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Multifaceted polo-like kinases: drug targets and antitargets for cancer therapy

Klaus Strebhardt1

  • 1Department of Obstetrics and Gynaecology, School of Medicine, J.W. Goethe University, Theodor Stern Kai 7, 60590 Frankfurt, Germany. strebhardt@em.uni-frankfurt.de

Nature Reviews. Drug Discovery
|July 31, 2010
PubMed

Insights

Polo-like kinase 1 (PLK1) is a key target for cancer therapies. Small-molecule inhibitors targeting PLK1 are advancing, while related PLKs may act as tumor suppressors in cancer.

Area of Science:

  • Cell Biology
  • Molecular Oncology
  • Drug Discovery

Background:

  • Polo-like kinase 1 (PLK1) is crucial for cell cycle regulation, collaborating with CDK1-cyclin B1 and Aurora kinases.
  • PLK1 is a validated preclinical cancer target, driving interest in small-molecule inhibitors for anticancer drug development.
  • The roles of PLK2, PLK3, and PLK4 in cancer are less understood, but PLK2 and PLK3 may function as tumor suppressors via the p53 signaling network.

Purpose of the Study:

  • To review recent biological insights into polo-like kinases (PLKs).
  • To emphasize the role of PLKs in malignant transformation.
  • To examine the progress in developing small-molecule PLK1 inhibitors.

Main Methods:

  • Literature review of recent studies on PLK biology and cancer.
  • Analysis of preclinical data for PLK1 inhibitors.
  • Examination of the role of PLKs in cell cycle regulation and cancer.

Main Results:

  • PLK1's established role in cell cycle orchestration makes it a promising anticancer target.
  • Small-molecule PLK1 inhibitors show potential for cancer therapy.
  • Emerging evidence suggests PLK2 and PLK3 function as tumor suppressors, impacting the p53 signaling pathway.

Conclusions:

  • PLK1 is a significant target in oncology, with ongoing development of targeted inhibitors.
  • Further research into PLK2, PLK3, and PLK4 may reveal new therapeutic strategies and insights into tumor suppression mechanisms.

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