ArticleMolecular cancer2010
Quantitative analysis of the effect of tubulin isotype expression on sensitivity of cancer cell lines to a set of novel colchicine derivatives.
Article in Molecular cancer, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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Who cites it
19 citing papers in PubMed, 41 citations in OpenAlex.
- Review
- Computational Analysis and Experimental Testing of the Molecular Mode of Action of Gatastatin and Its Derivatives.Cancers · 2023Article
- βIII-tubulin suppression enhances the activity of Amuvatinib to inhibit cell proliferation in c-Met positive non-small cell lung cancer cells.Cancer medicine · 2023Article
- Investigation of the effects of overexpression of jumping translocation breakpoint (JTB) protein in MCF7 cells for potential use as a biomarker in breast cancer.American journal of cancer research · 2022Article
- Article
- 6-MOMIPP, a novel brain-penetrant anti-mitotic indolyl-chalcone, inhibits glioblastoma growth and viability.Cancer chemotherapy and pharmacology · 2019Article
- Antiproliferative Activity and Molecular Docking of Novel Double-Modified Colchicine Derivatives.Cells · 2018Article
- Novel mutations involving βI-, βIIA-, or βIVB-tubulin isotypes with functional resemblance to βIII-tubulin in breast cancer.Protoplasma · 2017Article
- Effect of CH-35, a novel anti-tumor colchicine analogue, on breast cancer cells overexpressing the βIII isotype of tubulin.Investigational new drugs · 2016Article
- Article
- Entropic analysis reveals a connection between the recurrence of cancer and chemotherapy.Saudi journal of biological sciences · 2015Article
- 6-Methoxy Podophyllotoxin Induces Apoptosis via Inhibition of TUBB3 and TOPIIA Gene Expressions in 5637 and K562 Cancer Cell Lines.Cell journal · 2015Article
- Targeting Toxoplasma tubules: tubulin, microtubules, and associated proteins in a human pathogen.Eukaryotic cell · 2015Review
- Molecular insight of isotypes specific β-tubulin interaction of tubulin heterodimer with noscapinoids.Journal of computer-aided molecular design · 2014Article
- Aptamers as both drugs and drug-carriers.BioMed research international · 2014Review
- Increased α-tubulin1b expression indicates poor prognosis and resistance to chemotherapy in hepatocellular carcinoma.Digestive diseases and sciences · 2013Article
- Tubulin-interactive stilbene derivatives as anticancer agents.Cellular & molecular biology letters · 2013Review
- Determination of the optimal tubulin isotype target as a method for the development of individualized cancer chemotherapy.Theoretical biology & medical modelling · 2013Article
- Article
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Authors and funding
8 authors at 2 institutions in 2 countries.
Funding
Abstract
backgroundA maximum entropy approach is proposed to predict the cytotoxic effects of a panel of colchicine derivatives in several human cancer cell lines. Data was obtained from cytotoxicity assays performed with 21 drug molecules from the same family of colchicine compounds and correlate these results with independent tubulin isoform expression measurements for several cancer cell lines. The maximum entropy method is then used in conjunction with computed relative binding energy values for each of the drug molecules against tubulin isotypes to which these compounds bind with different affinities.
resultsWe have found by using our analysis that alphabetaI and alphabetaIII tubulin isoforms are the most important isoforms in establishing predictive response of cancer cell sensitivity to colchicine derivatives. However, since alphabetaI tubulin is widely distributed in the human body, targeting it would lead to severe adverse side effects. Consequently, we have identified tubulin isotype alphabetaIII as the most important molecular target for inhibition of microtubule polymerization and hence cancer cell cytotoxicity. Tubulin isotypes alphabetaI and alphabetaII are concluded to be secondary targets.
conclusionsThe benefit of being able to correlate expression levels of specific tubulin isotypes and the resultant cell death effect is that it will enable us to better understand the origin of drug resistance and hence design optimal structures for the elimination of cancer cells. The conclusion of the study described herein identifies tubulin isotype alphabetaIII as a target for optimized chemotherapy drug design.
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