ent1

ent1
ENT1 is a protein that mediates the cellular uptake of nucleosides from the surrounding medium. It is encoded by the SLC29A1 gene and expressed in various tissues, especially the liver, heart, testis and brain.
ENT1 (SLC29A1) is a sodium-independent transporter for purine and pyrimidine nucleosides and for some nucleobases. Nucleoside transporters are classified into two major classes, equilibrative bi-directional facilitators (ENTs) and Na+-dependent concentrative transporters (CNTs) [1].
Localization of ENT1 and/or 2 in human (A) hepatocytes, (B) kidney proximal tubule epithelial cells, (C) enterocytes of the small and large intestine, (D) microvascular endothelial cells of the blood-brain barrier, (E) Sertoli cells of the blood-testis barrier, and (F) placental syncytiotrophoblasts. ENTs are bidirectional transporters that support nucleoside/-tide transport down their ...
May 12, 2025
Equilibrative Nucleoside Transporter 1 (ENT1) is a subtype of equilibrative nucleoside transporters that is highly sensitive to inhibition by the nucleoside analogue NBMPR at low nanomolar concentrations.
ENT1 and 2 are located on the plasma membrane while ENT3 is located on intracellular membranes. ENTs are ubiquitously expressed throughout the body. In the human CNS, ENT1 is enriched in the frontal and parietal lobes, thalamus, midbrain, and basal ganglia. The distribution of ENT1 correlates with the distribution of A1R (Jennings et al, 2000).
ENT1 is a nucleoside transporter that regulates nucleotide homeostasis and erythroid differentiation. The article reports on the clinical and molecular features of ENT1 deficiency in humans and mice, and the role of ABCC4 in compensation.
Feb 17, 2025
The type 1 equilibrative nucleoside transporter (ENT1) is essential for regulating extracellular adenosine levels and has been implicated in various psychiatric disorders. While previous studies have investigated the expression of ENT1 in fetal and neonatal brains, its neuroanatomical distribution in adult and aged mouse brains has not been fully elucidated. Therefore, in this study, we ...
ENT1 Equilibrative nucleoside transporter 1 (ENT1) is a type of equilibrative nucleoside transporter that facilitates the transport of nucleosides across cell membranes in both directions based on concentration gradients. It is one of four known ENTs (ENT1, ENT2, ENT3, and ENT4). Adenosine re-uptake is influenced by alcohol by obstructing ENT1.
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Dec 30, 2024
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The final dilazep-bound human ENT1 structure is of excellent quality with a Free-R factor of 24%. We also crystallized hENT1 cryst in complex with the nucleoside-derived AdoRI NBMPR, which exhibits merohedral twinning.
The human equilibrative nucleoside transporter 1 (hENT1) is an effective controller of adenosine signaling by regulating its extracellular and intrace…
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Nov 14, 2025
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The adenosine transporter 1 (ENT1) transports nucleosides, such as adenosine, and cytotoxic nucleoside analog drugs. ENT1 is well established to play a role in adenosinergic signaling in the cardiovascular system by modulating adenosine levels. ...
Equilibrative nucleoside transporters (ENTs) are polytopic integral membrane proteins that mediate the transport of nucleosides, nucleobases, and therapeutic analogs. The best-characterized ENTs are the human transporters hENT1 and hENT2. However, ...
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Learn about ENT1, it's role in acute kidney injury (AKI), and how RAP-0001 inhibits ENT1 to mitigate renal damage during renal stress.
Nov 5, 2024
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Equilibrative nucleoside transporters (ENTs) 1 and 2 facilitate nucleoside transport across the blood-testis barrier (BTB). Improving drug entry into the testes with drugs that use endogenous transport pathways may lead to more effective treatments ...
Measurement of Ent1 transcript level in the mouse heart revealed essentially undetectable Ent1 mRNA levels in Ent1-/- mice (Figure 2A), while Ent2 transcript level remained intact (Figure 2B).
The adenosine transporter 1 (ENT1) transports nucleosides, such as adenosine, and cytotoxic nucleoside analog drugs. ENT1 is well established to play a role in adenosinergic signaling in the cardiovascular system by modulating adenosine levels. Moderate ethanol consumption is cardioprotective and un …
Feb 17, 2025
ENT1-KOmiceareviableandexhibitmildhematologicalchanges17as wellasincreasedplasmaadenosinelevels18.Adelayintumorgrowth wasobservedwhenMCA205(fibrosarcoma),MC38(colonadenocar- cinoma)andPan02 ...
