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Fluorescence-based Monitoring of PAD4 Activity via a Pro-fluorescence Substrate Analog
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Therapeutic potential of targeting polo-like kinase 4

Qian Lei1, Quanwei Yu1, Na Yang2

  • 1Department of Respiratory and Critical Care Medicine, West China Hospital and Targeted Tracer Research and Development Laboratory, Precision Medicine Key Laboratory of Sichuan Province & Precision Medicine Center, West China Hospital, Sichuan University, Chengdu, Sichuan, 610041, China.

European Journal of Medicinal Chemistry
|January 10, 2024
PubMed

Insights

Polo-like kinase 4 (PLK4) regulates cell division and its abnormal expression drives cancer. PLK4 inhibitors show promise as cancer therapeutics, with several compounds in clinical trials.

Area of Science:

  • Cell Biology
  • Molecular Oncology

Background:

  • Polo-like kinase 4 (PLK4) is a crucial regulator of centriole duplication, essential for accurate cell division.
  • Aberrant PLK4 expression is linked to genomic instability and poor prognosis in various cancers.

Purpose of the Study:

  • To review the structure, function, and regulation of PLK4.
  • To summarize recent advancements in PLK4 inhibitors for cancer therapy.

Main Methods:

  • Literature review of PLK4 structure, function, and regulation.
  • Analysis of recent patents and publications on PLK4 inhibitors.
  • Discussion of therapeutic strategies involving PLK4 inhibition.

Main Results:

  • PLK4's role in centriole duplication and mitosis is well-established.
  • PLK4 dysregulation contributes significantly to cancer development and metastasis.
  • Numerous small-molecule PLK4 inhibitors have been developed, with some in clinical trials.

Conclusions:

  • PLK4 is a validated therapeutic target for human cancers.
  • PLK4 inhibitors demonstrate potential as monotherapies or in combination treatments for cancer.
Keywords:
Cancer therapyCentrosome duplicationDrug discoveryPLK4 inhibitorsPolo-like kinase 4 (PLK4)

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