Functional and molecular characteristics of Na(+)-dependent nucleoside transporters.

Abstract:

:Nucleoside transporters play a critical role in the absorption, disposition, and targeting of therapeutically used nucleosides and nucleoside analogs. This review is focused on the Na(+)-dependent, concentrative nucleoside transporters which are found in a variety of cells including renal, intestinal and hepatic epithelia. Five major Na(+)-dependent nucleoside transporter subtypes have been characterized in isolated tissue preparations: N1 is purine selective; N2 is pyrimidine selective and N3-N5 exhibit variable selectively for both purine and pyrimidine nucleosides. The recent cloning of N1 and N2 nucleoside transporters has provided the first information on the molecular function and structure of concentrative nucleoside transporters. In this manuscript we review the characteristics of the various subtypes of nucleoside transporters and the molecular structure, functional properties, and tissue distribution of the cloned Na(+)-dependent nucleoside transporters. In addition, the interactions of nucleosides and nucleoside analogs with the cloned transporters in mammalian and amphibian expression systems are presented. Mammalian expression systems may be particularly useful during drug development in screening potential compounds for improved bioavailability and tissue specific targeting. Finally, we present our view of future ares of study in the field of nucleoside transporters.

journal_name

Pharm Res

journal_title

Pharmaceutical research

authors

Wang J,Schaner ME,Thomassen S,Su SF,Piquette-Miller M,Giacomini KM

doi

10.1023/a:1012113931332

subject

Has Abstract

pub_date

1997-11-01 00:00:00

pages

1524-32

issue

11

eissn

0724-8741

issn

1573-904X

journal_volume

14

pub_type

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