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Updated: Jul 11, 2026

Screening Ion Channels in Cancer Cells
Published on: June 16, 2023
Drug transporters as targets for cancer chemotherapy
1The Program in Experimental Therapeutics, Marlene and Stewart Greenebaum Cancer Center, School of Medicine, University of Maryland at Baltimore, Baltimore, MD 21201, USA. tnakanishi@som.umaryland.edu
Abstract:
Transporter proteins play an important role in taking up nutrients into and effluxing xenobiotics out of cells to sustain cell survival. Transporters that affect drug absorption, distribution and excretion are the so-called drug transporters. In the last decade, a number of studies revealed interactions between drug transporters and clinically important anticancer agents. Utilizing the knowledge of transporter functions offers us the possibility of delivering a drug to the target tissues, avoiding distribution to other tissues and improving oral bioavailability. Many transporters have been reported to be differentially up-regulated in cancer cells compared to normal tissues, suggesting that the differential expression of transporters in cancer cells may provide good targets for enhancing drug delivery as well as diagnostic markers for cancer therapy. This review will focus on the role of drug transporters in the adaptation and growth of tumors and in their potential usefulness as therapeutic targets in cancer.
Insights
Drug transporters are crucial for cell survival and drug efficacy. Targeting these transporters in cancer cells offers new strategies for improved anticancer drug delivery and diagnostics.
Area of Science:
- Pharmacology and molecular biology
- Cancer biology and therapeutics
Background:
- Transporter proteins regulate nutrient uptake and xenobiotic efflux, essential for cell survival.
- Drug transporters specifically influence the absorption, distribution, metabolism, and excretion of pharmaceuticals.
- Interactions between drug transporters and anticancer agents are increasingly recognized.
Purpose of the Study:
- To review the role of drug transporters in tumor adaptation and growth.
- To explore the potential of drug transporters as therapeutic targets in cancer therapy.
- To highlight how understanding transporter functions can optimize anticancer drug delivery and diagnostics.
Main Methods:
- Literature review of studies on drug transporters and anticancer agents.
- Analysis of differential transporter expression in cancer versus normal tissues.
- Synthesis of information on transporter-mediated drug delivery and diagnostic applications.
Main Results:
- Drug transporters are implicated in the adaptation and growth of tumors.
- Differential up-regulation of transporters in cancer cells suggests potential as therapeutic targets.
- Exploiting transporter functions can enhance drug delivery to target tissues and improve oral bioavailability.
- Transporter expression patterns may serve as diagnostic markers for cancer therapy.
Conclusions:
- Drug transporters are critical players in cancer progression and drug response.
- Targeting drug transporters presents a promising strategy for novel cancer therapies.
- Understanding transporter roles can lead to personalized medicine approaches in oncology.
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