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Updated: Oct 22, 2025
Identification of Cyclin-dependent Kinase 1 Specific Phosphorylation Sites by an In Vitro Kinase Assay
Published on: May 3, 2018
Polo-like kinase 1 (PLK1) signaling in cancer and beyond
Styliani Iliaki1, Rudi Beyaert1, Inna S Afonina1
1Center for Inflammation Research, Unit of Molecular Signal Transduction in Inflammation, VIB, B-9052 Ghent, Belgium; Department of Biomedical Molecular Biology, Ghent University, B-9052 Ghent, Belgium.
Abstract:
PLK1 is an evolutionary conserved Ser/Thr kinase that is best known for its role in cell cycle regulation and is expressed predominantly during the G2/S and M phase of the cell cycle. PLK1-mediated phosphorylation of specific substrates controls cell entry into mitosis, centrosome maturation, spindle assembly, sister chromatid cohesion and cytokinesis. In addition, a growing body of evidence describes additional roles of PLK1 beyond the cell cycle, more specifically in the DNA damage response, autophagy, apoptosis and cytokine signaling. PLK1 has an indisputable role in cancer as it controls several key transcription factors and promotes cell proliferation, transformation and epithelial-to-mesenchymal transition. Furthermore, deregulation of PLK1 results in chromosome instability and aneuploidy. PLK1 is overexpressed in many cancers, which is associated with poor prognosis, making PLK1 an attractive target for cancer treatment. Additionally, PLK1 is involved in immune and neurological disorders including Graft versus Host Disease, Huntington's disease and Alzheimer's disease. Unfortunately, newly developed small compound PLK1 inhibitors have only had limited success so far, due to low therapeutic response rates and toxicity. In this review we will highlight the current knowledge about the established roles of PLK1 in mitosis regulation and beyond. In addition, we will discuss its tumor promoting but also tumor suppressing capacities, as well as the available PLK1 inhibitors, elaborating on their efficacy and limitations.
Insights
Polo-like kinase 1 (PLK1) is crucial for cell division and cancer progression. While targeted inhibitors show promise, their limited success necessitates further research into PLK1
Area of Science:
- Molecular Biology
- Cell Biology
- Oncology
Background:
- Polo-like kinase 1 (PLK1) is a key Ser/Thr kinase regulating cell cycle progression, particularly mitosis.
- PLK1 influences critical processes including centrosome maturation, spindle assembly, and cytokinesis.
- Emerging evidence highlights PLK1's roles beyond the cell cycle in DNA damage response, autophagy, and apoptosis.
Purpose of the Study:
- To review the established roles of PLK1 in mitosis and other cellular processes.
- To discuss PLK1's dual role in cancer, acting as both a tumor promoter and suppressor.
- To evaluate the efficacy and limitations of current PLK1 inhibitors for therapeutic applications.
Main Methods:
- Comprehensive literature review of studies on PLK1 function and inhibition.
- Analysis of PLK1's involvement in cell cycle regulation, DNA damage response, and cancer.
- Assessment of clinical data and research findings on PLK1 inhibitors.
Main Results:
- PLK1 is essential for accurate cell division and is frequently overexpressed in various cancers.
- PLK1 dysregulation contributes to genomic instability and aneuploidy, promoting tumorigenesis.
- Current PLK1 inhibitors exhibit limited therapeutic success due to toxicity and response rates.
Conclusions:
- PLK1 is a critical regulator of cell division with significant implications in cancer and other diseases.
- Understanding PLK1's complex roles is vital for developing effective targeted therapies.
- Further research is needed to overcome the limitations of existing PLK1 inhibitors and improve treatment outcomes.
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