Recent advancements in microtubule targeting agents for breast cancer: design strategies and pharmacological insights
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Updated: May 22, 2026

Live Imaging to Study Microtubule Dynamic Instability in Taxane-resistant Breast Cancers
Published on: February 20, 2017
Paramjeet Kaur1, Rajiv Sharma2
1University Institute of Pharma Sciences, Chandigarh University, Mohali, 140413, India.
Abstract:
Despite advances in the current treatment strategies for breast cancer management, chemotherapeutic resistance and recurrence are now recognised as a substantial global health problem. Microtubule-targeting agents are key clinical candidates in breast cancer therapy that abrogate tubulin dynamics, lead to arrest in mitosis, and enhance apoptosis of cancer cells. However, traditional agents like taxanes and vinca alkaloids suffer from the serious issue of toxicity, suboptimal pharmacokinetics, and multidrug resistance. Novel scaffolds and molecular hybrids have been reported to exhibit potent activity against resistant breast cancer cells by targeting the colchicine or taxane sites of tubulin. In addition, multi-targeting and dual-targeting ligands showed interesting combinatory effects. This review discusses the design strategies, structure-activity relationship studies, and pharmacological knowledge of a new class of microtubule-targeting agents to encourage further scope in the development of next-generation, selective, and safer antimitotic agents for better management of breast cancers.
Insights
Novel microtubule-targeting agents show promise for overcoming drug resistance in breast cancer treatment. This review explores new designs and strategies for developing safer, more effective antimitotic drugs to combat cancer recurrence.
Area of Science:
- Oncology
- Pharmacology
- Molecular Biology
Background:
- Chemotherapeutic resistance and recurrence remain significant challenges in breast cancer management.
- Microtubule-targeting agents are crucial for breast cancer therapy, but traditional drugs face limitations like toxicity and resistance.
- Novel agents targeting tubulin offer potential solutions against resistant cancer cells.
Purpose of the Study:
- To review the design strategies, structure-activity relationships, and pharmacology of novel microtubule-targeting agents.
- To explore the potential of multi-targeting and dual-targeting ligands in combination therapy.
- To encourage the development of next-generation, selective, and safer antimitotic agents for breast cancer.
Main Methods:
- Literature review of recent advancements in microtubule-targeting agents for breast cancer.
- Analysis of structure-activity relationships for novel scaffolds and molecular hybrids.
- Discussion of pharmacological properties and potential therapeutic applications.
Main Results:
- Novel scaffolds and molecular hybrids demonstrate potent activity against resistant breast cancer cells.
- Targeting colchicine or taxane sites on tubulin is a viable strategy.
- Multi-targeting and dual-targeting ligands exhibit promising combinatory effects.
Conclusions:
- New classes of microtubule-targeting agents offer improved efficacy and safety profiles.
- Further research into these novel agents can lead to better breast cancer treatment outcomes.
- Development of selective and safer antimitotic drugs is essential for managing resistant breast cancer.
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