase assay; PPAR transcription factor transfection; organic cation uptake functional assay American journal of physiology. Gastrointestinal and liver physiology High 15458920
2013 SLC22A1 (OCT1) transports sorafenib; two novel truncating variants (R61S fs*10 and C88A fs*16) produce proteins that fail to reach the plasma membrane and abolish OCT1-mediated sorafenib uptake, as validated by quinine-sensitive sorafenib uptake in Xenopus oocytes measured by HPLC-MS/MS. Directed mutagenesis; expression in HCC cell lines and Xenopus laevis oocytes; plasma membrane localization; [3H]TEA uptake; quinine-sensitive sorafenib uptake by HPLC-MS/MS Hepatology (Baltimore, Md.) High 23532667
2013 PXR activation (by rifampicin or hyperforin) downregulates OCT1 mRNA and reduces hepatic [3H]MPP+ accumulation; this occurs by PXR competing for (squelching) the SRC-1 coactivator from HNF4α response elements and USF1 E-box elements in the OCT1 promoter, requiring both PXR and HNF4α. Primary human hepatocytes and HepaRG cells; qRT-PCR; [3H]MPP+ transport assay; OCT1 promoter reporter constructs; siRNA knockdown of PXR and HNF4α; chromatin immunoprecipitation (ChIP); mutagenesis of promoter elements; SRC-1 overexpression rescue British journal of pharmacology High 26920453
2013 Glucocorticoid receptor (GR) activation by dexamethasone indirectly upregulates OCT1 mRNA and protein expression in primary human hepatocytes via HNF4α induction; C/EBPβ and PGC1α also contribute to OCT1 gene regulation, with C/EBPβ co-transfection stimulating OCT1 promoter activity. Primary human hepatocytes and hepatocyte-derived cell lines (HepG2, MZ-Hep1); qRT-PCR; Western blot; luciferase gene reporter assays with OCT1 promoter constructs; viral transduction of transcription factors Pharmacological reports : PR Medium 24399729
2011 DNA methylation of the SLC22A1 promoter region is mechanistically associated with transcriptional downregulation of OCT1 in hepatocellular carcinoma; treatment with the demethylating agent 5-aza-2-deoxycytidine restores Slc22a1 expression in tumor-derived cells. MALDI-TOF mass spectrometry quantification of DNA methylation in paired HCC and non-tumor liver tissues; tissue microarray IHC; 5-aza-2-deoxycytidine and trichostatin A treatment of cultured Tsc1 renal tumor cells (corroborated in PMID:23228442) Genome medicine / European journal of cancer Medium 22196450 23228442
2013 Multiple fluoroquinolones (gatifloxacin, moxifloxacin, prulifloxacin, sparfloxacin) competitively inhibit hOCT1-mediated transport with Ki values of 94–250 µM; hOCT1 selectively mediates their disposition compared with hOCT2 and hOCT3, implicating hOCT1 in sinusoidal hepatic uptake of fluoroquinolones. Heterologous expression in oocyte/cell systems; competitive inhibition kinetics with Ki determination using [3H]TEA or MPP+ as model substrates Antimicrobial agents and chemotherapy Medium 23545524
2013 Rilpivirine is transported by SLC22A1 (OCT1), showing 27% higher accumulation in SLC22A1-overexpressing KCL22 cells versus controls; rilpivirine inhibits SLC22A1 function with an IC50 of 28.5 µM and SLC22A2 with IC50 of 5.13 µM. Stable SLC22A1-expressing KCL22 cells; cellular accumulation assay; TEA uptake inhibition assay Antimicrobial agents and chemotherapy Medium 24002095
2017 SLC22A1 (OCT1) mediates efflux of acylcarnitines from the liver to the circulation; loss-of-function in Slc22a1 knockout mice and gain-of-function cell models with isotope tracing demonstrate that OCT1 transports acylcarnitines out of hepatocytes, and human SLC22A1 coding variants impair this acylcarnitine efflux activity in vitro. Slc22a1 knockout mice; gain-of-function cell models; targeted metabolomics; isotope tracing experiments; in vitro functional validation of human variants American journal of human genetics High 28942964
