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Updated: Apr 20, 2026
High-throughput Screening for Chemical Modulators of Post-transcriptionally Regulated Genes
Published on: March 3, 2015
Target driven preclinical screening for new antimitotic chemotherapy agents
S Novío, M Freire-Garabal, M J Núñez1
1Lennart Levi Stress and Neuroimmunology Laboratory, Department of Pharmacology, School of Medicine, C/ San Francisco, s/n, 15782 Santiago de Compostela, A Coruna, Spain. snl@usc.es.
Abstract:
Currently approved antimitotic therapies used in chemotherapy are microtubule-targeting agents (MTAs). Despite they achieved some level of success, they have limited efficacy as single agents, with issues of slippages and resistance, and cause significant side effects. The advances in the identification of other mitosis-related targets led to the development of new mitotic regulators aimed to perturb mitosis without interfering with microtubule dynamics in non-dividing cells trying to reduce side effects in patients. Some of these compounds like those targeted to entry and mitotic kinases, mitotic kinesins/motor proteins, and multiprotein complexes have been evaluated in vitro and in animal models, and some of them have reached clinical trials. Despite promising preclinical results, in many cases, the efficacy demonstrated by these new antimitotics was not better than current microtubule inhibitors. In this paper we review present and future strategies on the search for new antimitotic compounds based on identification of new protein targets and development of multifunctional inhibitors of mitosis in cancer cells.
Insights
New cancer therapies target mitosis beyond microtubules. While promising, novel antimitotic drugs show limited efficacy compared to current agents, necessitating further research into new targets and combination strategies.
Area of Science:
- Oncology
- Cell Biology
- Pharmacology
Background:
- Approved antimitotic therapies (microtubule-targeting agents) have efficacy limitations and side effects.
- New strategies focus on novel mitosis targets to reduce patient side effects.
Purpose of the Study:
- Review current and future strategies for novel antimitotic compound discovery.
- Evaluate new targets and multifunctional inhibitors for cancer therapy.
Main Methods:
- Literature review of antimitotic drug development.
- Analysis of novel targets beyond microtubule dynamics.
- Assessment of preclinical and clinical trial data for new agents.
Main Results:
- New antimitotics target kinases, kinesins, and multiprotein complexes.
- Preclinical data show promise, but clinical efficacy often matches current microtubule inhibitors.
- Resistance and side effects remain challenges for both old and new agents.
Conclusions:
- Developing novel antimitotic compounds requires identifying new protein targets.
- Multifunctional inhibitors offer a promising strategy to overcome resistance and reduce side effects.
- Further research is crucial for advancing cancer chemotherapy beyond microtubule-targeting agents.
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