Affinage

SLC29A1

Equilibrative nucleoside transporter 1 · UniProt Q99808

Length
456 aa
Mass
50.2 kDa
Annotated
2026-04-28
100 papers in source corpus 44 papers cited in narrative 44 extracted findings

Mechanistic narrative

Synthesis pass · prose summary of the discoveries below

SLC29A1 (ENT1) is a facilitative, equilibrative nucleoside transporter that bidirectionally shuttles purine and pyrimidine nucleosides, nicotinamide, and nucleoside analog drugs across the plasma membrane, thereby serving as the primary determinant of extracellular adenosine concentration in multiple tissues and governing adenosine receptor-mediated signaling. Structurally, ENT1 requires N-glycosylation at Asn48 for proper oligomerization and function, is phosphorylated by PKC (Ser279, Ser286, Thr274) and PKA in the TM6–TM7 intracellular loop, and its transport cycle involves conformational transitions driven by TM1, TM2, TM7, and TM9 with high-affinity NBMPR sensitivity (Kd ~0.4 nM) and a distinct inhibitor-binding site for dilazep (PMID:31235912, PMID:10722669, PMID:27480168, PMID:21809900). ENT1-mediated adenosine uptake controls the AMPK–BPGM–2,3-BPG axis in erythrocytes to regulate oxygen delivery (PMID:37725437, PMID:32434995), modulates A2A/A2B adenosine receptor signaling to confer cardioprotection and renoprotection after ischemia–reperfusion injury (PMID:37288658, PMID:22269324), suppresses T cell pyrimidine synthesis through PRPS inhibition to limit antitumor immunity (PMID:40355731, PMID:39652568), and regulates striatal dopamine release and ethanol-related behaviors via adenosine–A2AR–CREB signaling (PMID:23467349, PMID:35042768). Loss-of-function mutations in SLC29A1 define the Augustine-null blood group and cause ectopic mineralization and macrocytosis with defective erythropoiesis in humans (PMID:25896650, PMID:33690842).

Mechanistic history

Synthesis pass · year-by-year structured walk · 16 steps
  1. 2000 High

    Functional reconstitution of hENT1 in transport-null cells established its identity as a broadly selective, high-affinity NBMPR-sensitive equilibrative nucleoside transporter with defined kinetic parameters, resolving the molecular basis of the classical 'es' transport activity.

    Evidence Stable expression in PK15NTD cells with radioligand binding, uridine uptake kinetics, and deglycosylation analysis

    PMID:10722669

    Open questions at the time
    • Oligomeric state unknown at this point
    • No structural information on inhibitor or substrate binding sites
    • Phosphorylation and post-translational regulation not characterized
  2. 2003 High

    ENT1 was shown to control extracellular adenosine tone in neural tissue, establishing its physiological role beyond drug uptake: ENT1 inhibition elevated synaptic adenosine and suppressed glutamatergic transmission via presynaptic A1 receptors.

    Evidence Whole-cell patch clamp in rat spinal cord slices with NBMPR, A1R antagonists, and paired-pulse analysis

    PMID:12611914

    Open questions at the time
    • Cell-type specificity of ENT1 in CNS circuits not resolved
    • Whether ENT2 compensates in vivo unknown
  3. 2006 High

    Transcriptional repression of SLC29A1 by nitric oxide was mapped to a promoter region between −2154 and −1114 bp, with subsequent work identifying the hCHOP–C/EBPα complex and Sp1 as mediators under diabetic (high glucose) conditions, revealing how metabolic disease downregulates adenosine clearance.

    Evidence Promoter-reporter deletion constructs, ChIP, eNOS siRNA, Sp1 overexpression, and pharmacological pathway dissection in primary HUVECs

    PMID:16688763 PMID:18064606 PMID:20032083

    Open questions at the time
    • Whether these transcriptional mechanisms operate in non-endothelial tissues not tested
    • Relative contribution of each transcription factor in vivo unknown
  4. 2010 High

    JNK–c-Jun signaling was identified as a negative transcriptional regulator of ENT1 via an AP-1 site at −1196 bp, later shown to be engaged by ZIP4–ZEB1–integrin α3β1 signaling in pancreatic cancer, establishing a pathway linking the tumor microenvironment to gemcitabine resistance.

    Evidence c-Jun overexpression/dominant-negative mutants, promoter luciferase assays, ChIP, and shRNA knockdown with in vivo xenograft validation

    PMID:21145879 PMID:31711924

    Open questions at the time
    • Whether JNK-mediated repression is reversible therapeutically not shown
    • Direct binding of ZEB1 to ENT1 promoter not demonstrated
  5. 2011 High

    Direct phosphorylation sites on ENT1 were mapped: PKC targets Ser279/Ser286/Thr274 and PKA targets multiple sites in the TM6–TM7 intracellular loop, providing the molecular basis for kinase-dependent modulation of transport activity including ethanol sensitivity.

    Evidence In vitro kinase assays on purified intracellular loop peptides with phosphoamino acid analysis

    PMID:21809900

    Open questions at the time
    • Functional consequence of each individual phosphosite on transport kinetics not resolved
    • In vivo phosphorylation stoichiometry unknown
  6. 2012 High

    Genetic deletion of ENT1 in mice demonstrated its non-redundant role in controlling systemic and local adenosine levels, conferring protection against both renal and cardiac ischemia–reperfusion injury through adenosine receptor (particularly A2B) signaling on vascular and myeloid cells.

    Evidence Global Ent1−/− and Ent2−/− mice with kidney and cardiac I/R models, epistasis with A1/A2A/A2B/A3 receptor knockouts, adenosine measurements

    PMID:21872611 PMID:22269324

    Open questions at the time
    • Cell-type-specific contributions of ENT1 not yet dissected at this stage
    • Whether chronic ENT1 loss causes compensatory changes that confound acute protection unclear
  7. 2013 High

    ENT1 was placed at the apex of a striatal adenosine–A2AR–CREB signaling axis controlling goal-directed ethanol drinking, with ENT1 loss reducing A2AR-driven PKA/CREB activity specifically in the dorsomedial striatum.

    Evidence ENT1−/− mice, CRE-lacZ reporter, dominant-negative CREB viral injection in DMS, A2AR antagonist pharmacology, operant ethanol self-administration

    PMID:23467349

    Open questions at the time
    • Whether ENT1-adenosine-A2AR axis generalizes to other reward-related behaviors not established
    • Astrocytic vs neuronal ENT1 contribution not separated in this study
  8. 2015 Medium

    Human genetic studies identified SLC29A1 as the Augustine blood group gene: a missense variant (p.Glu391Lys) defines the At(a−) phenotype, and a null splice-site mutation causes ENT1 absence with ectopic mineralization, directly linking ENT1 loss to a human skeletal phenotype.

    Evidence Genetic sequencing of Augustine-negative and Augustine-null individuals, phenotypic assessment of ectopic mineralization

    PMID:25896650

    Open questions at the time
    • Mechanism connecting ENT1 loss to ectopic mineralization not elucidated
    • Small number of Augustine-null individuals studied
  9. 2016 High

    N-glycosylation at Asn48 was shown to be essential not only for ENT1 surface expression and transport function but also for homo-oligomerization, revealing an unexpected structural requirement for ENT1 assembly.

