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Plk1 Inhibitors in Cancer Therapy: From Laboratory to Clinics
Rosie Elizabeth Ann Gutteridge1, Mary Ann Ndiaye1, Xiaoqi Liu2
1Department of Dermatology, University of Wisconsin, Madison, Wisconsin.
Abstract:
Polo-like kinase 1 (Plk1) overexpression has been shown to occur in a wide range of tumors, prompting research and development of Plk1 inhibitors as a means of cancer treatment. This review discusses recent advances in the development of Plk1 inhibitors for cancer management. Plk1 inhibition has been shown to cause mitotic block and apoptosis of cells with higher mitotic index and therefore higher Plk1 expression. The potential of Plk1 inhibitors as cancer therapeutics has been widely investigated. However, a complete understanding of Plk1 biology/mechanism is yet to be fully achieved. Resistance to certain chemotherapeutic drugs has been linked to Plk1 overexpression, and Plk1-mediated mitotic events such as microtubule rearrangement have been found to reduce the efficacy of chemotherapeutic agents. The Plk1 inhibitor volasertib has shown considerable promise in clinical studies, having reached phase III trials. However, preclinical success with Plk1 inhibitors has not translated well into clinical success. In our view, combined therapies targeting other relevant pathways together with Plk1 may be vital to combat issues observed with monotherapy, especially resistance. In addition, research should also be directed toward understanding the mechanisms of Plk1 and designing additional next generations of specific, potent Plk1 inhibitors to target cancer. Mol Cancer Ther; 15(7); 1427-35. ©2016 AACR.
Insights
Polo-like kinase 1 (Plk1) inhibitors show promise for cancer treatment by inducing cell death. However, clinical success is limited, suggesting combined therapies and further research into Plk1 mechanisms are crucial.
Area of Science:
- Oncology
- Molecular Biology
- Drug Development
Background:
- Polo-like kinase 1 (Plk1) is overexpressed in various tumors.
- Plk1 plays a critical role in cell division and is a target for cancer therapy.
- Understanding Plk1 biology is essential for developing effective cancer treatments.
Purpose of the Study:
- To review recent advances in the development of Plk1 inhibitors for cancer management.
- To discuss the potential and challenges of Plk1 inhibitors in clinical settings.
- To highlight the need for combined therapies and next-generation Plk1 inhibitors.
Main Methods:
- Literature review of Plk1 inhibitor research.
- Analysis of Plk1's role in cell cycle and cancer.
- Evaluation of clinical trial data for Plk1 inhibitors like volasertib.
Main Results:
- Plk1 inhibition leads to mitotic arrest and apoptosis in cancer cells.
- Volasertib has shown promise in Phase III trials, but overall clinical success is limited.
- Plk1 overexpression can contribute to drug resistance and reduced efficacy of chemotherapy.
Conclusions:
- Combined therapies targeting Plk1 and other pathways may overcome monotherapy resistance.
- Further research into Plk1 mechanisms and development of potent, specific inhibitors are necessary.
- Advancing Plk1 inhibitor development requires addressing challenges in clinical translation.
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