Fluorescent Nucleoside Derivatives as a Tool for the Detection of Concentrative Nucleoside Transporter Activity Using Confocal Microscopy and Flow Cytometry
| Autor: | María Pilar Lostao, Carlos Sancho-Mateo, Marçal Pastor-Anglada, Dolors Colomer, Anna Grandas, Paula Fernández-Calotti, Ana Claudio-Montero, Itziar Pinilla-Macua |
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| Rok vydání: | 2015 |
| Předmět: |
Microscopy
Confocal medicine.diagnostic_test Pharmaceutical Science Nucleosides Transporter Nucleoside Transport Proteins Biology Flow Cytometry Fluorescence Flow cytometry law.invention Biochemistry In vivo Confocal microscopy law Drug Discovery medicine Fluorescence microscope Humans Molecular Medicine Nucleoside Function (biology) |
| Zdroj: | Molecular Pharmaceutics. 12:2158-2166 |
| ISSN: | 1543-8392 1543-8384 |
| DOI: | 10.1021/acs.molpharmaceut.5b00142 |
| Popis: | The abundance and function of transporter proteins at the plasma membrane are likely to be crucial in drug responsiveness. Functional detection of human concentrative nucleoside transporters (hCNTs) is of interest for predicting drug sensitivity because of their ability to transport most nucleoside-derived drugs. In the present study, two fluorescent nucleoside analogues, uridine-furan and etheno-cytidine, were evaluated as tools to study in vivo nucleoside transporter-related functions. These two molecules showed high affinity interactions with hCNT1 and hCNT3 and were shown to be substrates of both transporters. Both fluorescence microscopy and flow cytometry experiments showed that uridine-furan uptake was better suited for distinguishing cells that express hCNT1 or hCNT3. These data highlight the usefulness of fluorescent nucleoside derivatives, as long as they fulfill the requirements of confocal microscopy and flow cytometry, for in vivo analysis of hCNT-related function. |
| Databáze: | OpenAIRE |
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