New insights into the anticancer therapeutic potential of maytansine and its derivatives - 13/08/23
Abstract |
Maytansine is a pharmacologically active 19-membered ansamacrolide derived from various medicinal plants and microorganisms. Among the most studied pharmacological activities of maytansine over the past few decades are anticancer and anti-bacterial effects. The anticancer mechanism of action is primarily mediated through interaction with the tubulin thereby inhibiting the assembly of microtubules. This ultimately leads to decreased stability of microtubule dynamics and cause cell cycle arrest, resulting in apoptosis. Despite its potent pharmacological effects, the therapeutic applications of maytansine in clinical medicine are quite limited due to its non-selective cytotoxicity. To overcome these limitations, several derivatives have been designed and developed mostly by modifying the parent structural skeleton of maytansine. These structural derivatives exhibit improved pharmacological activities as compared to maytansine. The present review provides a valuable insight into maytansine and its synthetic derivatives as anticancer agents.
Le texte complet de cet article est disponible en PDF.Graphical Abstract |
Highlights |
• | Maytansine is a naturally occurring microtubule destabilizing agent. |
• | High systemic toxicity of maytansine limited its therapeutic window. |
• | Development of synthetic derivatives has enhanced the therapeutic potential of the parent compound. |
• | Conjugation of monoclonal antibodies with maytansine derivatives have increased their efficiency against various types of cancer. |
• | T-DM1, is an FDA approved ADC targeting the Her2 + breast cancer. |
Keywords : Maytansine, Derivatives, Antibody-drug conjugate, Cytotoxicity, Anticancer activity, Tubulin instability
Plan
Vol 165
Article 115039- septembre 2023 Retour au numéroBienvenue sur EM-consulte, la référence des professionnels de santé.
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