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A therapeutic keypad lock decoded in drug resistant cancer cells

Gulsen Turkoglu1,2, Gozde Kayadibi Koygun3, Mediha Nur Zafer Yurt2

  • 1Department of Molecular Biology and Genetics, Konya Food and Agriculture University Meram Konya Turkey sundus.erbascakmak@gidatarim.edu.tr.

Chemical Science
|August 5, 2021
PubMed

Insights

Researchers developed a molecular keypad lock that selectively kills paclitaxel-resistant breast cancer cells. This novel system uses glutathione, esterase, and light sequentially to activate a photodynamic response, demonstrating a new approach for targeted cancer therapy.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Cancer Research

Background:

  • Drug resistance in cancer, particularly in MCF7 breast cancer cells, poses a significant therapeutic challenge.
  • Tumor markers like glutathione (GSH) and esterase are often overexpressed in resistant cancer cells.
  • Photodynamic therapy (PDT) offers a targeted approach to cancer treatment but requires effective activators.

Purpose of the Study:

  • To design and fabricate a novel molecular keypad lock system for targeted cancer therapy.
  • To investigate the sequential activation mechanism of the molecular keypad lock using specific biological inputs.
  • To evaluate the efficacy of the activated system in selectively killing drug-resistant MCF7 cancer cells.

Main Methods:

  • Fabrication of a molecular keypad lock sensitive to sequential stimuli.
  • Utilizing glutathione (GSH) and esterase as the first two sequential inputs to trigger molecular changes.
  • Exposure to light as the final input to induce a photodynamic response and generate cytotoxic singlet oxygen.
  • Testing the system's efficacy on paclitaxel-resistant MCF7 cancer cells.

Main Results:

  • The molecular keypad lock demonstrated sequential activation upon exposure to GSH, esterase, and light in the correct order.
  • GSH exposure caused a shift in the agent's absorption wavelength.
  • Esterase cleavage further activated the agent by removing a quencher.
  • The activated agent, upon light exposure, produced singlet oxygen, leading to selective cell death in paclitaxel-resistant MCF7 cells.

Conclusions:

  • A novel molecular keypad lock system has been successfully developed for biological applications.
  • The system enables selective activation and targeted cell killing in drug-resistant cancer cells.
  • This work represents the first biological application of small molecular keypad locks, opening new avenues in targeted therapy.

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