UNIT 23.6 Assessment of Drug Transporter Function Using Fluorescent Cell Imaging

  1. Kristin M. Bircsak1,
  2. Christopher J. Gibson1,
  3. Robert W. Robey2,
  4. Lauren M. Aleksunes1,3

Published Online: 23 SEP 2013

DOI: 10.1002/0471140856.tx2306s57

Current Protocols in Toxicology

Current Protocols in Toxicology

How to Cite

Bircsak, K. M., Gibson, C. J., Robey, R. W. and Aleksunes, L. M. 2013. Assessment of Drug Transporter Function Using Fluorescent Cell Imaging. Current Protocols in Toxicology. 57:23.6:23.6.1–23.6.15.

Author Information

  1. 1

    Department of Pharmacology and Toxicology, Ernest Mario School of Pharmacy, Rutgers University, Piscataway, New Jersey

  2. 2

    Medical Oncology Branch, National Cancer Institute, National Institutes of Health, Bethesda, Maryland

  3. 3

    Environmental and Occupational Health Sciences Institute, Piscataway, New Jersey

Publication History

  1. Published Online: 23 SEP 2013


ATP-binding cassette (ABC) proteins, including the breast cancer resistance protein (BCRP) and multidrug resistance proteins (MDRs), actively transport structurally diverse chemicals from a number of tissues and are being increasingly cited as mediators of clinically relevant drug-drug interactions. The potential outcomes of concomitantly administering two drugs that interact at the same transporter include altered disposition and toxicity and/or efficacy of one or both of the drugs. Research demonstrating the role of transporters in clinical pharmacokinetics has shed light on the need for in vitro screening methods that detect drug-transporter interactions during preclinical development. This unit describes cell-based procedures for detecting functional inhibitors of BCRP and MDR1 by measuring fluorescent substrate accumulation in suspended cells using an automated cell counter, which offers convenience, sensitivity, and speed in measuring intracellular fluorescence and identifying new inhibitors. An alternative method is provided for making similar measurements using a spectrophotometer with fluorescence detection capabilities. Curr. Protoc. Toxicol. 57:21.12.1-21.12.15. © 2013 by John Wiley & Sons, Inc.


  • ABC transporter;
  • MDR1;
  • BCRP;
  • ABCB1;
  • ABCG2