2018 The -201C>G SNP (rs58812592) in the OCT1 promoter causes allele-dependent differences in USF1/2 transcription factor binding and nearly complete loss of OCT1 promoter activity for the G-allele; the -1795G>A SNP (rs6935207) shows allele-specific NF-Y binding and increased enhancer activity but no significant effect on the native OCT1 promoter or on pharmacokinetics of OCT1 substrates. Electrophoretic mobility shift assay (EMSA); luciferase reporter gene assay in HepG2, Hep3B, Huh7 cells; pharmacokinetic analysis of metformin, fenoterol, sumatriptan, proguanil in healthy volunteers Journal of personalized medicine Medium 30544975
2023 Systematic missense and deletion variant scanning of OCT1 (SLC22A1) reveals that most human variants impair function via protein misfolding rather than direct disruption of substrate binding; the first 300 amino acids (including TM1–6 and extracellular domain with a conserved stabilizing helical motif) are major determinants of folding; molecular dynamics simulations identify biophysical mechanisms for specific variant transport phenotypes. Comprehensive single-variant mutagenesis; expression and substrate uptake assays; computational modeling and molecular dynamics simulations; population database mining bioRxivpreprint Medium 37333090
2024 OCT1 (SLC22A1) in 3D primary human hepatocyte spheroids has a Km of ~14 µM for the fluorescent substrate ASP+; OCT1 activity is inhibited 35–52% by known inhibitors and remains stable upon activation of nuclear receptor signaling (including PXR), distinguishing OCT1 regulation from P-glycoprotein and CYP3A4 induction. 3D spheroids of primary human hepatocytes; ASP+ fluorescent transport kinetics assay; known inhibitor co-incubation; global proteomics; 7-day nuclear receptor ligand exposure Scientific reports Medium 39068198
2025 Overexpression of SLC22A1 in HepG2.2.15 cells suppresses hepatitis B surface antigen (HBsAg) and hepatitis B e antigen (HBeAg) expression through activation of the JAK/STAT signaling pathway, as confirmed by transcriptome sequencing and targeted overexpression experiments. SLC22A1 overexpression in HepG2.2.15 cells; ELISA for HBsAg and HBeAg; RNA sequencing; immunohistochemistry The Journal of infectious diseases Low 40036258
2024 The SLC22A1 1022C>T variant (rs2282143) reduces OCT1-mediated hepatic uptake of proguanil; CT heterozygotes showed 1.2-fold higher proguanil systemic exposure and 0.5-fold lower cycloguanil exposure compared to wild-type CC, with population PK modeling estimating 0.42-fold reduced OCT1 activity in CT carriers. Clinical pharmacokinetic study in Korean subjects; population PK modeling with well-stirred liver compartment; prospective SLC22A1 genotyping Clinical and translational science Medium 39668580

Source papers

Stage 0 corpus · 72 papers · ranked by NIH iCite citations
Year Title Journal Citations PMID
2009 Expression of organic cation transporters OCT1 (SLC22A1) and OCT3 (SLC22A3) is affected by genetic factors and cholestasis in human liver. Hepatology (Baltimore, Md.) 308 19591196
2006 Cisplatin and oxaliplatin, but not carboplatin and nedaplatin, are substrates for human organic cation transporters (SLC22A1-3 and multidrug and toxin extrusion family). The Journal of pharmacology and experimental therapeutics 269 16914559
2001 Reduced hepatic uptake and intestinal excretion of organic cations in mice with a targeted disruption of the organic cation transporter 1 (Oct1 [Slc22a1]) gene. Molecular and cellular biology 171 11463829
2013 Expression of SLC22A1 variants may affect the response of hepatocellular carcinoma and cholangiocarcinoma to sorafenib. Hepatology (Baltimore, Md.) 130 23532667
2011 DNA methylation is associated with downregulation of the organic cation transporter OCT1 (SLC22A1) in human hepatocellular carcinoma. Genome medicine 119 22196450
2007 Vectorial transport of the plant alkaloid berberine by double-transfected cells expressing the human organic cation transporter 1 (OCT1, SLC22A1) and the efflux pump MDR1 P-glycoprotein (ABCB1). Naunyn-Schmiedeberg's archives of pharmacology 88 18157518
2005 Differential substrate and inhibitory activities of ranitidine and famotidine toward human organic cation transporter 1 (hOCT1; SLC22A1), hOCT2 (SLC22A2), and hOCT3 (SLC22A3). The Journal of pharmacology and experimental therapeutics 83 16141367