    Evidence N48Q mutagenesis with NBMPR binding, chloroadenosine transport, immunofluorescence, and co-immunoprecipitation

    PMID:27480168

    Open questions at the time
    • Stoichiometry of the oligomer not determined
    • Whether oligomerization is functionally required beyond surface targeting unclear
  10. 2019 High

    Crystal structures of hENT1 with two inhibitors revealed two distinct inhibitory mechanisms — competitive substrate-site occupancy by dilazep versus a separate binding mode for NBMPR — and identified residues critical for adenosine recognition, providing the first atomic-resolution view of ENT1 function.

    Evidence X-ray crystallography with mutagenesis validation and functional transport assays

    PMID:31235912

    Open questions at the time
    • No substrate-bound structure obtained
    • Conformational cycle (outward-open to inward-open) not captured crystallographically
  11. 2020 High

    Erythrocyte-specific ENT1 was shown to control oxygen delivery via adenosine-driven AMPK–BPGM–2,3-BPG signaling, with maternal eENT1 loss causing placental hypoxia and fetal growth restriction, and subsequent work demonstrating CKD progression through the same axis.

    Evidence Erythrocyte-specific eEnt1−/− mice, isotopic adenosine flux, metabolomics, AMPK/BPGM pathway analysis, Ampd3−/− genetic rescue, CKD models

    PMID:32434995 PMID:37725437

    Open questions at the time
    • Whether pharmacological ENT1 modulation can rescue 2,3-BPG levels therapeutically not tested
    • Human erythrocyte eENT1 conditional studies not possible
  12. 2021 High

    ENT1-null humans (Augustine-null) were found to exhibit macrocytosis and defective erythropoiesis linked to disrupted cAMP homeostasis; pharmacological ABCC4 inhibition rescued erythroid differentiation in Ent1−/− mice, establishing an ENT1–cAMP–ABCC4 regulatory axis in erythropoiesis.

    Evidence Augustine-null human subjects, shRNA ENT1 knockdown in CD34+ progenitors, Ent1−/− mice, nucleotide metabolomics, ABCC4 inhibitor rescue

    PMID:33690842

    Open questions at the time
    • Exact mechanism by which ENT1 controls intracellular cAMP levels not fully elucidated
    • Long-term hematologic consequences in ENT1-null humans not characterized
  13. 2022 High

    Astrocytic ENT1 was demonstrated to set the adenosine tone that tonically inhibits dopamine release in nucleus accumbens via A1 receptors, with ethanol acutely reducing ENT1-mediated clearance to suppress dopamine output.

    Evidence Fast-scan cyclic voltammetry, viral ENT1 overexpression in astrocytes, GRAB-adenosine fiber photometry, pharmacological ENT1/A1R manipulation in ex vivo slices

    PMID:35042768

    Open questions at the time
    • In vivo behavioral consequences of astrocyte-specific ENT1 manipulation not yet shown
    • Whether chronic ethanol alters astrocytic ENT1 expression not tested
  14. 2023 High

    Myocyte-specific Ent1 deletion was shown to reduce infarct size through elevated reperfusion adenosine that signals via A2B receptors specifically on myeloid cells, resolving the inter-cellular pathway of ENT1-mediated cardioprotection.

    Evidence Myocyte-specific and myeloid-specific Adora2b conditional KO mice with myocardial I/R, adenosine measurements

    PMID:37288658

    Open questions at the time
    • Downstream myeloid effector mechanisms not identified
    • Temporal window for ENT1 inhibition-based cardioprotection not defined
  15. 2025 High

    ENT1-mediated adenosine uptake into T cells was shown to inhibit PRPS activity and suppress de novo pyrimidine synthesis, establishing a metabolic checkpoint that limits antitumor immunity; ENT1 inhibition or deletion enhanced CD8+ T cell effector function and potentiated PD-1 blockade.

    Evidence ENT1-deficient mice, PRPS enzymatic assay, pyrimidine metabolite quantification, co-culture killing assays, humanized mouse tumor model with anti-PD-1

    PMID:39652568 PMID:40355731

    Open questions at the time
    • Whether ENT1 inhibition synergizes with other checkpoint immunotherapies not tested
    • Impact on T cell exhaustion programs not characterized
  16. 2025 High

    ENT1 was identified as a plasma membrane transporter for nicotinamide, establishing its role in NAD+ homeostasis beyond nucleosides; ENT1/2 knockdown impaired mitochondrial respiration and promoted cellular senescence.

    Evidence ENT1/2 knockdown, NAM uptake assays, metabolomics, transcriptomics, mitochondrial respiration and senescence assays with NMN rescue

    PMID:39885119

    Open questions at the time
    • Relative contribution of ENT1 vs ENT2 to NAM transport not individually quantified
    • In vivo NAD+ homeostasis in ENT1-null tissues not measured

Open questions

Synthesis pass · forward-looking unresolved questions
  • Key unresolved questions include the substrate-bound structure and full conformational cycle of ENT1, the molecular mechanism linking ENT1 loss to ectopic mineralization, the oligomeric stoichiometry and its functional significance, and whether therapeutic ENT1 inhibition can be harnessed for immuno-oncology or cardioprotection without disrupting nucleotide homeostasis.
  • No substrate-bound or inward-open conformation structure available
  • Mechanism of ectopic mineralization in Augustine-null individuals unknown
  • Therapeutic window for ENT1 inhibition in immunotherapy not defined

Mechanism profile

Synthesis pass · controlled-vocabulary classification · explore literature graph →
Molecular activity
GO:0005215 transporter activity 6
Localization
GO:0005886 plasma membrane 5
Pathway
R-HSA-162582 Signal Transduction 7 R-HSA-382551 Transport of small molecules 6 R-HSA-1430728 Metabolism 3 R-HSA-168256 Immune System 2
Partners
ADORA1ADORA2AADORA2BAMPKBPGMCALM1PRKCE

