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Related Concept Videos

Inhibition of Cdk Activity02:34

Inhibition of Cdk Activity

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The orderly progression of the cell cycle depends on the activation of Cdk protein by binding to its cyclin partner. However, the cell cycle must be restricted when undergoing abnormal changes. Most cancers correlate to the deregulated cell cycle, and since Cdks are a central component of the cell cycle, Cdk inhibitors are extensively studied to develop anticancer agents. For instance, cyclin D associates with several Cdks, such as Cdk 4/6, to form an active complex. The cyclin D-Cdk4/6 complex...
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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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Drugs that Destabilize Microtubules01:10

Drugs that Destabilize Microtubules

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Microtubules are dynamic structures and can be regulated by microtubule targeting agents (MTAs). Microtubule destabilizing drugs are a class of MTAs that destabilize and prevent microtubules' polymerization. Both natural and synthetic chemicals can be found under this class of drugs. Vincristine and vinblastine, two vinca alkaloids, and colchicine were among the first to be discovered. These drugs can affect cells in various ways, either by inducing a change in cell morphology, preventing...
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Chemotherapy-Induced Nausea and Vomiting: Dopamine Receptor Antagonists01:29

Chemotherapy-Induced Nausea and Vomiting: Dopamine Receptor Antagonists

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Dopamine receptor antagonists, also known as antipsychotic agents, are critical in managing chemotherapy-induced vomiting. These antiemetic agents block dopamine receptors in the chemoreceptor trigger zone (CTZ), inhibiting signal transmission to the vomiting center. Antipsychotic agents encompass phenothiazines (PTZ), butyrophenones, benzamides, and thienobenzodiazepines (Zyprexa), which are utilized for their antiemetic and sedative properties.
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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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Cancer Therapies02:49

Cancer Therapies

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Cancer therapies are various modes of treatment, such as surgery, radiation therapy, and chemotherapy that are administered to cancer patients.
However, cancer treatments can pose several challenges, as therapies used to kill cancer cells are generally also toxic to normal cells. Moreover, cancer cells mutate rapidly and can develop resistance to chemical agents or radiation therapy. Besides, all types of cancer cells may not respond to the same therapy. Some cancer cells respond to one...
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Related Experiment Video

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Potentiation of Anticancer Antibody Efficacy by Antineoplastic Drugs: Detection of Antibody-drug Synergism Using the Combination Index Equation
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Anthracyclines as effective anticancer drugs.

Janos Nadas1, Duxin Sun

  • 1Department of Chemistry, College of Pharmacy, The Ohio Sate University, Columbus, OH 43210, USA;

Expert Opinion on Drug Discovery
|March 20, 2013
PubMed
Summary

Researchers are developing improved anthracyclines to combat cancer drug resistance and cardiotoxicity. Recent advances in medicinal chemistry and structural biology offer new strategies for designing more effective anticancer agents.

Area of Science:

  • Pharmacology and Medicinal Chemistry
  • Structural Biology
  • Oncology

Background:

  • Anthracyclines are vital anticancer drugs, but their efficacy is limited by tumor resistance and cardiotoxicity.
  • A continuous search for novel anthracyclines with improved therapeutic profiles is ongoing.
  • Understanding drug mechanisms and resistance pathways is crucial for developing next-generation therapies.

Purpose of the Study:

  • To review recent advancements in the design and application of anthracyclines.
  • To explore novel strategies for overcoming drug resistance and reducing toxicity.
  • To highlight future research directions for developing superior anthracycline-based cancer treatments.

Main Methods:

  • Analysis of crystal structures and molecular modeling to elucidate topoisomerase poisoning mechanisms.

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  • Investigation of chemical and sugar modifications of anthracyclines.
  • Review of clinical trials and drug delivery advancements.

    • Main Results:

    • Detailed mechanisms of topoisomerase poisoning by novel anthracyclines have been elucidated.
    • Chemical modifications can alter target selectivity and anticancer activity.
    • Sugar modifications show promise in overcoming P-glycoprotein-mediated drug resistance.

    Conclusions:

    • Structural insights and medicinal chemistry modifications are key to designing better anthracyclines.
    • Targeting topoisomerases and overcoming drug resistance mechanisms are critical areas of focus.
    • Further research into structural elucidation, molecular modeling, and drug delivery is essential for clinical translation.