2004 Novel single nucleotide polymorphisms of organic cation transporter 1 (SLC22A1) affecting transport functions. Biochemical and biophysical research communications 83 14697261
2011 Development of imatinib and dasatinib resistance: dynamics of expression of drug transporters ABCB1, ABCC1, ABCG2, MVP, and SLC22A1. Leukemia & lymphoma 59 21663515
2019 Variation in the Plasma Membrane Monoamine Transporter (PMAT) (Encoded by SLC29A4) and Organic Cation Transporter 1 (OCT1) (Encoded by SLC22A1) and Gastrointestinal Intolerance to Metformin in Type 2 Diabetes: An IMI DIRECT Study. Diabetes care 56 30885951
2017 Fine Mapping and Functional Analysis Reveal a Role of SLC22A1 in Acylcarnitine Transport. American journal of human genetics 50 28942964
2010 Characterization of human organic cation transporter 1 (OCT1/SLC22A1)- and OCT2 (SLC22A2)-mediated transport of 1-(2-methoxyethyl)-2-methyl-4,9-dioxo-3-(pyrazin-2-ylmethyl)- 4,9-dihydro-1H-naphtho[2,3-d]imidazolium bromide (YM155 monobromide), a novel small molecule survivin suppressant. Drug metabolism and disposition: the biological fate of chemicals 50 19833842
1997 The two human organic cation transporter genes SLC22A1 and SLC22A2 are located on chromosome 6q26. Cytogenetics and cell genetics 50 9605850
1999 Molecular cloning, functional characterization and genomic organization of four alternatively spliced isoforms of the human organic cation transporter 1 (hOCT1/SLC22A1). Annals of human genetics 44 11388889
2013 Downregulation of organic cation transporter 1 (SLC22A1) is associated with tumor progression and reduced patient survival in human cholangiocellular carcinoma. International journal of oncology 43 23440379
2014 Influence of SLC22A1 rs622342 genetic polymorphism on metformin response in South Indian type 2 diabetes mellitus patients. Clinical and experimental medicine 41 25492374
2016 The pregnane X receptor down-regulates organic cation transporter 1 (SLC22A1) in human hepatocytes by competing for ("squelching") SRC-1 coactivator. British journal of pharmacology 33 26920453
2019 Metformin Pharmacogenetics: Effects of SLC22A1, SLC22A2, and SLC22A3 Polymorphisms on Glycemic Control and HbA1c Levels. Journal of personalized medicine 32 30934600
2013 A common novel splice variant of SLC22A1 (OCT1) is associated with impaired responses to imatinib in patients with chronic myeloid leukaemia. British journal of haematology 31 24117365
2016 Impact of ATM and SLC22A1 Polymorphisms on Therapeutic Response to Metformin in Iranian Diabetic Patients. International journal of molecular and cellular medicine 30 27386433
2014 Reduced ABCG2 and increased SLC22A1 mRNA expression are associated with imatinib response in chronic myeloid leukemia. Medical oncology (Northwood, London, England) 30 24469953
2013 Human organic cation transporters 1 (SLC22A1), 2 (SLC22A2), and 3 (SLC22A3) as disposition pathways for fluoroquinolone antimicrobials. Antimicrobial agents and chemotherapy 29 23545524
2013 Glucocorticoid receptor regulates organic cation transporter 1 (OCT1, SLC22A1) expression via HNF4α upregulation in primary human hepatocytes. Pharmacological reports : PR 27 24399729
2004 Seven novel single nucleotide polymorphisms in the human SLC22A1 gene encoding organic cation transporter 1 (OCT1). Drug metabolism and pharmacokinetics 27 15499200
2018 Impact of SLC22A1 and CYP3A5 genotypes on imatinib response in chronic myeloid leukemia: A systematic review and meta-analysis. Pharmacological research 26 29427770
2015 Role of SLC22A1 polymorphic variants in drug disposition, therapeutic responses, and drug-drug interactions. The pharmacogenomics journal 26 26526073
2019 Altered Glycemic Control Associated With Polymorphisms in the SLC22A1 (OCT1) Gene in a Mexican Population With Type 2 Diabetes Mellitus Treated With Metformin: A Cohort Study. Journal of clinical pharmacology 25 31012983
2004 Transcriptional regulation of murine Slc22a1 (Oct1) by peroxisome proliferator agonist receptor-alpha and -gamma. American journal of physiology. Gastrointestinal and liver physiology 25 15458920