Evidence

Reading pass · 44 per-paper findings extracted from the source corpus
Year Finding Method Journal Conf PMIDs
2019 Crystal structures of hENT1 in complex with two adenosine reuptake inhibitors (dilazep and NBMPR) were solved, revealing two distinct inhibitory mechanisms: dilazep occupies the substrate-binding site while NBMPR engages a distinct binding mode. Combined mutagenesis validated residues critical for adenosine recognition and transport. X-ray crystallography combined with site-directed mutagenesis and functional transport assays Nature structural & molecular biology High 31235912
2000 hENT1 stably expressed in nucleoside transporter-deficient PK15NTD cells shows high-affinity NBMPR binding (Kd ~0.4 nM), ~34,000 transporters per cell, a turnover number of 46 molecules/s for uridine, and broad selectivity for purine and pyrimidine nucleosides; it is ~7000-fold more sensitive to NBMPR than hENT2. hENT1 runs as a 40 kDa protein on SDS-PAGE and is N-glycosylated (deglycosylates to 37 kDa). Stable transfection in nucleoside transporter-deficient cells, radioligand binding ([3H]NBMPR), [3H]uridine uptake kinetics, peptide-N-glycosidase F and endoglycosidase H treatment The Journal of biological chemistry High 10722669
2016 N-linked glycosylation of hENT1 occurs exclusively at Asn48 in the first extracellular loop; the N48Q mutant reaches the plasma membrane but at reduced levels and is non-functional in chloroadenosine transport assays. N48Q ENT1 also fails to co-immunoprecipitate with itself or wild-type hENT1, indicating glycosylation is required for oligomerization as well as localization and function. Site-directed mutagenesis, PNGase-F deglycosylation, NBMPR binding (Bmax), chloroadenosine transport assay, immunofluorescence microscopy, co-immunoprecipitation Bioscience reports High 27480168
2011 ENT1 (hENT1 and mENT1) is directly phosphorylated at serine residues. PKC specifically phosphorylates serines 279 and 286 and threonine 274 in the large intracellular loop (between TM6 and TM7), while PKA phosphorylates multiple sites within this loop, as determined by in vitro kinase assays on His/Ub-tagged loop peptides. Affinity purification of overexpressed tagged ENT1, phosphoamino acid analysis, in vitro kinase assays with PKA and PKC on intracellular loop peptides Molecular membrane biology High 21809900
2016 Calmodulin (CaM) interacts with hENT1 via a conserved 1-5-10 CaM-binding motif in a calcium-dependent manner. Calcium chelation (EGTA, BAPTA-AM) decreases nucleoside and nucleoside analog drug uptake, while increasing intracellular calcium (thapsigargin) increases uptake. NMDA receptor activation also increases ENT1-mediated nucleoside uptake via CaM, blocked by CaM antagonist W7. Co-immunoprecipitation/biochemical pull-down for CaM-ENT1 interaction, pharmacological manipulation of calcium and CaM in functional uptake assays (HEK293, RT4, U-87 MG cells), NMDA receptor activation/antagonism American journal of physiology. Cell physiology Medium 27009875
2009 Nitric oxide reduces SLC29A1 promoter activity and hENT1-mediated adenosine transport in HUVECs from gestational diabetes via the hCHOP-C/EBPα transcription factor complex binding to the SLC29A1 promoter. Mutation of the hCHOP-C/EBPα consensus site (-1845G>T, -1844C>A) blocks this repression, and eNOS knockdown reverses the effect. Luciferase reporter assay (SLC29A1 promoter constructs), chromatin immunoprecipitation, overlap extension mutagenesis, eNOS siRNA adenovirus knockdown, adenosine uptake assays in primary HUVECs Cardiovascular research High 20032083
2006 Nitric oxide reduces SLC29A1 promoter activity and hENT1 expression in HUVECs from gestational diabetes; the effect maps to the region between -2154 and -1114 bp of the promoter and is blocked by NOS inhibitor L-NAME and mimicked by NO donor SNAP in normal cells. Adenovirus-silenced eNOS increases hENT1 expression and activity. Luciferase reporter assays with SLC29A1 promoter deletion constructs, adenoviral eNOS siRNA knockdown, adenosine uptake assays, pharmacological NOS inhibitors and NO donors in primary HUVECs Journal of cellular physiology High 16688763
2008 High D-glucose reduces hENT1-mediated adenosine transport and SLC29A1 promoter activity in HUVECs through increased Sp1 binding to the promoter, in a manner dependent on eNOS, MEK/ERK, and PKC activity. Sp1 overexpression alone reduces SLC29A1 promoter activity in normal glucose. Luciferase reporter assay (SLC29A1 promoter constructs), chromatin immunoprecipitation for Sp1 binding, pharmacological inhibitors (L-NAME, PD-98059, calphostin C), Sp1 overexpression, adenosine uptake assays in primary HUVECs Journal of cellular physiology High 18064606
2008 High glucose suppresses ENT1 expression and NBTI-sensitive adenosine uptake in rat cardiac fibroblasts via PKC-ζ, Raf-1, MEK, and p38 MAPK signaling pathways (not via nitric oxide or PI3K/mTOR). Isozyme-selective inhibitors demonstrated that Ca2+-dependent PKC isoforms are not involved. Pharmacological inhibitors targeting PKC (Go 6983, Go 6976, PKC-ζ pseudosubstrate), MEK (PD98059), Raf (GW 5074), p38 MAPK (SB 203580), PI3K (wortmannin), mTOR (rapamycin); ENT1 mRNA quantification and [3H]adenosine uptake assays in primary rat cardiac fibroblasts Journal of cellular physiology Medium 17941087
2010 JNK activation rapidly reduces mENT1 mRNA, promoter activity, and transport function. c-Jun (but not its Ser63/73Ala mutant) decreases mENT1 promoter activity and binds an AP-1 site at -1196 of the promoter, demonstrating that JNK-c-Jun signaling negatively regulates ENT1 transcription. JNK pharmacological activation, mENT1 promoter luciferase assay, c-Jun overexpression and dominant-negative mutant (Ser63/73Ala), chromatin binding assay (AP-1 site), mRNA quantification, [3H]uridine uptake in mouse myeloid leukemic cells Biochemical and biophysical research communications High 21145879
2001 Mouse ENT1 has an alternatively spliced isoform (mENT1.2) lacking Ser254 in a consensus casein kinase II phosphorylation site; both isoforms show similar pharmacological inhibition by NBMPR and dipyridamole and comparable selectivity for purine and pyrimidine nucleosides when stably expressed in CEM/C19 cells. cDNA cloning, genomic DNA analysis (alternative splicing at exon 7), stable transfection in nucleoside transporter-deficient cells, [3H]adenosine uptake inhibition assays Gene Medium 11179696
