Molecular-Level Understanding of the Anticancer Action Mechanism of Anthracyclines / / written by Manish Shandilya [and three others].

• VerfasserIn: Shandilya, Manish,
• Place / Publishing House: London : : IntechOpen,, 2020.
• Year of Publication: 2020
• Language: English
• Physical Description: 1 online resource (260 pages)

Anthracyclines drugs are used as a treatment regime to combat cancer owing to their great chemotherapeutic potential. They are characterized by the presence of a wide range of derivatives, the most famous are doxorubicin and daunorubicin. The proposed action mechanism of anthracyclines and their derivatives to exert cytotoxic effect involves the intercalation of the drug molecule into nucleic acid and inhibition of the activity of topoisomerases. These events consequences in halting DNA replication and transcription mechanisms of the cell. Understanding of the structural and conformational changes associated with nucleic acid after binding with drugs provides significant knowledge for the development of more effective drugs. A comprehensive elucidation of the molecular mechanism(s) of action of anthracyclines drugs plays a significant role in the rational drug designing to obtain an effective, selective, and safe anti-cancer drugs.

Table of Contents

1. Introduction -- 2. Proposed action mechanisms -- 2.1 Anthracyclines as DNA intercalators -- 2.2 How anthracyclines damage DNA? -- 2.2.1 Via topoisomerase II poisoning -- 2.2.2 Via oxidative stress -- 2.2.3 Via forming DNA-anthracycline adduct -- 3. Side effects -- 4. Anthracycline resistance -- 5. Anthracycline analogs -- 6. Conclusion -- Acknowledgments -- Conflict of interest -- References.