2013 Rilpivirine inhibits drug transporters ABCB1, SLC22A1, and SLC22A2 in vitro. Antimicrobial agents and chemotherapy 23 24002095
2016 SLC22A1/OCT1 Genotype Affects O-desmethyltramadol Exposure in Newborn Infants. Therapeutic drug monitoring 22 27082504
2012 Renal tumours in a Tsc1+/- mouse model show epigenetic suppression of organic cation transporters Slc22a1, Slc22a2 and Slc22a3, and do not respond to metformin. European journal of cancer (Oxford, England : 1990) 20 23228442
2020 Effect of Sex, Use of Pantoprazole and Polymorphisms in SLC22A1, ABCB1, CES1, CYP3A5 and CYP2D6 on the Pharmacokinetics and Safety of Dabigatran. Advances in therapy 19 32564268
2022 Role of human organic cation transporter-1 (OCT-1/SLC22A1) in modulating the response to metformin in patients with type 2 diabetes. BMC endocrine disorders 18 35619086
2008 Regulation of basal core promoter activity of human organic cation transporter 1 (OCT1/SLC22A1). American journal of physiology. Gastrointestinal and liver physiology 18 18845576
2020 Cellular uptake properties of lamotrigine in human placental cell lines: Investigation of involvement of organic cation transporters (SLC22A1-5). Drug metabolism and pharmacokinetics 16 32303459
2015 Interactions of antiretroviral drugs with the SLC22A1 (OCT1) drug transporter. Frontiers in pharmacology 14 25914645
2022 Association of SLC22A1, SLC22A2, SLC47A1, and SLC47A2 Polymorphisms with Metformin Efficacy in Type 2 Diabetic Patients. Biomedicines 13 36289808
2019 The influence of SLC22A1 rs622342 and ABCC8 rs757110 genetic variants on the efficacy of metformin and glimepiride combination therapy in Egyptian patients with type 2 diabetes. Journal of drug assessment 13 31231590
2018 Genetic variations in influx transporter gene SLC22A1 are associated with clinical responses to imatinib mesylate among Malaysian chronic myeloid leukaemia patients. Journal of genetics 13 30262695
2014 Genetic polymorphisms and haplotypes of the organic cation transporter 1 gene (SLC22A1) in the Xhosa population of South Africa. Genetics and molecular biology 13 25071399
2018 Polymorphisms of SLCO1B1 rs4149056 and SLC22A1 rs2282143 are associated with responsiveness to acitretin in psoriasis patients. Scientific reports 12 30181619
2020 Relationship between changes in the exon-recognition machinery and SLC22A1 alternative splicing in hepatocellular carcinoma. Biochimica et biophysica acta. Molecular basis of disease 11 31953214
2019 SLC22A1 And ATM Genes Polymorphisms Are Associated With The Risk Of Type 2 Diabetes Mellitus In Western Saudi Arabia: A Case-Control Study. The application of clinical genetics 11 31814751
2023 Genetic Variation in CYP2D6 and SLC22A1 Affects Amlodipine Pharmacokinetics and Safety. Pharmaceutics 9 36839726
2022 Effect of Metformin on Glycemic Control Regarding Carriers of the SLC22A1/OCT1 (rs628031) Polymorphism and Its Interactions with Dietary Micronutrients in Type 2 Diabetes. Diabetes, metabolic syndrome and obesity : targets and therapy 8 35711690
2014 Genetic polymorphisms of the organic cation transporter 1 gene (SLC22A1) within the Cape Admixed population of South Africa. Molecular biology reports 8 25398212
2023 The full spectrum of OCT1 (SLC22A1) mutations bridges transporter biophysics to drug pharmacogenomics. bioRxiv : the preprint server for biology 7 37333090
2011 Screening of genetic variations of SLC15A2, SLC22A1, SLC22A2 and SLC22A6 genes. Journal of human genetics 7 21796140
2024 OCT1 (SLC22A1) transporter kinetics and regulation in primary human hepatocyte 3D spheroids. Scientific reports 6 39068198
2020 SLC22A1 rs622342 Polymorphism Predicts Insulin Resistance Improvement in Patients with Type 2 Diabetes Mellitus Treated with Metformin: A Cross-Sectional Study. International journal of endocrinology 6 32454819
2023 Pharmacogenetic impact of SLC22A1 gene variant rs628031 (G/A) in newly diagnosed Indian type 2 diabetes patients undergoing metformin monotherapy. Pharmacogenetics and genomics 5 36853844