2000 The mouse ENT1 gene is located on chromosome 17C, spans ~12 kb, contains 12 exons and 11 introns, and its 5'-flanking region contains functional Sp1 and MAZ binding sites (-296 to -313 and -353 to -528 bp) that serve as positive regulators of transcription, as demonstrated by luciferase reporter assays in NG108-15 cells. Genomic cloning, primer extension (transcription start site mapping), luciferase reporter assay with 5'-flanking deletion constructs in NG108-15 cells Biochemical and biophysical research communications Medium 11027664
2009 FLT3-ITD expression in myeloid leukemia cells reduces ENT1 promoter activity and cellular ara-C uptake via HIF-1α upregulation. HIF-1α overexpression alone reduces ENT1 promoter activity, and the FLT3 inhibitor PKC412 rescues ENT1 promoter activity and ara-C uptake in FLT3-ITD cells. ENT1 promoter luciferase assay, [3H]ara-C uptake, HIF-1α overexpression, FLT3 inhibitor (PKC412) treatment in FLT3-ITD-expressing murine and human myeloid cell lines Biochemical and biophysical research communications Medium 19853583
2008 ENT1 contains a single missense mutation G24R in transmembrane domain 1 (TM1) in ara-C-resistant CCRF-CEM cells. G24R ENT1 localizes to the plasma membrane but cannot bind [3H]NBMPR or transport nucleosides. Additional G24 mutants (G24E, G24A) also show reduced ENT1-dependent activity, identifying G24 as a critical residue for nucleoside uptake. DNA sequencing of resistant cells, site-directed mutagenesis (G24R, G24E, G24A), EGFP-tagged ENT1 localization by fluorescence microscopy, [3H]NBMPR binding, [3H]uridine and [3H]ara-C uptake assays FEBS letters High 19116148
2003 ENT1 (rENT1) is expressed in dorsal horn laminae I-III and modulates glutamatergic synaptic transmission in rat spinal cord. NBMPR (ENT1 inhibitor) attenuates evoked EPSCs in a concentration-dependent, adenosine A1 receptor-dependent manner, reduces miniature EPSC frequency (not amplitude), and increases the paired-pulse ratio, consistent with presynaptic modulation. Immunohistochemistry, whole-cell patch-clamp recording in spinal cord slices, pharmacological dissection with NBMPR, A1 receptor antagonist (DPCPX), adenosine deaminase, and A1 receptor agonist (CCPA) The Journal of physiology High 12611914
2012 ENT1 deletion (Ent1-/-) in mice results in elevated circulating adenosine levels (~2-fold higher) and increased extracellular adenosine in isolated cardiomyocytes following hypoxic challenge. ENT1-null cardiomyocytes show elevated expression of cardioprotective genes and increased cAMP levels via adenosine receptor activation, indicating ENT1 modulates purinergic/adenosine receptor-dependent signaling. ENT1 knockout mice, HPLC nucleoside/nucleotide quantification in plasma and cardiomyocytes, hypoxic challenge of isolated cardiomyocytes, cAMP measurement, PCR array for hypoxia-related gene expression, dipyridamole pharmacology Life sciences High 21872611
2012 In mice, Ent1 deletion (but not Ent2 deletion) confers protection against renal ischemia-reperfusion injury. The protective mechanism involves crosstalk between renal Ent1 and Adora2b (A2B adenosine receptor) on vascular endothelia to prevent a postischemic no-reflow phenomenon, as demonstrated by adenosine receptor knockout studies. Global Ent1-/- and Ent2-/- mice, pharmacological ENT inhibition, kidney ischemia-reperfusion model, adenosine receptor (A1, A2A, A2B, A3) knockout mice, measurement of renal adenosine levels and perfusion The Journal of clinical investigation High 22269324
2013 ENT1 in cardiomyocytes is inhibited by ethanol (5-200 mM) by up to 27%, reducing [3H]2-chloroadenosine uptake. This inhibition is kinase-dependent: pharmacological PKA/PKC activation alters ethanol sensitivity, and primary cardiomyocytes from PKCε-null mice show ~37% greater ENT1 inhibition by ethanol, implicating PKCε in the ethanol-ENT1 interaction. [3H]2-chloroadenosine uptake in HL-1 cardiomyocytes with ethanol, PKA/PKC pharmacological modulators, primary cardiomyocytes from PKCε-null mice Purinergic signalling Medium 24163005
2010 ENT1 knockdown or pharmacological inhibition in cultured astrocytes reduces EAAT2 (glutamate transporter) mRNA expression and glutamate uptake activity; ENT1 overexpression upregulates EAAT2. Ethanol exposure increases EAAT2 expression, and ENT1 siRNA knockdown blocks this ethanol-induced upregulation, placing ENT1 upstream of EAAT2 regulation. ENT1 siRNA knockdown, ENT1 overexpression, pharmacological ENT1 inhibition, qRT-PCR (EAAT2 mRNA), glutamate uptake assay in cultured astrocytes Alcoholism, clinical and experimental research Medium 20374202
2013 In mice lacking ENT1, decreased A2A adenosine receptor-mediated CREB activity in the dorsomedial striatum (DMS) enhances goal-directed ethanol drinking. A2A receptor antagonist ZM241385 dampens PKA signaling in the DMS and promotes excessive ethanol drinking in WT but not ENT1-/- mice. Dominant-negative CREB in DMS causally reduces A2AR signaling and increases ethanol drinking, establishing ENT1→adenosine→A2AR→CREB as the pathway. ENT1 knockout mice, CRE-lacZ reporter mice, dominant-negative CREB viral injection, A2AR antagonist pharmacology, operant conditioning for ethanol, immunohistochemistry The Journal of neuroscience High 23467349
2016 Ticagrelor inhibits platelet ENT1, leading to accumulation of extracellular adenosine, activation of Gs-coupled adenosine A2A receptors, and elevated cAMP and VASP phosphorylation. Ticagrelor also acts as an inverse agonist at P2Y12R, blocking constitutive agonist-independent Gi signaling and increasing cAMP independently of adenosine receptors. Ca2+ flux assays in washed platelets, cAMP measurement, VASP-P (flow cytometry), adenosine A2A receptor antagonists, 1321N1 cells stably transfected with P2Y12R, pharmacological dissection Blood High 27694321
2021 ENT1-mediated adenosine transport is critical for cAMP homeostasis and regulation of erythroid transcription factors. ENT1-null individuals (Augustine-null blood type) exhibit macrocytosis, abnormal nucleotide metabolome, and defective erythropoiesis. CD34+ shRNA-ENT1 knockdown shows defective erythroid differentiation. Pharmacological inhibition of the ABCC4 cyclic nucleotide exporter rescues erythropoiesis in Ent1-/- mice, establishing ENT1-cAMP-ABCC4 axis. Human ENT1-null (Augustine-null) subjects, shRNA knockdown of ENT1 in human CD34+ progenitors, Ent1-/- mouse model, nucleotide metabolomics, ABCC4 inhibitor pharmacology, flow cytometry for erythroid differentiation Blood High 33690842
