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Related Concept Videos

Destabilization of Microtubules01:45

Destabilization of Microtubules

The destabilization of microtubules can occur during different stages of the microtubule lifecycle, such as nucleation or elongation. It can take place at either end of the microtubule or in the microtubule lattices as a whole. The lifespan of individual microtubules within a cell varies according to the cell type and stage of the cell cycle. During interphase, the lifespan of the microtubule is about 30 minutes, while during cell division, it is about 15 minutes. In axonal microtubules of...
Drugs that Destabilize Microtubules01:10

Drugs that Destabilize Microtubules

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...
Microtubule Instability02:17

Microtubule Instability

Microtubules are hollow cylindrical filaments having a diameter of approximately 25 nm and a length that varies from 200 nm to 25 μm. GTP-bound tubulin subunits form αβ-heterodimers for microtubule assembly. These core building blocks interact longitudinally, polymerizing into protofilaments. The protofilaments then interact with one another through lateral bonding forces to form stable cylindrical microtubules. These cylindrical filaments are dynamic as they undergo repeated assembly and...
Microtubule Instability02:17

Microtubule Instability

Microtubules are hollow cylindrical filaments having a diameter of approximately 25 nm and a length that varies from 200 nm to 25 μm. GTP-bound tubulin subunits form αβ-heterodimers for microtubule assembly. These core building blocks interact longitudinally, polymerizing into protofilaments. The protofilaments then interact with one another through lateral bonding forces to form stable cylindrical microtubules. These cylindrical filaments are dynamic as they undergo repeated assembly and...
Drugs that Stabilize Microtubules01:15

Drugs that Stabilize Microtubules

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...
Microtubule Associated Proteins (MAPs)01:42

Microtubule Associated Proteins (MAPs)

Microtubule function and architecture are regulated by an array of specialized proteins called microtubule-associated proteins or MAPs. These proteins are widespread across different organisms and have conserved protein motifs, like the multi-TOG domain for tubulin binding found in the CLASP family of MAPs. Some MAPs are lineage-specific based on their conserved domains. Their functions depend upon the cytoskeletal architecture and cell type they are located within. In-plant cells, a specific...

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Spatiotemporal Subcellular Manipulation of the Microtubule Cytoskeleton in the Living Preimplantation Mouse Embryo using Photostatins
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Chimeric microtubule disruptors.

Mathew P Leese1, Fabrice Jourdan, Meriel R Kimberley

  • 1Medicinal Chemistry & Sterix Ltd., Department of Pharmacy & Pharmacology, University of Bath, Claverton Down, Bath, BA2 7AY, UK.

Chemical Communications (Cambridge, England)
|April 14, 2010
PubMed
Summary

Researchers developed novel microtubule disruptors using a chimeric approach, achieving high in vitro activity and oral bioavailability. Carbonic anhydrase interaction enhances drug delivery, showing significant therapeutic potential in preclinical cancer models.

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Area of Science:

  • Medicinal Chemistry
  • Pharmacology
  • Structural Biology

Background:

  • Microtubule disruptors are crucial in cancer therapy.
  • Achieving both high efficacy and oral bioavailability remains a challenge.

Purpose of the Study:

  • To discover novel microtubule disruptors with improved in vitro activity and oral bioavailability.
  • To elucidate the mechanism of bioavailability enhancement through ligand-protein interactions.

Main Methods:

  • Chimeric drug design approach.
  • In vitro activity assays.
  • Protein X-ray crystallography to characterize ligand-protein interactions.
  • Tumor xenograft models for in vivo efficacy studies.

Main Results:

  • Identified chimeric compounds with potent in vitro microtubule-disrupting activity.
  • Characterized a key interaction with carbonic anhydrase that significantly enhances oral bioavailability.
  • Demonstrated excellent therapeutic potential in a preclinical tumor xenograft model.

Conclusions:

  • The chimeric approach is effective for developing orally bioavailable microtubule disruptors.
  • Targeting carbonic anhydrase offers a viable strategy to improve drug bioavailability.
  • This class of compounds holds significant promise for cancer treatment.