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Updated: Aug 22, 2026

Implementation of In Vitro Drug Resistance Assays: Maximizing the Potential for Uncovering Clinically Relevant Resistance Mechanisms
08:46

Implementation of In Vitro Drug Resistance Assays: Maximizing the Potential for Uncovering Clinically Relevant Resistance Mechanisms

Published on: December 9, 2015

Predicting drug sensitivity and resistance: profiling ABC transporter genes in cancer cells

Gergely Szakács1, Jean-Philippe Annereau, Samir Lababidi

  • 1Laboratory of Cell Biology, Center for Cancer Research, NCI, NIH, Bethesda, MD, 20892, USA. szakacsg@mail.nih.gov

Cancer Cell
|August 25, 2004
PubMed

Insights

Researchers analyzed multidrug resistance (MDR) in cancer by profiling ABC transporters in NCI-60 cell lines. They identified transporters conferring resistance and found compounds potentiated by the MDR1 transporter, offering new therapeutic leads.

Area of Science:

  • Molecular Biology
  • Pharmacology
  • Oncology

Background:

  • Multidrug resistance (MDR) is a significant challenge in cancer chemotherapy.
  • ATP-binding cassette (ABC) transporters play a crucial role in mediating MDR.

Purpose of the Study:

  • To analyze mRNA expression of human ABC transporters in the NCI-60 cancer cell line panel.
  • To correlate transporter expression with drug sensitivity profiles to identify resistance mechanisms.
  • To discover novel drug candidates or strategies to overcome MDR.

Main Methods:

  • Real-time RT-PCR was used to profile mRNA expression of 48 human ABC transporters.
  • The NCI-60 cancer cell line panel was utilized for comprehensive analysis.
  • Growth inhibitory data for 1,429 anticancer drugs were correlated with transporter expression.

Main Results:

  • Specific ABC transporters were identified as conferring resistance to particular anticancer agents.
  • Unexpectedly, some compounds demonstrated potentiated activity mediated by the MDR1 transporter.
  • This suggests a dual role for certain transporters in drug response.

Conclusions:

  • The study provides a detailed map of ABC transporter expression in the NCI-60 cell lines.
  • It identifies key transporters involved in drug resistance and sensitivity.
  • Findings offer potential for developing new therapeutic strategies targeting MDR, including compounds whose efficacy is enhanced by MDR1.

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