Related Experiment Video
Updated: Jul 19, 2026

Studying TGF-β Signaling and TGF-β-induced Epithelial-to-mesenchymal Transition in Breast Cancer and Normal Cells
Published on: October 27, 2020
Thiazolidinedione anti-cancer activity: Is inhibition of microtubule assembly implicated?
1Department of Pharmaceutics and Medicinal Chemistry, Thomas J. Long School of Pharmacy and Health Sciences, University of the Pacific, 3601 Pacific Avenue, Stockton, CA 95211, USA. wrussu@pacific.edu
Abstract:
An hypothesis is presented which seeks to explain the anti-cancer activity of thiazolidinediones (TZDs), a class of drugs currently used to treat type 2 diabetes mellitus. Empirical data from the scientific literature is used to support the hypothesis that TZDs are inhibitors of microtubule assembly. The similarities between the affects of TZDs on cellular processes and known inhibitors of tubulin polymerization are identified. Similarities between TZDs and currently used inhibitors of microtubule assembly, such as cell cycle arrest in G1 phase, anti-angiogenesis activity, and inhibition of cell motility, are striking. In addition to the similarities in biological function, certain molecular structure similarities are also identified. The possibility that TZDs inhibit the polymerization of actin is presented as an alternative interpretation of the available data. Finally suggestions for testing the hypothesis, by using commercially available tubulin polymerization assays and fluorescence based binding assays, as well as isothermal titration calorimetry, are given. Considering TZD position as third-line therapy for treatment of type 2 diabetes mellitus and the potential loss of market share to newly introduced inhalable insulin, a better understanding of TZD anti-cancer activity may lead to revival for this drug class in cancer treatment.
Insights
Thiazolidinediones (TZDs), used for diabetes, may fight cancer by inhibiting microtubule assembly. This research explores their anti-cancer potential and suggests methods to confirm their mechanism of action.
Area of Science:
- Pharmacology
- Cell Biology
- Oncology
Background:
- Thiazolidinediones (TZDs) are primarily used for type 2 diabetes.
- Emerging evidence suggests TZDs possess anti-cancer properties.
- The precise mechanism behind TZD's anti-cancer activity remains unclear.
Purpose of the Study:
- To hypothesize and investigate the anti-cancer activity of TZDs.
- To explore the potential of TZDs as inhibitors of microtubule assembly.
- To identify potential therapeutic applications for TZDs in cancer treatment.
Main Methods:
- Literature review of empirical data on TZD effects.
- Comparative analysis of TZD cellular effects with known microtubule inhibitors.
- Identification of molecular structure similarities between TZDs and microtubule inhibitors.
Main Results:
- TZDs exhibit similarities to known microtubule assembly inhibitors.
- Observed effects include G1 phase cell cycle arrest, anti-angiogenesis, and inhibition of cell motility.
- Alternative hypothesis suggests TZDs may inhibit actin polymerization.
Conclusions:
- TZDs show promise as anti-cancer agents through microtubule inhibition.
- Further research using tubulin polymerization assays and calorimetry is recommended.
- Understanding TZD's anti-cancer role could revitalize the drug class.
Related Concept Videos
Oral Hypoglycemic Agents: Biguanides and Glitazones
Drugs that Stabilize Microtubules
Inhibition of Cdk Activity
Inhibition of CDK Activity
Drugs that Destabilize Microtubules
Dipeptidyl Peptidase 4 Inhibitors