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Updated: Jun 21, 2026

Biosensor-based High Throughput Biopanning and Bioinformatics Analysis Strategy for the Global Validation of Drug-protein Interactions
08:31

Biosensor-based High Throughput Biopanning and Bioinformatics Analysis Strategy for the Global Validation of Drug-protein Interactions

Published on: December 1, 2020

Evaluation of current methods used to analyze the expression profiles of ATP-binding cassette transporters yields an

Josiah N Orina1, Anna Maria Calcagno, Chung-Pu Wu

  • 1Laboratory of Cell Biology, Center for Cancer Research, National Cancer Institute, NIH, Bethesda, MD 20892-4256, USA.

Molecular Cancer Therapeutics
|July 9, 2009
PubMed

Insights

Multidrug resistance (MDR) in cancer is a major challenge. This study identifies superior methods for analyzing gene expression and improves a database by discovering new substrates for key transporters involved in MDR.

Area of Science:

  • Oncology
  • Pharmacology
  • Molecular Biology

Background:

  • Multidrug resistance (MDR) to chemotherapy is a significant obstacle in cancer treatment.
  • Existing MDR mechanisms are complex, often involving multiple synergistic pathways, leading to resistance against various drugs.
  • Translating in vitro findings on MDR mechanisms to clinical applications remains largely unsuccessful.

Purpose of the Study:

  • To identify genes and mechanisms critical for in vivo MDR development.
  • To establish reliable methods for analyzing highly homologous genes from limited tissue samples.
  • To improve understanding of MDR and develop strategies to circumvent it.

Main Methods:

  • Utilized a pre-existing database for identifying non-ATP-binding cassette (ABC) transporter substrates in early drug discovery.
  • Evaluated current methods for analyzing ABC transporter expression profiles for accuracy and sensitivity.
  • Employed two superior platforms for analyzing expression profiles of highly homologous gene superfamilies.

Main Results:

  • Identified two platforms as superior for analyzing highly homologous gene superfamily expression.
  • Enhanced an existing database by discovering previously unknown substrates for ABCB1, ABCC1, and ABCG2 transporters.
  • These transporters are known contributors to multidrug resistance in cancer.

Conclusions:

  • The developed methods and improved database are crucial for advancing the understanding of in vivo MDR mechanisms.
  • Accurate analysis of gene expression profiles, particularly for highly homologous genes, is fundamental to overcoming MDR.
  • This research paves the way for novel therapeutic strategies targeting MDR in cancer treatment.

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