ArticleThe Journal of pharmacology and experimental therapeutics2013
Basolateral uptake of nucleosides by Sertoli cells is mediated primarily by equilibrative nucleoside transporter 1.
Article in The Journal of pharmacology and experimental therapeutics, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers.
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Who cites it
26 citing papers in PubMed, 33 citations in OpenAlex.
- Testicular immunity.Molecular aspects of medicine · 2024Review
- Blood-testis barrier: a review on regulators in maintaining cell junction integrity between Sertoli cells.Cell and tissue research · 2024Review
- Addressing the Clinical Importance of Equilibrative Nucleoside Transporters in Drug Discovery and Development.Clinical pharmacology and therapeutics · 2023Review
- In Vitro and In Vivo Models for Drug Transport Across the Blood-Testis Barrier.Drug metabolism and disposition: the biological fate of chemicals · 2023Review
- Drug Transporters at the Human Blood-Testis Barrier.Drug metabolism and disposition: the biological fate of chemicals · 2023Review
- Localization of Xenobiotic Transporters Expressed at the Human Blood-Testis Barrier.Drug metabolism and disposition: the biological fate of chemicals · 2022Article
- Drug transport across the blood-testis barrier.American journal of translational research · 2022Review
- Mutation inFrontiers in cell and developmental biology · 2022Article
- Remdesivir and EIDD-1931 Interact with Human Equilibrative Nucleoside Transporters 1 and 2: Implications for Reaching SARS-CoV-2 Viral Sanctuary Sites.Molecular pharmacology · 2021Article
- Testicular disposition of clofarabine in rats is dependent on equilibrative nucleoside transporters.Pharmacology research & perspectives · 2021Article
- Multiple Computational Approaches for Predicting Drug Interactions with Human Equilibrative Nucleoside Transporter 1.Drug metabolism and disposition: the biological fate of chemicals · 2021Article
- Implications of Species Differences in Function and Localization of Transporters at the Blood-Testis Barrier.Toxicological sciences : an official journal of the Society of Toxicology · 2021Article
- Predicting Drug Interactions with Human Equilibrative Nucleoside Transporters 1 and 2 Using Functional Knockout Cell Lines and Bayesian Modeling.Molecular pharmacology · 2021Article
- Generation of a hTERT-Immortalized Human Sertoli Cell Model to Study Transporter Dynamics at the Blood-Testis Barrier.Pharmaceutics · 2020Article
- Nucleoside Reverse Transcriptase Inhibitor Interaction with Human Equilibrative Nucleoside Transporters 1 and 2.Drug metabolism and disposition: the biological fate of chemicals · 2020Article
- Population Modeling Highlights Drug Disposition Differences Between Tenofovir Alafenamide and Tenofovir Disoproxil Fumarate in the Blood and Semen.Clinical pharmacology and therapeutics · 2019Article
- Differential extracellular, but similar intracellular, disposition of two tenofovir formulations in the male genital tract.Antiviral therapy · 2019Article
- Transepithelial transport across the blood-testis barrier.Reproduction (Cambridge, England) · 2018Review
- mRNA Expression and Activity of Nucleoside Transporters in Human Hepatoma HepaRG Cells.Pharmaceutics · 2018Article
- Antiretroviral Therapy and Alcohol Interactions: X-raying Testicular and Seminal Parameters Under the HAART Era.European journal of drug metabolism and pharmacokinetics · 2018Review
Corrections and comments
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
Abstract
The blood-testis barrier (BTB) prevents the entry of many xenobiotic compounds into seminiferous tubules thereby protecting developing germ cells. Understanding drug transport across the BTB may improve drug delivery into the testis. Members of one class of drug, nucleoside reverse transcriptase inhibitors (NRTIs), do penetrate the BTB, presumably through interaction with physiologic nucleoside transporters. By investigating the mechanism of nucleoside transport, it may be possible to design other drugs to bypass the BTB in a similar manner. We present a novel ex vivo technique to study transport at the BTB that employs isolated, intact seminiferous tubules. Using this system, we found that over 80% of total uptake by seminiferous tubules of the model nucleoside uridine could be inhibited by 100 nM nitrobenzylmercaptopurine riboside (NBMPR, 6-S-[(4-nitrophenyl)methyl]-6-thioinosine), a concentration that selectively inhibits equilibrative nucleoside transporter 1 (ENT1) activity. In primary cultured rat Sertoli cells, 100 nM NBMPR inhibited all transepithelial transport and basolateral uptake of uridine. Immunohistochemical staining showed ENT1 to be located on the basolateral membrane of human and rat Sertoli cells, whereas ENT2 was located on the apical membrane of Sertoli cells. Transepithelial transport of uridine by rat Sertoli cells was partially inhibited by the NRTIs zidovudine, didanosine, and tenofovir disoproxil fumarate, consistent with an interaction between these drugs and ENT transporters. These data indicate that ENT1 is the primary route for basolateral nucleoside uptake into Sertoli cells and a possible mechanism for nucleosides and nucleoside-based drugs to undergo transepithelial transport.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.