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Related Concept Videos

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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Microtubules are dynamic structures that undergo cycles of catastrophe and rescue. The microtubules play a central role in cell division by forming the spindle apparatus for segregating the chromosomes. This makes them ideal targets for regulating dividing cells in tumors and malignant cancer cells. Microtubule stabilizing drugs help stabilize the microtubule formation and promote its polymerization. Paclitaxel was the first microtubule stabilizing agent used as anticancer drug in chemotherapy...
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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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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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Related Experiment Video

Updated: Mar 30, 2026

Transfer of Manipulated Tumor-associated Neutrophils into Tumor-Bearing Mice to Study their Angiogenic Potential In Vivo
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Novel antiproliferative antitumor agents.

Mary M Mader1

  • 1Eli Lilly & Co, Lilly Research Laboratories, Discovery Chemistry Research and Technologies, Indianapolis, IN 46285, USA. mader_mary@lilly.com

Current Opinion in Drug Discovery & Development
|September 15, 2005
PubMed
Summary

Identifying small molecules with antitumor activity is crucial for cancer drug development. Some potent anticancer drugs are advanced even when their mechanism of action remains unknown.

Area of Science:

  • Oncology
  • Medicinal Chemistry
  • Drug Discovery

Background:

  • Small molecules with potent and selective antitumor activity are continually identified through cellular screening.
  • Progression of these molecules into clinical development sometimes occurs even when their precise mechanism of action is not fully understood.
  • Examples of such compounds with unknown mechanisms include LY-573636, CHS-828, and SPC-595.

Purpose of the Study:

  • To highlight the ongoing identification and development of small molecule antitumor agents.
  • To discuss the challenges and facilitators in advancing compounds with unknown mechanisms of action.
  • To compare the development paradigm of these compounds with traditional targeted therapies.

Main Methods:

  • Utilizing cellular assays for screening and identification of potent antitumor small molecules.

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  • Clinical development progression of selected compounds.
  • Analysis of structure-activity relationships (SAR) in early discovery phases.

    • Main Results:

    • Several small molecules with significant antitumor potential have been identified and entered clinical trials.
    • The mechanism of action for some of these promising compounds remains unknown during early development stages.
    • Solubility and cell permeability are key factors for demonstrating activity, aiding early SAR elucidation.

    Conclusions:

    • The discovery and development of small molecule anticancer drugs continue, with some progressing despite unknown mechanisms.
    • Early-stage SAR studies are facilitated by basic compound properties like solubility and permeability.
    • Optimizing pharmacokinetic properties, toxicity, and clinical efficacy remain critical challenges, similar to targeted therapy development.