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Related Experiment Videos

Antimitotic peptides and depsipeptides.

Ernest Hamel1, David G Covell

  • 1National Cancer Institute at Frederick, National Institutes of Health, Frederick, Maryland 21702, USA. hamele@mail.nih.gov

Current Medicinal Chemistry. Anti-Cancer Agents
|April 8, 2003
PubMed
Summary
This summary is machine-generated.

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Numerous natural peptides and depsipeptides target tubulin, disrupting microtubule assembly and cell division. These compounds show potential as cytotoxic agents by inhibiting mitosis and inducing tubulin polymerization defects.

Area of Science:

  • Cell Biology
  • Biochemistry
  • Pharmacology

Background:

  • Tubulin is a key protein in cellular microtubules, essential for cell shape and the mitotic spindle.
  • An increasing number of peptides and depsipeptides from various organisms target tubulin.
  • These compounds often exhibit high toxicity to mammalian cells due to microtubule disruption.

Purpose of the Study:

  • To provide a comprehensive overview of tubulin-targeting peptides and depsipeptides.
  • To review their cellular, biochemical, in vivo, and structure-activity relationship (SAR) aspects.
  • To summarize computational modeling efforts for pharmacophore identification.

Main Methods:

  • Literature review of cellular and biochemical studies.
  • Analysis of in vivo data and SAR.

Related Experiment Videos

  • Summary of computer modeling approaches.

    • Main Results:

    • Compounds inhibit tubulin polymerization and suppress microtubule dynamics.
    • They interfere with nucleotide binding and hydrolysis at the GTP site on beta-tubulin.
    • Aberrant tubulin oligomers, including rings, are induced, with morphology varying by compound.

    Conclusions:

    • Tubulin-targeting peptides and depsipeptides represent a significant class of cytotoxic agents.
    • Their diverse mechanisms involve disruption of microtubule assembly and dynamics.
    • Further research, including computational modeling, is needed to understand their pharmacophore and therapeutic potential.