2023 Erythrocyte ENT1 (eENT1) mediates adenosine uptake that activates AMPK (by controlling the AMP/ATP ratio) and its downstream target BPGM, which produces 2,3-BPG to enhance O2 delivery. Loss of eENT1 abolishes AMPK-BPGM activation, reduces 2,3-BPG and glutathione, increases ROS, activates AMPD3, and leads to severe renal hypoxia and CKD progression. Genetic ablation of AMPD3 preserves the adenine nucleotide pool and rescues the phenotype. Erythrocyte-specific eEnt1-/- mice and global Ampd3-/- mice, two CKD models (Ang II infusion, UUO), unbiased metabolomics, isotopic adenosine flux, AMPK/BPGM/2,3-BPG/ROS measurements, translational studies in patients with CKD and cultured human erythrocytes Journal of the American Society of Nephrology High 37725437
2020 Maternal erythrocyte ENT1 (eENT1)-dependent adenosine uptake activates AMPK (via AMP/ATP ratio control) and BPGM, increasing 2,3-BPG production and O2 delivery to the placenta. Loss of maternal eENT1 elevates placental HIF-1α, reduces LAT1 expression/activity and amino acid supply to the fetus, causing fetal growth restriction. Erythrocyte-specific eENT1 knockout dams, isotopic adenosine flux, high-throughput metabolomics, AMPK/BPGM pathway analysis, placental HIF-1α and LAT1 measurement, human trophoblast cell culture with HIF-1α manipulation JCI insight High 32434995
2025 ENT1-mediated adenosine uptake into activated T cells inhibits phosphoribosyl pyrophosphate synthetase (PRPS) activity, thereby suppressing de novo pyrimidine nucleotide (UMP) synthesis required for DNA and RNA synthesis, resulting in T cell suppression. ENT1 inhibition with EOS301984 restores pyrimidine levels and enhances T cell anti-tumor activity; ENT1 deficiency potentiates PD-1 blockade in a humanized mouse model. ENT1-deficient mice, CD8+ T cell functional assays, transcriptomic profiling, PRPS activity assay, pyrimidine metabolite quantification, co-culture tumor killing assay, in vivo humanized mouse tumor model with anti-PD-1 Nature immunology High 40355731
2025 ENT1 (SLC29A1) and ENT2 (SLC29A2) transport nicotinamide (NAM) across the plasma membrane, establishing cellular NAD+ homeostasis. ENT1/2 knockdown reduces cellular NAM uptake, alters NAD+-dependent metabolite composition and gene expression, impairs mitochondrial respiration, and promotes cellular senescence — effects reversed by NMN supplementation. ENT1/ENT2 knockdown, cellular NAM uptake assays, metabolomics, transcriptomics, mitochondrial respiration assays, senescence assays, NMN rescue Nature communications High 39885119
2025 ENT1-mediated adenosine uptake into T cells suppresses antitumor immunity. Blocking or deleting host ENT1 enhances CD8+ T cell-dependent anti-tumor responses with increased effector cytokines (IFNγ, TNFα, IL-2, granzyme B, CXCL10), reduced T regulatory cells and CD206hi macrophages, and decreased CCL17 production. ENT1-deficient mice, CD8+ T cell depletion, transcriptomic profiling, flow cytometry for immune infiltration, ex vivo tumor-infiltrating lymphocyte expansion, co-culture tumor killing assays Cancer research High 39652568
2022 ENT1 mediates salvage of extracellular uridine to generate pyrimidine nucleotides independent of DHODH, conferring resistance to DHODH inhibitors in pancreatic cancer. CNX-774 inhibits ENT1 (independently of BTK), and dual blockade of DHODH and ENT1 causes profound pyrimidine starvation and tumor suppression in vivo. Small molecule combination screen, mechanistic studies with BTK-null cell lines, [3H]uridine uptake assays, pyrimidine nucleotide quantification, cell viability assays, immunocompetent mouse pancreatic cancer model Cancer letters High 36341997
2012 ENT1 is the primary ribavirin transporter in a hepatitis C virus replication cell system (OR6 cells). Inhibition of ENT1 by NBMPR or miR-ENT1 knockdown proportionally reduces ribavirin accumulation and antiviral activity, demonstrating that ENT1-mediated uptake directly determines ribavirin efficacy. mRNA expression analysis, [3H]ribavirin uptake assays, NBMPR pharmacological inhibition, miR-ENT1 knockdown, HCV replication assay (OR6 cells) Antimicrobial agents and chemotherapy High 22232287
2018 ENT1 (SLC29A1) plays the dominant role in abacavir uptake across the placenta. ENT1 activity was identified in BeWo cells, human villous fragments, and microvillous plasma membrane vesicles using [3H]abacavir uptake and selective inhibitors. Dually perfused rat placentas confirmed that Ent1 contributes significantly to overall placental abacavir transport. BeWo cell uptake assays, human placental villous fragment and MVM vesicle transport assays, NBMPR and Na+-free conditions, dually perfused rat term placenta model, SLC29A1 expression quantification (first and third trimester) Drug metabolism and disposition High 30097436
2022 Astrocytic ENT1 limits the striatal extracellular adenosine tone that tonically inhibits dopamine release in nucleus accumbens core via adenosine A1 receptors. Viral overexpression of ENT1 in astrocytes enhances dopamine release and relieves A1R-mediated inhibition; ENT1 inhibition elevates adenosine tone. Ethanol (50 mM) promotes A1R-mediated inhibition of dopamine release by diminishing adenosine uptake via ENT1. Fast-scan cyclic voltammetry for dopamine release in ex vivo slices, optogenetic stimulation, viral ENT1 overexpression in astrocytes, GRAB-adenosine sensor (fiber photometry), gliotoxin (fluorocitrate), pharmacological ENT1 inhibition, A1R agonists and antagonists The Journal of neuroscience High 35042768
2010 In ENT1-/- microvascular endothelial cells (MVECs), ENT2 and ENBT1 expression are unchanged, leaving very low nucleoside uptake but intact nucleobase accumulation. Loss of ENT1 is accompanied by dramatically increased adenosine deaminase activity and adenosine A2a receptor expression (transcript and protein), representing adaptive compensatory mechanisms. ENT1-/- mouse-derived MVECs, transport assays, immunoblotting, transcript analysis for ENT subtypes and adenosine deaminase/A2a receptor in WT vs KO cells American journal of physiology. Heart and circulatory physiology Medium 20543083
