This article discusses the role of nucleoside transport processes in t
he cytotoxicity of clinically important anticancer nucleosides. This a
rticle summarizes recent advances in the molecular biology of nucleosi
de transport proteins, review the current state of knowledge of the tr
ansportability of therapeutically useful anticancer nucleosides, and p
rovide an overview of the role of nucleoside transport deficiency as a
mechanism of resistance to nucleoside cytotoxicity are summarized. Se
veral strategies for utilization of nucleoside transport processes to
improve the therapeutic index of anticancer therapies, including the u
se of nucleoside-transport inhibitors to modulate toxicity of both nuc
leoside and nonnucleoside antimetabolite drugs are also presented.