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Electron Transport Chain: Complex I and II01:46

Electron Transport Chain: Complex I and II

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The mitochondrial electron transport chain (ETC) is the main energy generation system in the eukaryotic cells. However, mitochondria also produce cytotoxic reactive oxygen species (ROS) due to the large electron flow during oxidative phosphorylation. While Complex I is one of the primary sources of superoxide radicals, ROS production by Complex II is uncommon and may only be observed in cancer cells with mutated complexes.
ROS generation is regulated and maintained at moderate levels necessary...
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Targeted Cancer Therapies02:57

Targeted Cancer Therapies

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The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against...
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Combination Therapies and Personalized Medicine02:50

Combination Therapies and Personalized Medicine

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Combining two or more treatment methods increases the life span of cancer patients while reducing damage to vital organs or tissue from the overuse of a single treatment. Combination therapy also targets different cancer-inducing pathways, thus reducing the chances of developing resistance to treatment.
The combination of the drug acetazolamide and sulforaphane is a good example of combination therapy to treat cancer. The cells in the interior of a large tumor often die due to the hypoxic and...
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The Electron Transport Chain01:30

The Electron Transport Chain

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The electron transport chain or oxidative phosphorylation is an exothermic process in which free energy released during electron transfer reactions is coupled to ATP synthesis. This process is a significant source of energy in aerobic cells, and therefore inhibitors of the electron transport chain can be detrimental to the cell's metabolic processes.
Inhibitors of the electron transport chain
Rotenone, a widely used pesticide, prevents electron transfer from Fe-S cluster to ubiquinone or Q...
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Mitochondrial Membranes01:45

Mitochondrial Membranes

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A single mitochondrion is a bean-shaped organelle enclosed by a double-membrane system. The outer membrane of mitochondria is smooth and contains many porins - the integral membrane transporters. Porins enable free diffusion of ions and small uncharged molecules through the outer mitochondrial membrane but limit the transport of molecules larger than 5000 Daltons. Further, the outer mitochondrial membrane forms a unique structure called membrane contact sites with other subcellular organelles,...
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Treatment Resistant Cancers02:56

Treatment Resistant Cancers

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Cancer is the second leading cause of death in the United States. A cancer cell is genetically unstable and hence can mutate faster. They can also modify their microenvironment and escape immune surveillance. The difficulties in treating cancer are further compounded by the emergence of rapid resistance to anticancer drugs. The most common ways to attain resistance in cancer cells include alteration in drug transport and metabolism, modification of drug target, elevated DNA damage response, or...
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Related Experiment Video

Updated: Mar 9, 2026

Experimental Protocol for Detecting Mitochondrial Function in Hepatocytes Exposed to Organochlorine Pesticides
08:39

Experimental Protocol for Detecting Mitochondrial Function in Hepatocytes Exposed to Organochlorine Pesticides

Published on: September 16, 2020

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Targeted combinational therapy inducing mitochondrial dysfunction.

Weon Sup Shin1, Soon Ki Park2, Peter Verwilst1

  • 1Department of Chemistry, Korea University, Seoul 02841, Korea. jongskim@korea.ac.kr.

Chemical Communications (Cambridge, England)
|January 10, 2017
PubMed
Summary
This summary is machine-generated.

We developed a novel theranostic agent that targets cancer cell mitochondria. Upon activation by glutathione, it releases a chemotherapy drug and emits fluorescence, inducing cancer cell death.

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Related Experiment Videos

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Experimental Protocol for Detecting Mitochondrial Function in Hepatocytes Exposed to Organochlorine Pesticides
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An In Vitro Approach to Study Mitochondrial Dysfunction: A Cybrid Model
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An In Vitro Approach to Study Mitochondrial Dysfunction: A Cybrid Model

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Area of Science:

  • Biomedical Engineering
  • Materials Science
  • Pharmacology

Background:

  • Mitochondria play a crucial role in cancer cell survival and apoptosis.
  • Targeted drug delivery systems can enhance therapeutic efficacy and reduce side effects.
  • Aggregation-induced emission (AIE) probes offer unique fluorescence properties for bioimaging.

Purpose of the Study:

  • To design and synthesize a mitochondria-specific combinational theranostic agent.
  • To investigate the intracellular triggered release of a chemotherapeutic agent.
  • To evaluate the theranostic potential of the agent for cancer therapy.

Main Methods:

  • Synthesis of a novel theranostic agent (compound 1) incorporating a chlorambucil prodrug, AIE dye, thiol-responsive moiety, and mitochondria-targeting unit.
  • In vitro studies to assess glutathione (GSH)-induced prodrug activation and chlorambucil release.
  • Mitochondrial targeting and AIE fluorescence imaging in cancer cells.
  • Evaluation of apoptosis induction via the caspase pathway.

Main Results:

  • Compound 1 demonstrated selective accumulation in cancer cell mitochondria.
  • GSH triggered the release of active chlorambucil from the prodrug.
  • Activated compound 1 exhibited mitochondria-targeted AIE fluorescence.
  • The agent induced cancer cell apoptosis through mitochondrial dysfunction and caspase activation.

Conclusions:

  • The developed mitochondria-specific theranostic agent shows promise for targeted cancer therapy.
  • The combination of chemotherapy and AIE imaging offers a theranostic approach for monitoring treatment response.
  • This strategy holds potential for overcoming drug resistance and improving cancer treatment outcomes.