Related Experiment Video
Updated: Jun 6, 2026

Real-Time Monitoring of Aurora kinase A Activation using Conformational FRET Biosensors in Live Cells
Published on: July 30, 2020
Shared and separate functions of polo-like kinases and aurora kinases in cancer
Susanne M A Lens1, Emile E Voest, René H Medema
1Department of Medical Oncology and Cancer Genomics Centre, UMC Utrecht, Universiteitsweg 100, Stratenum 2. 118, Utrecht 3584 CG, The Netherlands. s.m.a.lens@umcutrecht.nl
Abstract:
Large numbers of inhibitors for polo-like kinases and aurora kinases are currently being evaluated as anticancer drugs. Interest in these drugs is fuelled by the idea that these kinases have unique functions in mitosis. Within the polo-like kinase family, the emphasis for targeted therapies has been on polo-like kinase 1 (PLK1), and in the aurora kinase family drugs have been developed to specifically target aurora kinase A (AURKA; also known as STK6) and/or aurora kinase B (AURKB; also known as STK12). Information on the selectivity of these compounds in vivo is limited, but it is likely that off-target effects within the same kinase families will affect efficacy and toxicity profiles. In addition, it is becoming clear that interplay between polo-like kinases and aurora kinases is much more extensive than initially anticipated, and that both kinase families are important factors in the response to classical chemotherapeutics that damage the genome or the mitotic spindle. In this Review we discuss the implications of these novel insights on the clinical applicability of polo-like kinase and aurora kinase inhibitors.
Insights
Targeting polo-like kinases (PLK) and aurora kinases with anticancer drugs shows promise. Understanding their complex interactions and potential off-target effects is crucial for effective and safe clinical applications.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- Polo-like kinases (PLK) and aurora kinases are key regulators of mitosis.
- Numerous inhibitors targeting PLK1, AURKA, and AURKB are under investigation as anticancer agents.
- Current understanding of kinase inhibitor selectivity in vivo and their complex interplay is limited.
Purpose of the Study:
- To review the clinical applicability of polo-like kinase and aurora kinase inhibitors.
- To discuss the implications of novel insights into kinase interactions and off-target effects.
- To evaluate the impact of these kinases on responses to conventional chemotherapeutics.
Main Methods:
- Literature review of current research on PLK and aurora kinase inhibitors.
- Analysis of in vivo selectivity data for kinase inhibitors.
- Discussion of the interplay between PLK and aurora kinases in mitosis and cancer.
Main Results:
- Interest in PLK and aurora kinase inhibitors is high due to their mitotic roles.
- Limited in vivo selectivity data suggests potential off-target effects impacting efficacy and toxicity.
- Extensive interplay exists between PLK and aurora kinases, influencing responses to DNA-damaging and spindle-targeting chemotherapeutics.
Conclusions:
- Novel insights into PLK and aurora kinase biology necessitate careful consideration for clinical applications.
- Understanding kinase family interplay and off-target effects is critical for optimizing anticancer drug development.
- These kinases are important factors in the efficacy of classical chemotherapeutics, suggesting combination therapy potential.
Related Concept Videos
mTOR Signaling and Cancer Progression
The mTOR pathway or the...
mTOR Signaling and Cancer Progression
The mTOR pathway or the...
PI3K/mTOR/AKT Signaling Pathway
Anaphase Promoting Complex
Adaptive Mechanisms in Cancer Cells
Some of the advantages that cancer cells have on normal cells include - enhanced ability to divide without terminally differentiating, induce new blood vessel formation,...
Adaptive Mechanisms in Cancer Cells
Some of the advantages that cancer cells have on normal cells include - enhanced ability to divide without terminally differentiating, induce new blood vessel formation,...