2010 Human erythrocyte ENT1 functions at ice-cold temperatures (~0.5-0.7°C), displaying saturable [3H]uridine uptake kinetics, NBMPR inhibition, and trans-stimulation (overshoot) by unlabeled uridine or ribavirin in rightside-out membrane vesicles, demonstrating that ENT1 operates as a facilitative exchanger/transporter at near-freezing temperatures. Rightside-out membrane vesicles from human erythrocytes, [3H]uridine and [3H]ribavirin uptake at 23°C and ~0.6°C, NBMPR and dipyridamole inhibition, trans-stimulation assays, intact red blood cell studies Drug metabolism and pharmacokinetics Medium 20814156
2023 Myocyte-specific Ent1 deletion (Ent1loxP/loxP Myosin Cre+) reduces myocardial infarct size. The cardioprotection works by maintaining elevated postischemic adenosine levels during reperfusion, which signals through Adora2b on myeloid-inflammatory cells (Adora2bloxP/loxP LysM Cre+ studies). Global Ent1-/- but not Ent2-/- mice are cardioprotected, and the effect is abolished by myeloid-specific Adora2b deletion. Myocyte-specific and myeloid-specific conditional KO mice, global Ent1/Ent2 KO, myocardial ischemia-reperfusion model, infarct size measurement, cardiac adenosine level measurement, dipyridamole pharmacology JCI insight High 37288658
2003 Genetic variants of hENT1 (ENT1-I216T and ENT1-E391K) show no differences in nucleoside or nucleoside analog uptake kinetics compared to reference ENT1 when expressed in Saccharomyces cerevisiae, indicating these coding variants do not alter transport function. Expression of variant ENT1 in S. cerevisiae, kinetic uptake assays for nucleosides and nucleoside analogs, haplotype analysis Pharmacogenetics Medium 12724623
2011 ENT1 deletion in mice leads to loss of ENT1-mediated nucleoside uptake with elevated plasma thymidine levels (~1.65-fold), altered 18F-FLT biodistribution (reduced blood uptake, increased spleen and bone marrow uptake), and reduced 18F-FLT uptake in ENT1-knockdown xenograft tumors, demonstrating ENT1 as an important mediator of thymidine analog uptake in vivo. ENT1-/- mice, NBMPR-P pharmacological inhibition, 18F-FLT PET imaging, ex vivo gamma counting, [3H]FLT uptake assay in ENT1-knockdown A549 cells, LC-MS for plasma thymidine, immunoblotting and immunohistochemistry Journal of nuclear medicine High 20720035
2014 Bone marrow stromal cells secrete a soluble factor that reduces ENT1 activity by ~50% in leukemia cells (measured as [3H]adenosine uptake), reducing cytarabine incorporation and conferring chemoprotection. CXCR4 inhibitor-mediated mobilization of leukemia cells from bone marrow reverses this protection in vivo. [3H]adenosine uptake assay in leukemia cells exposed to BM stromal cell-conditioned media, in vivo CXCR4 inhibitor treatment, mouse leukemia model survival analysis, flow cytometry/western blot for apoptosis PloS one Medium 22629369
2017 FBW7 overexpression in pancreatic cancer cells increases ENT1 protein levels (not mRNA), and lysosome inhibition also increases ENT1 protein, suggesting ENT1 is regulated post-translationally via lysosomal degradation. Increased ENT1 by FBW7 correlates with enhanced gemcitabine sensitivity. FBW7 overexpression, lysosome inhibitor treatment, immunoblotting for ENT1 protein and mRNA, gemcitabine cytotoxicity assay in pancreatic cancer cell lines Oncology reports Medium 28765935
2022 Molecular dynamics simulations reveal that hENT1 transitions from outward-open to occluded state are driven primarily by TM1, TM2, TM7, and TM9. One trimethoxyphenyl ring of dilazep competitively occupies the orthosteric adenosine-binding site, while the other occupies an opportunistic extracellular site via VDW interactions with N30, M33, M84, P308, and F334, blocking the transport cycle. Long-time unbiased molecular dynamics simulations based on crystal structure of hENT1 Current research in structural biology Low 35677775
2011 Functional analysis showed that prolonged ethanol exposure increases adenosine uptake activity of the ENT1-216Thr variant (encoded by the 647C SNP) compared to wild-type ENT1-216Ile transfected cells, suggesting this variant reduces extracellular adenosine levels and may contribute to alcohol withdrawal seizure risk. Stable transfection of ENT1-216Ile vs ENT1-216Thr in cells, [3H]adenosine uptake assay before and after prolonged ethanol exposure PloS one Medium 21283641
2003 NBMPR binding (reflecting ENT1 surface expression/activity) is significantly decreased in the basal forebrain but not cortex after 6 hours of sleep deprivation in rats, without changes in ENT1 mRNA, suggesting post-translational regulation of ENT1 activity in the basal forebrain contributes to adenosine accumulation during prolonged wakefulness. [3H]NBMPR binding in brain tissue extracts, in situ hybridization for ENT1 mRNA in sleep-deprived vs control rats Journal of sleep research Medium 14633241
2019 Loss of ENT1 in the annulus fibrosus of intervertebral discs leads to increased E2f transcription factor and CDK1/Mcm5/PCNA expression, JNK MAPK pathway activation, and increased cell proliferation in AF tissue, linking ENT1-mediated adenosine transport to cell cycle control. ENT1-/- mice, microarray analysis of AF tissue, qPCR validation of E2f family and Rb1/Cdk2, immunoblotting (JNK, CDK1, Mcm5, PCNA), PCNA immunostaining for proliferating cells Journal of cellular physiology Medium 31010267
2019 ZIP4 activates STAT3 to induce ZEB1 expression, which activates ITGA3 and ITGB1 (integrin α3β1). Subsequent integrin α3β1 signaling via JNK inhibits ENT1 expression (transcriptionally), reducing gemcitabine uptake in pancreatic cancer cells. Chromatin immunoprecipitation, luciferase reporter assays for ENT1 promoter, shRNA knockdown of ZIP4/ZEB1/ITGA3/ITGB1, LC-MS/MS for gemcitabine quantification, xenograft mouse models Gastroenterology High 31711924
2015 A nonsynonymous SNP in SLC29A1 (rs45458701, p.Glu391Lys) is responsible for the Augustine-negative (At(a-)) blood type, while a null mutation (c.589+1G>C) causes the Augustine-null blood type. Individuals homozygous for the null mutation (lacking ENT1) exhibit periarticular and ectopic mineralization, establishing ENT1's role in bone/tissue homeostasis in humans. Genetic sequencing of At(a-) individuals, identification of SLC29A1 null mutation in individuals with ectopic mineralization, functional assessment of p.Glu391Lys (previously shown not to alter nucleoside transport) Blood Medium 25896650

