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Updated: Mar 9, 2026

Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors
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ABCG2/BCRP: Specific and Nonspecific Modulators

Diana Peña-Solórzano1, Simone Alexandra Stark2, Burkhard König2

  • 1Grupo de Investigación en Macromoléculas, Departamento de Química, Universidad Nacional de Colombia-Sede Bogotá, 5997, Bogotá, Colombia.

Medicinal Research Reviews
|December 23, 2016
PubMed

Insights

Multidrug resistance (MDR) in cancer is a major hurdle in chemotherapy. This review focuses on ABCG2 modulators, aiming to overcome resistance and improve cancer treatment success.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Multidrug resistance (MDR) in cancer cells impedes chemotherapy efficacy, leading to poor clinical outcomes.
  • MDR involves increased drug efflux mediated by ATP-binding cassette (ABC) transporters, notably ABCG2.
  • ABCG2 overexpression is observed in various human cancers, making it a critical target for overcoming resistance.

Purpose of the Study:

  • To review and highlight specific and nonspecific modulators of the ABCG2 transporter.
  • To discuss the selectivity of ABCG2 modulators against various ABC transport proteins.
  • To emphasize the challenge in designing effective ABCG2 inhibitors for clinical application.

Main Methods:

  • Literature review of studies reporting modulators of ABCG2.
  • Analysis of compound selectivity and effectiveness against ABC transport proteins.
  • Synthesis of information on known ABCG2 modulators and their properties.

Main Results:

  • A growing list of ABCG2 modulators has been identified.
  • Many modulators exhibit activity against multiple ABC transport proteins.
  • Limited understanding of the clinical impact of ABCG2 modulation exists.

Conclusions:

  • Developing potent, non-toxic ABCG2 inhibitors is crucial for reversing MDR.
  • Further research is needed to understand the clinical consequences of ABCG2 modulation.
  • Targeting ABCG2 offers a promising strategy to enhance cancer chemotherapy success.
Keywords:
ABC inhibitorABC modulatorABC transporterABCG2/BCRPmultidrug resistance

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