Journal
CURRENT VASCULAR PHARMACOLOGY
Volume 7, Issue 4, Pages 426-434Publisher
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/157016109789043892
Keywords
Nucleoside transport; proteins; pharmacology
Funding
- Fondo de Investigaciones Sanitarias [PI-020934]
- Ministerio de Sanidad y Consumo [BFU2006-07556/BFI]
- Fundacion Ramon Areces to F. Javier Casado
- Ministerio de Educacion y Ciencia [SAF2005-01259, SAF2008-00577]
- FIPSE
- DURSI, Generalitat de Catalunya [2005SGR00315]
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Concentrative nucleoside transporters (CNT; SLC28) and equilibrative nucleoside transporters (ENT; SLC29) mediate the uptake of natural nucleosides and a variety of nucleoside-derived drugs, mostly used in anticancer therapy. SLC28 and SLC29 families consist in three and four members, respectively, which differ in their substrate selectivity and their energy requirements. Tissue distribution of these transporters is not homogeneous among tissues, and their expression can be regulated. In epithelia, CNT and ENT proteins are mostly localized in the apical and basolateral membranes, respectively, which results in nucleoside and nucleoside-derived drugs vectorial flux. Nucleoside transporters can play physiological roles other than salvages, such as the modulation of extracellular and intracellular adenosine concentrations. Moreover, these transporters also have clinical significance. ENT proteins are target of dipyridamole and dilazep, used as vasodilatory drugs in the treatment of heart and vascular diseases. On the other hand, nucleoside transporters are responsible for the cellular uptake of currently used anticancer nucleoside-derived drugs, thus these membrane proteins might play a significant role in nucleoside-based chemotherapy. Finally, several polymorphisms have been described in CNT and ENT proteins that could affect nucleoside homeostasis, adenosine signalling events or nucleoside-derived drug cytotoxicity or pharmacokinetics.
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