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Author Spotlight: Exploring the Role of FAM83A in Cervical Cancer
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Ovarian cancer cells cisplatin sensitization agents selected by mass cytometry target ABCC2 inhibition

Elisabeta Comsa1,2, Kim-Anh Nguyen3,4, Felicia Loghin2

  • 1Drug Resistance & Membrane Proteins Laboratory, Molecular Microbiology & Structural Biochemistry, UMR 5086 CNRS/Université Lyon 1, Institut de Biologie et Chimie des Protéines, Lyon, France.

Future Medicinal Chemistry
|June 1, 2018
PubMed
Abstract

Insights

Researchers identified novel compounds that overcome cisplatin resistance in ovarian cancer by blocking the ABCC2 pump. These compounds restore cisplatin sensitivity in resistant cells, offering a promising approach for personalized cancer therapy.

Area of Science:

  • Oncology
  • Biochemistry
  • Pharmacology

Background:

  • Cisplatin resistance in ovarian cancer is a significant clinical challenge.
  • ATP-Binding Cassette (ABC) transporters, particularly ABCC2, are implicated in mediating drug resistance by facilitating cisplatin efflux.
  • Targeting these efflux mechanisms is crucial for overcoming treatment failure.

Purpose of the Study:

  • To identify novel inhibitors that specifically block cisplatin efflux mediated by the ABCC2 pump.
  • To evaluate the efficacy of 2-indolylmethylenebenzofuranone derivatives in resensitizing cisplatin-resistant ovarian cancer cells.

Main Methods:

  • Development of an original method using cyTOF (cytometry time-of-flight) mass cytometry for direct platinum quantitation.
  • Testing a library of 2-indolylmethylenebenzofuranone derivatives for their ability to inhibit ABCC2-mediated cisplatin efflux.
  • Assessing the impact of compounds on cellular platinum accumulation and calcein efflux.

Main Results:

  • Several 2-indolylmethylenebenzofuranone derivatives demonstrated potent inhibition of ABCC2-mediated cisplatin efflux.
  • These compounds led to complete platinum accumulation in resistant cells.
  • The identified derivatives effectively resensitized cisplatin-resistant A2780 ovarian cancer cells to cisplatin therapy.
  • Compound efficacy was confirmed while preserving significant calcein efflux activity, indicating specificity.

Conclusions:

  • CyTOF mass cytometry is a powerful tool for quantifying platinum accumulation in cancer cells.
  • Specific ABCC2 inhibitors derived from 2-indolylmethylenebenzofuranones can overcome cisplatin resistance in ovarian cancer.
  • This approach holds potential for improving and personalizing ovarian cancer treatment strategies.
Keywords:
ABCC2 auronescisplatin resistancecyTOF inhibitorsmass cytometrymultidrug resistanceovarian cancer

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