To better understand the role of equilibrative nucleoside transporters (ENT) in purine nucleoside-dependent physiology of the cardiovascular system, we investigated whether the ENT1-null mouse heart was cardioprotected in response to ischemia ...
Mechanistically, we found that ENT1-mediated adenosine transport is critical for cyclic adenosine monophosphate homeostasis and the regulation of erythroid transcription factors.
Finally, we review data from recent attempts to heterologously express and purify human ENT1 for structural studies and discuss recent discoveries of new isoform-selective potent small-molecule ENT inhibitors, including new natural product-inspired compounds.19
ENT1 The type 1 equilibrative nucleoside transporter (ENT1) gene is also known as solute carrier family 29 (equilibrative nucleoside transporter), member 1 (SLC29A1) and is located at 6p21.1. 91 The ENT1 that regulates adenosine levels is known to regulate ethanol sensitivity and preference. Analyses of the combined data set in subjects of European ancestry, recruited from two independent ...
The human equilibrative nucleoside transporter 1 (hENT1) is an effective controller of adenosine signaling by regulating its extracellular and intracellular concentration, and has become a solid drug target of clinical used adenosine reuptake ...
Background and Objectives Equilibrative nucleoside transporter (ENT) 1 is a widely-expressed drug transporter, handling nucleoside analogues as well as endogenous nucleosides. ENT1 has been postulated to be inhibited by some marketed tyrosine kinase inhibitors (TKIs). To obtain insights into this point, the interactions of 24 TKIs with ENT1 activity have been analyzed. Methods Inhibition of ...
Epilepsy is associated with adenosine dysregulation, and equilibrative nucleoside transporters-1 (ENT-1) functions as a regulator of extracellular adenosine....
Jan 15, 2025
ENT1 is a widely expressed transporter, mainly found at the plasma membrane, being considered the main regulator of homeostatic maintenance of adenosine levels (Bone, Robillard, Stolk, & Hammond, 2007).
ENT1 inhibition, therefore, augments anti-cancer immune responses through the restoration of pyrimidine nucleotide synthesis in T cells suppressed by adenosine.
A specific role for ENT1 in human erythropoiesis was demonstrated by a defective erythropoiesis of human CD34 + progenitors following short hairpin RNA-mediated knockdown of ENT1. Furthermore, genetic deletion of ENT1 in mice was associated with reduced erythroid progenitors in the bone marrow, anemia, and macrocytosis.
In regard to our ENT1 model, there are no significant compensatory changes noted in gene expression of nucleoside transporter or metabolism after genetic deletion of murine ENT1. 34, 35 Likewise, previous studies have indicated that genetic deficiency of OATP1B2 is not associated with any pronounced compensatory alterations in metabolic enzyme ...
The human equilibrative nucleoside transporter 1 (hENT1), a member of the SLC29 family, plays crucial roles in adenosine signaling, cellular uptake of nucleoside for DNA and RNA synthesis, and nucleoside-derived anticancer and antiviral drug transport in humans. Because of its central role in adenos …
Here, we systematically compared the nucleoside selectivity of Plasmodium ENT1 orthologs from P. falciparum (PfENT1), Plasmodium berghei (PbENT1), and Plasmodium vivax (PvENT1), revealing that Plasmodium ENT1 orthologs present a distinct nucleoside recognition pattern.
Mechanistic studies showed that this effect is independent of BTK and instead results from inhibition of equilibrative nucleoside transporter 1 (ENT1) by CNX-774. We show that ENT1 mediates BQ resistance by taking up extracellular uridine, which is salvaged to generate pyrimidine nucleotides in a DHODH-independent manner.
The final dilazep-bound human ENT1 structure is of excellent quality with a Free-R factor of 24%. We also crystallized hENT1 cryst in complex with the nucleoside-derived AdoRI NBMPR, which exhibits merohedral twinning.
ENT1-dependent uptake was calculated as the difference between total transport (ENT1+ENT2) and transport in the presence of 1 µM NBMPR (ENT2). To rule out efflux of the labelled uridine during washes, we performed as a control an assay on a 200µl layer of 84% silicone 16% mineral oil.