Source papers

Stage 0 corpus · 100 papers · ranked by NIH iCite citations
Year Title Journal Citations PMID
2000 Kinetic and pharmacological properties of cloned human equilibrative nucleoside transporters, ENT1 and ENT2, stably expressed in nucleoside transporter-deficient PK15 cells. Ent2 exhibits a low affinity for guanosine and cytidine but a high affinity for inosine. The Journal of biological chemistry 271 10722669
2019 ZIP4 Increases Expression of Transcription Factor ZEB1 to Promote Integrin α3β1 Signaling and Inhibit Expression of the Gemcitabine Transporter ENT1 in Pancreatic Cancer Cells. Gastroenterology 126 31711924
2003 The yeast Epsin Ent1 is recruited to membranes through multiple independent interactions. The Journal of biological chemistry 105 12529323
2012 Equilibrative nucleoside transporter 1 (ENT1) regulates postischemic blood flow during acute kidney injury in mice. The Journal of clinical investigation 90 22269324
2019 Structures of human ENT1 in complex with adenosine reuptake inhibitors. Nature structural & molecular biology 89 31235912
1999 Distribution of equilibrative, nitrobenzylthioinosine-sensitive nucleoside transporters (ENT1) in brain. Journal of neurochemistry 85 10428086
2013 Ceftriaxone treatment affects the levels of GLT1 and ENT1 as well as ethanol intake in alcohol-preferring rats. Journal of molecular neuroscience : MN 82 23893122
2013 Adenosine transporter ENT1 regulates the acquisition of goal-directed behavior and ethanol drinking through A2A receptor in the dorsomedial striatum. The Journal of neuroscience : the official journal of the Society for Neuroscience 80 23467349
2016 Inverse agonism at the P2Y12 receptor and ENT1 transporter blockade contribute to platelet inhibition by ticagrelor. Blood 75 27694321
2003 Functional characterization in yeast of genetic variants in the human equilibrative nucleoside transporter, ENT1. Pharmacogenetics 62 12724623
2003 Control of glutamatergic neurotransmission in the rat spinal dorsal horn by the nucleoside transporter ENT1. The Journal of physiology 52 12611914
2018 Adenosine Augmentation Evoked by an ENT1 Inhibitor Improves Memory Impairment and Neuronal Plasticity in the APP/PS1 Mouse Model of Alzheimer's Disease. Molecular neurobiology 50 29616397
2011 Equilibrative nucleoside transporter 1 (ENT1) is critical for pollen germination and vegetative growth in Arabidopsis. Journal of experimental botany 48 21642237
2001 Characterisation of a concentrative type of adenosine transporter from Arabidopsis thaliana (ENT1,At). FEBS letters 48 11749958
2010 Biodistribution and uptake of 3'-deoxy-3'-fluorothymidine in ENT1-knockout mice and in an ENT1-knockdown tumor model. Journal of nuclear medicine : official publication, Society of Nuclear Medicine 45 20720035
2009 Nitric oxide reduces SLC29A1 promoter activity and adenosine transport involving transcription factor complex hCHOP-C/EBPalpha in human umbilical vein endothelial cells from gestational diabetes. Cardiovascular research 42 20032083
2010 ENT1 regulates ethanol-sensitive EAAT2 expression and function in astrocytes. Alcoholism, clinical and experimental research 40 20374202
2006 Nitric oxide reduces adenosine transporter ENT1 gene (SLC29A1) promoter activity in human fetal endothelium from gestational diabetes. Journal of cellular physiology 40 16688763
2015 Lack of the nucleoside transporter ENT1 results in the Augustine-null blood type and ectopic mineralization. Blood 38 25896650
2004 Distribution of CNT2 and ENT1 transcripts in rat brain: selective decrease of CNT2 mRNA in the cerebral cortex of sleep-deprived rats. Journal of neurochemistry 38 15287894
2017 Targeting ENT1 and adenosine tone for the treatment of Huntington's disease. Human molecular genetics 37 28069792
2009 FLT3-ITD induces ara-C resistance in myeloid leukemic cells through the repression of the ENT1 expression. Biochemical and biophysical research communications 35 19853583
2013 Genetic polymorphisms of SLC28A3, SLC29A1 and RRM1 predict clinical outcome in patients with metastatic breast cancer receiving gemcitabine plus paclitaxel chemotherapy. European journal of cancer (Oxford, England : 1990) 34 24361227
2011 Functional role of the polymorphic 647 T/C variant of ENT1 (SLC29A1) and its association with alcohol withdrawal seizures. PloS one 33 21283641
2011 Absence of equilibrative nucleoside transporter 1 in ENT1 knockout mice leads to altered nucleoside levels following hypoxic challenge. Life sciences 33 21872611
2006 Thirty novel genetic variations in the SLC29A1 gene encoding human equilibrative nucleoside transporter 1 (hENT1). Drug metabolism and pharmacokinetics 33 16858130
2021 The equilibrative nucleoside transporter ENT1 is critical for nucleotide homeostasis and optimal erythropoiesis. Blood 32 33690842
2001 Cloning of a novel isoform of the mouse NBMPR-sensitive equilibrative nucleoside transporter (ENT1) lacking a putative phosphorylation site. Gene 32 11179696
2012 Bone marrow stromal cells modulate mouse ENT1 activity and protect leukemia cells from cytarabine induced apoptosis. PloS one 31 22629369
2017 FBW7 increases the chemosensitivity of pancreatic cancer cells to gemcitabine through upregulation of ENT1. Oncology reports 29 28765935
2012 ENT1, a ribavirin transporter, plays a pivotal role in antiviral efficacy of ribavirin in a hepatitis C virus replication cell system. Antimicrobial agents and chemotherapy 28 22232287
2020 ENT1 inhibition attenuates apoptosis by activation of cAMP/pCREB/Bcl2 pathway after MCAO in rats. Experimental neurology 27 32445645
2018 Equilibrative Nucleoside Transporter 1 (ENT1, SLC29A1) Facilitates Transfer of the Antiretroviral Drug Abacavir across the Placenta. Drug metabolism and disposition: the biological fate of chemicals 27 30097436
2011 Role of nucleoside transporters SLC28A2/3 and SLC29A1/2 genetics in ribavirin therapy: protection against anemia in patients with chronic hepatitis C. Pharmacogenetics and genomics 27 21346688
2011 The Equilibrative Nucleoside Transporter (ENT1) can be phosphorylated at multiple sites by PKC and PKA. Molecular membrane biology 27 21809900
2004 Gene-expression profiling reveals down-regulation of equilibrative nucleoside transporter 1 (ENT1) in Ara-C-resistant CCRF-CEM-derived cells. Journal of biochemistry 27 15632314
2014 ENT1 inhibition attenuates epileptic seizure severity via regulation of glutamatergic neurotransmission. Neuromolecular medicine 26 25490964
2012 Characterization of the Salmonella bacteriophage vB_SenS-Ent1. The Journal of general virology 26 22694898
2000 Genomic organization and expression of the mouse equilibrative, nitrobenzylthioinosine-sensitive nucleoside transporter 1 (ENT1) gene. Biochemical and biophysical research communications 25 11027664
2017 Potential role of polymorphisms in the transporter genes ENT1 and MATE1/OCT2 in predicting TAS-102 efficacy and toxicity in patients with refractory metastatic colorectal cancer. European journal of cancer (Oxford, England : 1990) 24 28992563
2008 High D-glucose reduces SLC29A1 promoter activity and adenosine transport involving specific protein 1 in human umbilical vein endothelium. Journal of cellular physiology 24 18064606
2023 Erythrocyte ENT1-AMPD3 Axis is an Essential Purinergic Hypoxia Sensor and Energy Regulator Combating CKD in a Mouse Model. Journal of the American Society of Nephrology : JASN 22 37725437
2019 Affinity, binding kinetics and functional characterization of draflazine analogues for human equilibrative nucleoside transporter 1 (SLC29A1). Biochemical pharmacology 22 31830468
2022 ENT1 blockade by CNX-774 overcomes resistance to DHODH inhibition in pancreatic cancer. Cancer letters 21 36341997
2016 Equilibrative nucleoside transporter ENT1 as a biomarker of Huntington disease. Neurobiology of disease 21 27567601
2014 Aberrant bone density in aging mice lacking the adenosine transporter ENT1. PloS one 21 24586402
2010 Regulation of ENT1 expression and ENT1-dependent nucleoside transport by c-Jun N-terminal kinase. Biochemical and biophysical research communications 21 21145879
2008 Identification of a novel point mutation in ENT1 that confers resistance to Ara-C in human T cell leukemia CCRF-CEM cells. FEBS letters 21 19116148
2022 Dopamine Release in Nucleus Accumbens Is under Tonic Inhibition by Adenosine A1 Receptors Regulated by Astrocytic ENT1 and Dysregulated by Ethanol. The Journal of neuroscience : the official journal of the Society for Neuroscience 20 35042768
2025 Inhibition of ENT1 relieves intracellular adenosine-mediated T cell suppression in cancer. Nature immunology 19 40355731
2020 Maternal erythrocyte ENT1-mediated AMPK activation counteracts placental hypoxia and supports fetal growth. JCI insight 19 32434995
