Nucleoside transporters are integral membrane proteins which facilitate the entry into cells of naturally occurring nucleosides essential for nucleic acid synthesis and nucleoside analog drugs which are widely used in anti-cancer, anti-viral and anti-parasitic treatments. Nucleoside analog drugs have been in use for many decades and are highly effective, but side effects and drug resistance continue to be clinical challenges. We have a long-standing interest in the structure, function and regulation of nucleoside transporters and, more recently, have begun to investigate novel combination approaches which combine nucleoside analog drug and targeted ultrasound microbubble treatment as an improved therapeutic modality.