Particular uptake rates mediated by ENT1 or ENT2 were assigned to transport activities that were inhibited by 1 µM NBTI or 2 mM hypoxanthine, respectively [32]. Total nucleoside uptake in cells mediated by concentrative and equilibrative systems was also measured using a transport buffer containing sodium chloride.
In this issue of Blood, Mikdar et al show that deficiency of ENT1, a nucleoside transporter, leads to defects in erythropoiesis and morphological changes i
Pancreatic Adenocarcinomas (PACs) are highly aggressive neoplasms. To date, surgery remains the most effective treatment. Adjuvant Gemcitabine is commonly is used as a chemotherapeutic for resected PAC patients. Previous studies demonstrate that Gemcitabine is incorporated into cancer cells via the Equilibrative Nucleoside Transporter 1 (ENT1). Hence, ENT1 expression has been proposed as a ...
Previous studies implicate extracellular adenosine signaling in attenuating myocardial ischemia and reperfusion injury (IRI). This extracellular adenosine signaling is terminated by its uptake into cells by equilibrative nucleoside transporters ...
Members of the Equilibrative Nucleoside Transporter (ENT) Family (TC# 2.A.57) are transport proteins that are specific to nucleosides and nucleobases, and are part of the major facilitator superfamily. They generally possess at least 6, typically 10, transmembrane segments (TMSs) and are 300-600 amino acyl residues in length.
The human equilibrative nucleoside transporter 1 (hENT1) is an effective controller of adenosine signaling by regulating its extracellular and intracellular concentration, and has become a solid drug target of clinical used adenosine reuptake inhibitors (AdoRIs). Currently, the mechanisms of adenosi …
Previous studies implicate extracellular adenosine signaling in attenuating myocardial ischemia and reperfusion injury (IRI). This extracellular adenosine signaling is terminated by its uptake into cells by equilibrative nucleoside transporters (ENTs). Thus, we hypothesized that targeting ENTs would …
Both transporter families are involved in cellular uptake of nucleoside drugs (Fig. 3 A), and human ENT1, and to a lesser extent ENT2, are pharmacologic targets for high-affinity NT inhibitors (Fig. 3 B). Table 1. SLC28 and SLC29 - the cation-coupled and equilibrative nucleoside transporter families.
Oct 25, 2024
ENT1 (equilibrative nucleoside transporter 1; also known as SLC29A1) is a ubiquitous protein located at the cell membrane and is a major transporter responsible for the cellular uptake and release of endogenous nucleosides such as adenosine, and nucleoside analogs used in chemotherapy.
About ENT1 Inhibition ENT1 inhibitors block the activity of the ENT1 transporter. By doing so, they prevent the uptake of adenosine into cells, leading to an increase in the extracellular concentration of adenosine.
Equilibrative nucleoside transporters (ENTs) 1 and 2 facilitate nucleoside transport across the blood-testis barrier (BTB). Improving drug entry into the testes with drugs that use endogenous transport pathways may lead to more effective treatments for diseases within the reproductive tract. In this …
Oncolytic herpes simplex virus-1 (oHSV) vectors selectively replicate in tumor cells where they kill through oncolysis, while sparing normal cells. One of the drawbacks of oHSV vectors is their limited replication and spread to neighboring cancer ...
equilibrative nucleoside transporter 1 (ENT1), the prototypic member of the SLC29 family of transporters, is an integral membrane protein responsible for transporting nucleosides and nucleoside analog drugs across cellular membranes (34, 66). There are four members of the SLC29 family and two isoforms, ENT1 and ENT2.
ENT1 is expressed ubiquitously in mammalian tissues and responsible for a significant portion of nucleoside analog drug uptake in humans. Despite the important clinical role of ENT1, many aspects of the regulation of this protein remain unknown. A major outstanding question in this field is the whether ENT1 is phosphorylated directly.
Our data unambiguously add ENT1 to the list of drug transporters inhibited by TKIs, especially by lorlatinib. This point likely merits attention in terms of possible drug-drug interactions, notably for nucleoside analogues, whose ENT1-mediated uptake into their target cells may be hampered by co-adm …
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