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Recent Advances in Microtubule Targeting Agents for Cancer Therapy
Henrique C Assunção1,2, Patrícia M A Silva3,4,5, Hassan Bousbaa5
1Laboratory of Organic and Pharmaceutical Chemistry, Department of Chemical Sciences, Faculty of Pharmacy, University of Porto, Rua de Jorge de Viterbo Ferreira, 288, 4050-313 Porto, Portugal.
Abstract:
Cancer mortality and the development of cancer resistance present significant challenges that must be addressed to ensure global health. Among anticancer agents, microtubule-targeting agents (MTAs) represent a well-recognized therapeutic approach that disrupts microtubule dynamics, thereby inhibiting cell division, and has been widely used to treat several types of cancers. However, even though MTAs are widely regarded as effective, their potential is limited primarily due to cancer resistance and toxicity. Consequently, in the last years, the exploration of new MTAs with the aim of identifying agents with improved cytotoxicity, selectivity, and adequate pharmacokinetic profile, as well as the ability to evade drug resistance mechanisms, has remained a major concern in the development of anticancer treatment. This review highlights the discovery of new MTAs since 2020, with the goal of understanding the advancements made in this field and its future directions. Special attention is given to structure-activity relationship (SAR) studies that could be important for the discovery of more effective MTAs in the future.
Insights
Researchers are discovering new microtubule-targeting agents (MTAs) to overcome cancer resistance and toxicity. This review focuses on advancements since 2020, emphasizing structure-activity relationship studies for more effective anticancer drugs.
Area of Science:
- Oncology
- Pharmacology
- Molecular Biology
Background:
- Microtubule-targeting agents (MTAs) are crucial in cancer therapy by disrupting cell division.
- Existing MTAs face limitations due to cancer resistance and significant toxicity.
- Developing novel MTAs is essential to improve treatment efficacy and patient outcomes.
Purpose of the Study:
- To review the discovery of new microtubule-targeting agents (MTAs) since 2020.
- To understand recent advancements in MTA development for cancer treatment.
- To identify future directions for novel anticancer drug discovery.
Main Methods:
- Literature review of scientific publications and patents since 2020.
- Analysis of structure-activity relationship (SAR) studies for new MTAs.
- Evaluation of cytotoxicity, selectivity, pharmacokinetics, and resistance evasion.
Main Results:
- Identification of several novel MTA candidates with improved properties.
- Highlighting SAR studies that guide the design of more effective agents.
- Demonstrating progress in overcoming resistance mechanisms and reducing toxicity.
Conclusions:
- Recent discoveries show promise for developing next-generation MTAs.
- SAR studies are critical for designing MTAs with enhanced efficacy and safety.
- Continued research into novel MTAs is vital for advancing cancer therapy.
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