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Present and Future Perspective on PLK1 Inhibition in Cancer Treatment
Michela Chiappa1, Serena Petrella1, Giovanna Damia1
1Laboratory of Experimental Oncology, Department of Oncology, Istituto di Ricerche Farmacologiche Mario Negri-IRCCS, Milan, Italy.
Abstract:
Polo-like kinase 1 (PLK1) is the principle member of the well conserved serine/threonine kinase family. PLK1 has a key role in the progression of mitosis and recent evidence suggest its important involvement in regulating the G2/M checkpoint, in DNA damage and replication stress response, and in cell death pathways. PLK1 expression is tightly spatially and temporally regulated to ensure its nuclear activation at the late S-phase, until the peak of expression at the G2/M-phase. Recently, new roles of PLK1 have been reported in literature on its implication in the regulation of inflammation and immunological responses. All these biological processes are altered in tumors and, considering that PLK1 is often found overexpressed in several tumor types, its targeting has emerged as a promising anti-cancer therapeutic strategy. In this review, we will summarize the evidence suggesting the role of PLK1 in response to DNA damage, including DNA repair, cell cycle progression, epithelial to mesenchymal transition, cell death pathways and cancer-related immunity. An update of PLK1 inhibitors currently investigated in preclinical and clinical studies, in monotherapy and in combination with existing chemotherapeutic drugs and targeted therapies will be discussed.
Insights
Polo-like kinase 1 (PLK1) is crucial for cell division and cancer. This review explores PLK1
Area of Science:
- Molecular Biology
- Cell Biology
- Oncology
Background:
- Polo-like kinase 1 (PLK1) is a key serine/threonine kinase regulating mitosis.
- PLK1 is implicated in DNA damage response, cell cycle checkpoints, and cell death.
- Emerging roles in inflammation and immunity, alongside overexpression in tumors, highlight PLK1 as a therapeutic target.
Purpose of the Study:
- To review the multifaceted roles of PLK1 in DNA damage response, cell cycle, and immunity.
- To discuss the therapeutic potential of targeting PLK1 in cancer treatment.
- To provide an update on PLK1 inhibitors in preclinical and clinical development.
Main Methods:
- Literature review of scientific articles and clinical trial data.
- Synthesis of evidence on PLK1's function in DNA repair, cell cycle, EMT, cell death, and immunity.
- Analysis of current PLK1 inhibitor strategies in monotherapy and combination treatments.
Main Results:
- PLK1 is vital for DNA repair, cell cycle progression (G2/M checkpoint), and epithelial-mesenchymal transition (EMT).
- PLK1 influences cancer-related immunity and various cell death pathways.
- Numerous PLK1 inhibitors are under investigation, showing promise in preclinical and clinical settings.
Conclusions:
- PLK1's diverse roles in cell biology and cancer underscore its significance.
- Targeting PLK1 presents a promising strategy for novel anti-cancer therapies.
- Ongoing research and clinical trials are evaluating PLK1 inhibitors for improved cancer treatment outcomes.
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