Abstract
The interaction of taxol with DNA has major biological importance since it is shown the presence of higher concentration of taxol in the nucleus, than in the human lung tumor cell. Therefore, in this report we examine the interaction of taxol with calf-thymus DNA in aqueous solution at physiological pH, using constant DNA concentration (25 or 1.25 mM phosphate) and various taxol / DNA (phosphate) ratios 1 / 200 to 1 / 2. Capillary electrophoresis and Fourier transform infrared (FTIR) difference spectroscopic methods are used to characterize the nature of drug-DNA interaction and to determine the taxol binding site, the binding constant, sequence selectivity, helix stability and biopolymer secondary structure in the taxol-DNA complexes in vitro. Structural analysis showed that taxol is an external DNA binder with no affinity towards DNA intercalation. The major target of taxol is A-T, G-C bases and the backbone PO2 groups. Two bindings were observed for taxol-DNA complexes with K1= 1.4 x 104 M-1 and K2=3.5 X 103 M-1. The taxol-DNA interaction is associated with a partial helix stabilization and no major alterations of B-DNA structures.
Keywords: dna, taxol, binding site, binding constant, conformation, helix stability, electrophoresis, ftir, uv-visible spectroscopy
Mini-Reviews in Medicinal Chemistry
Title: Taxol Anticancer Activity and DNA Binding
Volume: 5 Issue: 3
Author(s): H. Malonga, J. F. Neault, S. Diamantoglou and H. A. Tajmir-Riahi
Affiliation:
Keywords: dna, taxol, binding site, binding constant, conformation, helix stability, electrophoresis, ftir, uv-visible spectroscopy
Abstract: The interaction of taxol with DNA has major biological importance since it is shown the presence of higher concentration of taxol in the nucleus, than in the human lung tumor cell. Therefore, in this report we examine the interaction of taxol with calf-thymus DNA in aqueous solution at physiological pH, using constant DNA concentration (25 or 1.25 mM phosphate) and various taxol / DNA (phosphate) ratios 1 / 200 to 1 / 2. Capillary electrophoresis and Fourier transform infrared (FTIR) difference spectroscopic methods are used to characterize the nature of drug-DNA interaction and to determine the taxol binding site, the binding constant, sequence selectivity, helix stability and biopolymer secondary structure in the taxol-DNA complexes in vitro. Structural analysis showed that taxol is an external DNA binder with no affinity towards DNA intercalation. The major target of taxol is A-T, G-C bases and the backbone PO2 groups. Two bindings were observed for taxol-DNA complexes with K1= 1.4 x 104 M-1 and K2=3.5 X 103 M-1. The taxol-DNA interaction is associated with a partial helix stabilization and no major alterations of B-DNA structures.
Export Options
About this article
Cite this article as:
Malonga H., Neault F. J., Diamantoglou S. and Tajmir-Riahi A. H., Taxol Anticancer Activity and DNA Binding, Mini-Reviews in Medicinal Chemistry 2005; 5 (3) . https://dx.doi.org/10.2174/1389557053175371
DOI https://dx.doi.org/10.2174/1389557053175371 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
Call for Papers in Thematic Issues
Bioprospecting of Natural Products as Sources of New Multitarget Therapies
According to the Convention on Biological Diversity, bioprospecting is the exploration of biodiversity and indigenous knowledge to develop commercially valuable products for pharmaceutical and other applications. Bioprospecting involves searching for useful organic compounds in plants, fungi, marine organisms, and microorganisms. Natural products traditionally constituted the primary source of more than ...read more
Computational Frontiers in Medicinal Chemistry
The thematic issue "Computational Frontiers in Medicinal Chemistry" provides a robust platform for delving into state-of-the-art computational methodologies and technologies that significantly propel advancements in medicinal chemistry. This edition seeks to amalgamate top-tier reviews spotlighting the latest trends and breakthroughs in the fusion of computational approaches, including artificial intelligence (AI) ...read more
Natural Products and Dietary Supplements in Alleviation of Metabolic, Cardiovascular, and Neurological Disorders
Metabolic disorders like diabetes, obesity, inflammation, oxidative stress, cancer etc, cardiovascular disorders like angina, myocardial infarction, congestive heart failure etc as well as neurological disorders like Alzheimer?s, Parkinson?s, Epilepsy, Depression, etc are the global burden. They covered the major segment of the diseases and disorders from which the human community ...read more
Natural Products in Drug Discovery
Natural products have always been one of the important ways of drug discovery due to their novel skeleton and diverse functional group characteristics. According to statistics, between 1981 and 2019, the FDA approved a total of 1,394 small molecule drugs for marketing, of which 930 marketed drugs originated from the ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers