Background: Nucleoside/nucleobase transporters have been investigated since the 1960s. In particular, equilibrative nucleoside transporters were thought to be valuable drug targets, since they are involved in various kinds of viral and parasitic diseases as well as cancers.
Discussion: In the postgenomic era multiple transporters, including different subtypes, have been cloned and characterized on the molecular level. In this article we summarize recent advances regarding structure, function and localization of nucleoside/nucleobase transporters as well as the pharmacological profile of selected drugs.
Conclusion: Knowledge of the different kinetic properties and structural features of nucleoside transporters can either be used for the rational design of therapeutics directly targeting the transporter itself or for the delivery of drugs using the transporter as a port of entry into the target cell. Equilibrative nucleoside transporters are of considerable pharmacological interest as drug targets for the development of drugs tailored to each patient's need for the treatment of cardiac disease, cancer and viral infections.