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Updated: Jun 4, 2026

Transmitochondrial Cybrid Generation Using Cancer Cell Lines
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Transmitochondrial Cybrid Generation Using Cancer Cell Lines

Published on: March 17, 2023

Mitochondria-Damaging Self-Reporting Probe for Cancer Therapy.

Hai Xu1, Yura Lee2, Sanghee Yoon3

  • 1Department of Chemistry and Nanoscience, Ewha Womans University, Seoul, Republic of Korea.

Angewandte Chemie (International Ed. in English)
|June 3, 2026
PubMed
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This summary is machine-generated.

New self-reporting cancer drugs (DPPs) monitor their own mitochondrial action, avoiding unreliable probes. This allows precise tracking of drug effects for improved cancer therapy and diagnosis.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • Chemotherapy often damages mitochondria, disrupting mitochondrial membrane potential (ΔΨm), a key factor in drug efficacy.
  • Current methods using fluorescent probes to assess ΔΨm-targeting drugs are unreliable, leading to inaccurate conclusions and hindering drug development.

Purpose of the Study:

  • To develop a novel class of self-reporting chemotherapeutic agents (DPPs) for direct, non-invasive monitoring of mitochondrial drug action.
  • To evaluate the efficacy and safety of DPPs in preclinical cancer models.

Main Methods:

  • Synthesized and characterized a series of cationic chemotherapeutic small molecules (DPPs) with intrinsic fluorescence.
  • Assessed the ability of DPPs to disrupt mitochondrial function, induce reactive oxygen species (ROS), and trigger apoptosis.
Keywords:
cancer therapyfluorescence imagingmitochondriaself‐reporting probe

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  • Investigated the mitochondrial-to-nuclear translocation of DPPs in real-time.
  • Evaluated tumor growth inhibition and systemic toxicity in vivo.
  • Main Results:

    • DPPs exhibit intrinsic fluorescence, enabling self-reporting of their action without external probes.
    • DPP-1 and DPP-2 disrupt mitochondrial function, increase ROS generation, and induce selective apoptosis.
    • Concentration-dependent mitochondrial-to-nuclear translocation of DPPs allows real-time visualization of therapeutic progression.
    • In vivo studies demonstrated potent tumor growth inhibition with negligible systemic toxicity.

    Conclusions:

    • DPPs offer a reliable platform for monitoring mitochondria-targeted chemotherapy, overcoming limitations of current fluorescent probes.
    • The self-reporting capability of DPPs facilitates real-time assessment of drug efficacy at the subcellular level.
    • This mitochondria-targeted chemotherapeutic strategy holds promise for integrated cancer diagnosis and precision therapy.