2020 Decreased Equilibrative Nucleoside Transporter 1 (ENT1) Activity Contributes to the High Extracellular Adenosine Levels in Mesenchymal Glioblastoma Stem-Like Cells. Cells 19 32824670
2016 Novel regulation of equlibrative nucleoside transporter 1 (ENT1) by receptor-stimulated Ca2+-dependent calmodulin binding. American journal of physiology. Cell physiology 19 27009875
2003 Nitrobenzylthioinosine (NBMPR) binding and nucleoside transporter ENT1 mRNA expression after prolonged wakefulness and recovery sleep in the cortex and basal forebrain of rat. Journal of sleep research 18 14633241
2023 Targeting myocardial equilibrative nucleoside transporter ENT1 provides cardioprotection by enhancing myeloid Adora2b signaling. JCI insight 16 37288658
2019 Label-free detection of transporter activity via GPCR signalling in living cells: A case for SLC29A1, the equilibrative nucleoside transporter 1. Scientific reports 16 31551431
2014 Dilazep analogues for the study of equilibrative nucleoside transporters 1 and 2 (ENT1 and ENT2). Bioorganic & medicinal chemistry letters 16 25454272
2005 6-Benzylthioinosine analogues: promising anti-toxoplasmic agents as inhibitors of the mammalian nucleoside transporter ENT1 (es). Biochemical pharmacology 16 16310172
2022 Adenosine derivatives from Cordyceps exert antitumor effects against ovarian cancer cells through ENT1-mediated transport, induction of AMPK signaling, and consequent autophagic cell death. Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie 15 36076585
2016 SLC29A1 (ENT1) polymorphisms and outcome of complete remission in acute myeloid leukemia. Cancer chemotherapy and pharmacology 15 27422302
2010 Reduced effect of NMDA glutamate receptor antagonist on ethanol-induced ataxia and striatal glutamate levels in mice lacking ENT1. Neuroscience letters 15 20570605
2018 Identification of a Genomic Region between SLC29A1 and HSP90AB1 Associated with Risk of Bevacizumab-Induced Hypertension: CALGB 80405 (Alliance). Clinical cancer research : an official journal of the American Association for Cancer Research 14 29871907
2011 Sex-Specific Regulation of Depression, Anxiety-Like Behaviors and Alcohol Drinking in Mice Lacking ENT1. Journal of addiction research & therapy 14 23101030
2010 Nucleoside/nucleobase transport and metabolism by microvascular endothelial cells isolated from ENT1-/- mice. American journal of physiology. Heart and circulatory physiology 14 20543083
2010 Human erythrocyte nucleoside transporter ENT1 functions at ice-cold temperatures. Drug metabolism and pharmacokinetics 14 20814156
2025 SLC29A1 and SLC29A2 are human nicotinamide cell membrane transporters. Nature communications 13 39885119
2013 The adenosine transporter, ENT1, in cardiomyocytes is sensitive to inhibition by ethanol in a kinase-dependent manner: implications for ethanol-dependent cardioprotection and nucleoside analog drug cytotoxicity. Purinergic signalling 13 24163005
2022 PF-07321332 (Nirmatrelvir) does not interact with human ENT1 or ENT2: Implications for COVID-19 patients. Clinical and translational science 12 35505633
2019 Role of equilibrative nucleoside transporter 1 (ENT1) in the disposition of cytarabine in mice. Pharmacology research & perspectives 12 31832201
2016 Localization and Expression of Nucleoside Transporters ENT1 and ENT2 in Polar Cells of Intestinal Epithelium. Bulletin of experimental biology and medicine 12 27160886
2025 Adenosine Uptake through the Nucleoside Transporter ENT1 Suppresses Antitumor Immunity and T-cell Pyrimidine Synthesis. Cancer research 11 39652568
2018 Nrf2-ARE signaling pathway regulates the expressions of A1R and ENT1 in the brain of epileptic rats. European review for medical and pharmacological sciences 11 30402855
2017 Curcumin and its cyclohexanone analogue inhibited human Equilibrative nucleoside transporter 1 (ENT1) in pancreatic cancer cells. European journal of pharmacology 11 28365185
2014 Contribution of CNT1 and ENT1 to ribavirin uptake in human hepatocytes. Archives of pharmacal research 11 25011570
2012 Impact of solute carrier family 29 member 1 (SLC29A1) single nucleotide polymorphisms on mRNA expression in peripheral blood mononuclear cells. Biological & pharmaceutical bulletin 11 23095574
2008 High glucose suppresses expression of equilibrative nucleoside transporter 1 (ENT1) in rat cardiac fibroblasts through a mechanism dependent on PKC-zeta and MAP kinases. Journal of cellular physiology 11 17941087
2005 Localization of the NBMPR-sensitive equilibrative nucleoside transporter, ENT1, in the rat dorsal root ganglion and lumbar spinal cord. Brain research 11 16226730
2019 Quantification of ENT1 and ENT2 Proteins at the Placental Barrier and Contribution of These Transporters to Ribavirin Uptake. Journal of pharmaceutical sciences 10 31520644
2018 Regulation of hepatic glucose production and AMPK by AICAR but not by metformin depends on drug uptake through the equilibrative nucleoside transporter 1 (ENT1). Diabetes, obesity & metabolism 10 29962100
2016 N-linked glycosylation of N48 is required for equilibrative nucleoside transporter 1 (ENT1) function. Bioscience reports 10 27480168
2015 SLC29A1 polymorphism and prediction of anaemia severity in patients with chronic hepatitis C receiving triple therapy with telaprevir. The Journal of antimicrobial chemotherapy 10 25583751
2015 Effect of Hypoxanthine on Functional Activity of Nucleoside Transporters ENT1 and ENT2 in Caco-2 Polar Epithelial Intestinal Cells. Bulletin of experimental biology and medicine 10 26593410
2021 Differential Inhibition of Equilibrative Nucleoside Transporter 1 (ENT1) Activity by Tyrosine Kinase Inhibitors. European journal of drug metabolism and pharmacokinetics 9 34275128
2019 Loss of ENT1 increases cell proliferation in the annulus fibrosus of the intervertebral disc. Journal of cellular physiology 9 31010267
2019 Type 1 equilibrative nucleoside transporter (ENT1) regulates sex-specific ethanol drinking during disruption of circadian rhythms. Addiction biology 9 31267611
2016 Interleukin-1β Suppresses the Transporter Genes Ank and Ent1 Expression in Stromal Progenitor Cells Retaining Mineralization. Calcified tissue international 9 27086348
2002 Complex effects of sulfhydryl reagents on ligand interactions with nucleoside transporters: evidence for multiple populations of ENT1 transporters with differential sensitivities to N-ethylmaleimide. Archives of biochemistry and biophysics 8 12061806
2021 NBTI attenuates neuroinflammation and apoptosis partly by ENT1/NLRP3/Bcl2 pathway after subarachnoid hemorrhage in rats. Neuroreport 7 34718248
2012 On-pump inhibition of es-ENT1 nucleoside transporter and adenosine deaminase during aortic crossclamping entraps intracellular adenosine and protects against reperfusion injury: role of adenosine A1 receptor. The Journal of thoracic and cardiovascular surgery 7 22325325
2011 Analysis of recombinant tagged equilibrative nucleoside transporter 1 (ENT1) expressed in E. coli. Biochemistry and cell biology = Biochimie et biologie cellulaire 7 21455275
2024 Deep Brain Stimulation Inhibits Epileptic Seizures via Increase of Adenosine Release and Inhibition of ENT1, CD39, and CD73 Expression. Molecular neurobiology 6 39042219
2021 miR-33-3p Regulates PC12 Cell Proliferation and Differentiation In Vitro by Targeting Slc29a1. Neurochemical research 6 34152551
2021 Influence of FPGS, ABCC4, SLC29A1, and MTHFR genes on the pharmacogenomics of fluoropyrimidines in patients with gastrointestinal cancer from the Brazilian Amazon. Cancer chemotherapy and pharmacology 6 34331561
2024 The JNK Signaling Pathway Regulates Seizures Through ENT1 in Pilocarpine-Induced Epilepsy Rat Model. CNS neuroscience & therapeutics 5 39722194
2021 Potential role of CMPK1, SLC29A1, and TLE4 polymorphisms in gemcitabine-based chemotherapy in HER2-negative metastatic breast cancer patients: pharmacogenetic study results from the prospective randomized phase II study of eribulin plus gemcitabine versus paclitaxel plus gemcitabine (KCSG-BR-13-11). ESMO open 4 34438242
2018 Changes in aortic reactivity associated with the loss of equilibrative nucleoside transporter 1 (ENT1) in mice. PloS one 4 30408123
2012 Purification and crystallization of yeast Ent1 ENTH domain. Acta crystallographica. Section F, Structural biology and crystallization communications 4 22750874
2022 Insight into the nucleoside transport and inhibition of human ENT1. Current research in structural biology 3 35677775
2020 Adaptative mechanism of the equilibrative nucleoside transporter 1 (ENT-1) and blood adenosine levels in elite freedivers. European journal of applied physiology 3 33052430
2024 Development of a Novel HEK293 Cell Model Lacking SLC29A1 to Study the Pharmacology of Endogenous SLC29A2-Encoded Equilibrative Nucleoside Transporter Subtype 2. Drug metabolism and disposition: the biological fate of chemicals 2 39054074