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Updated: Jul 16, 2026

Implementation of In Vitro Drug Resistance Assays: Maximizing the Potential for Uncovering Clinically Relevant Resistance Mechanisms
Published on: December 9, 2015
Nucleoside transport and its significance for anticancer drug resistance
J R Mackey1, S A Baldwin, J D Young
1Department of Oncology, University of Alberta, and Cross Cancer Institute, Edmonton, Alberta, Canada.
Abstract:
This article discusses the role of nucleoside transport processes in the cytotoxicity of clinically important anticancer nucleosides. This article summarizes recent advances in the molecular biology of nucleoside transport proteins, review the current state of knowledge of the transportability of therapeutically useful anticancer nucleosides, and provide an overview of the role of nucleoside transport deficiency as a mechanism of resistance to nucleoside cytotoxicity are summarized. Several strategies for utilization of nucleoside transport processes to improve the therapeutic index of anticancer therapies, including the use of nucleoside-transport inhibitors to modulate toxicity of both nucleoside and non-nucleoside antimetabolite drugs are also presented.
Insights
Nucleoside transport is crucial for anticancer drug effectiveness. Understanding these processes can help overcome drug resistance and improve cancer therapies by modulating drug toxicity.
Area of Science:
- Pharmacology
- Molecular Biology
- Cancer Therapeutics
Background:
- Nucleoside analogs are vital anticancer drugs.
- Nucleoside transport significantly influences their efficacy and toxicity.
- Drug resistance can arise from impaired nucleoside transport.
Purpose of the Study:
- To review advances in nucleoside transporter biology.
- To assess the transportability of anticancer nucleosides.
- To explore strategies for improving anticancer therapies via nucleoside transport modulation.
Main Methods:
- Literature review of molecular biology of nucleoside transport proteins.
- Analysis of transportability of clinically used anticancer nucleosides.
- Overview of nucleoside transport deficiency as a resistance mechanism.
Main Results:
- Nucleoside transport is a key determinant of anticancer nucleoside cytotoxicity.
- Deficiency in nucleoside transport can lead to resistance to these drugs.
- Nucleoside transport inhibitors can modulate toxicity of antimetabolites.
Conclusions:
- Targeting nucleoside transport offers a strategy to enhance anticancer therapy.
- Modulating nucleoside transport can improve the therapeutic index of nucleoside-based drugs.
- Further research into nucleoside transporters is essential for optimizing cancer treatment.
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