2023 Association of SLC22A1, SLC47A1, and KCNJ11 polymorphisms with efficacy and safety of metformin and sulfonylurea combination therapy in Egyptian patients with type 2 diabetes. Research in pharmaceutical sciences 5 39005567
2022 MPP+-Induced Changes in Cellular Impedance as a Measure for Organic Cation Transporter (SLC22A1-3) Activity and Inhibition. International journal of molecular sciences 5 35163125
2022 The influence of metformin transporter gene SLC22A1 and SLC47A1 variants on steady-state pharmacokinetics and glycemic response. PloS one 5 35905099
2018 Imatinib Affects the Expression of SLC22A1 in a Non-Linear Concentration-Dependent Manner Within 24 Hours. Medical science monitor basic research 5 29567937
2018 Impact of Promoter Polymorphisms on the Transcriptional Regulation of the Organic Cation Transporter OCT1 (SLC22A1). Journal of personalized medicine 5 30544975
2025 Genetic Variants of SLC22A1 rs628031 and rs622342 and Glycemic Control in T2DM Patients from Northern Mexico. Genes 4 40004467
2025 Molecular Ancestry Across Allelic Variants of SLC22A1, SLC22A2, SLC22A3, ABCB1, CYP2C8, CYP2C9, and CYP2C19 in Mexican-Mestizo DMT2 Patients. Biomedicines 4 40426982
2023 Association of Met420del Variant of Metformin Transporter Gene SLC22A1 with Metformin Treatment Response in Ethiopian Patients with Type 2 Diabetes. Diabetes, metabolic syndrome and obesity : targets and therapy 4 37641646
2021 Association of SLC22A1,SLCO1B3 Drug Transporter Polymorphisms and Smoking with Disease Risk and Cytogenetic Response to Imatinib in Patients with Chronic Myeloid Leukemia. Laboratory medicine 4 34128532
2024 Effect of Genetic Polymorphisms of ABCB1, ABCG2, and SLC22A1 on the Steady-State Plasma Concentrations of Lamotrigine in Treatment-Resistant Depressed Patients Treated With Lamotrigine Augmentation Therapy. Clinical neuropharmacology 3 39171842
2022 The Role of SLC22A1 and Genomic Ancestry on Toxicity during Treatment in Children with Acute Lymphoblastic Leukemia of the Amazon Region. Genes 3 35456416
2021 Genetic variants in SLC22A1 are related to serum lipid levels in Mexican women. Lipids 3 34927264
2019 Allele Frequency of SLC22A1 Met420del Metformin Main Transporter Encoding Gene among Javanese-Indonesian Population. Open access Macedonian journal of medical sciences 3 30834005
2024 Influence of Solute Carrier Family 22 Member 1 (SLC22A1) Gene Polymorphism on Metformin Pharmacokinetics and HbA1c Levels: A Systematic Review. Current diabetes reviews 2 37550919
2024 Effect of SLC22A1 polymorphism on the pharmacokinetics of proguanil in Korean: A semi-physiologic population pharmacokinetic approach. Clinical and translational science 2 39668580
2018 Relationship Between SLC22A1 and SLC22A4 Gene Polymorphisms and Risk of Type 2 Diabetes in Chinese Han Population. Clinical laboratory 2 30274012
2025 SLC22A1 Resists Hepatitis B Virus by Activating the JAK/STAT Pathway and Predicts the Effect of Pegylated Interferon α-Based Therapy on Chronic Hepatitis B. The Journal of infectious diseases 1 40036258
2024 Association of the Reduced Function Met420del Polymorphism of SLC22A1 with Metformin-Induced Gastrointestinal Intolerance in Ethiopian Patients with Type 2 Diabetes Mellitus. Pharmacogenomics and personalized medicine 1 38715682
2024 Impact of SLC22A1 rs12208357 on therapeutic response to metformin in type 2 diabetes patients. Journal of diabetes and metabolic disorders 1 39610478
2025 Frequency of Polymorphisms in SLC47A1 (rs2252281 and rs2289669) and SLC47A2 (rs34834489 and rs12943590) and the Influence of SLC22A1 (rs72552763 and rs622342) on HbA1c Levels in Mexican-Mestizo Patients with DMT2 Treated with Metformin Monotherapy. International journal of molecular sciences 0 40943569
2025 Pharmacogenetics and Molecular Ancestry of SLC22A1, SLC22A2, SLC22A3, ABCB1, CYP2C8, CYP2C9, and CYP2C19 in Ecuadorian Subjects with Type 2 Diabetes Mellitus. Pharmaceuticals (Basel, Switzerland) 0 41011206

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