Related Experiment Video

Updated: Feb 2, 2026

Synthesis and Characterization of an Aspirin-fumarate Prodrug that Inhibits NFκB Activity and Breast Cancer Stem Cells
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Synthesis and Characterization of an Aspirin-fumarate Prodrug that Inhibits NFκB Activity and Breast Cancer Stem Cells

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Synergistic enzymatic and bioorthogonal reactions for selective prodrug activation in living systems

Qingxin Yao1,2, Feng Lin3,4, Xinyuan Fan4

  • 1CAS Center for Excellence in Nanoscience, CAS Key Laboratory of Biomedical Effects of Nanomaterials and Nanosafety, National Center for Nanoscience and Technology, Beijing, 100190, China.

Nature Communications
|November 30, 2018
PubMed

Insights

This study introduces a new strategy to reduce chemotherapy

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Cancer Therapeutics

Background:

  • Adverse drug reactions (ADRs) limit chemotherapy efficacy by restricting drug dosage.
  • Existing strategies like nano-drugs and prodrugs have limitations in reducing ADRs.
  • A novel approach is needed to mitigate ADRs and improve cancer treatment outcomes.

Purpose of the Study:

  • To develop a new strategy for reducing ADRs in chemotherapy.
  • To achieve spatiotemporally controlled and synergistic prodrug activation.
  • To enhance cancer cell potency while minimizing toxicity to normal cells.

Main Methods:

  • Utilized an enzymatic supramolecular self-assembly process.
  • Accumulated a bioorthogonal decaging reaction trigger within targeted cancer cells.
  • Enabled controlled prodrug activation through enzymatic and bioorthogonal reactions.

Main Results:

  • The bioorthogonally activated prodrug showed significantly enhanced potency against cancer cells.
  • Demonstrated high tumor inhibition efficacy in vivo.
  • Exhibited satisfactory biocompatibility, pharmacokinetics, and safety profiles.

Conclusions:

  • The integration of enzymatic and bioorthogonal reactions offers a promising strategy for ADR reduction.
  • This approach enables targeted and controlled prodrug activation for improved cancer therapy.
  • The developed method holds potential as a general small-molecule-based strategy for chemotherapy ADR alleviation.

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