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Polo-like Kinase 1 Inhibitors in Human Cancer Therapy: Development and Therapeutic Potential

Jifa Zhang1,2, Lele Zhang1,2, Jiaxing Wang3

  • 1Targeted Tracer Research and Development Laboratory, Institute of Respiratory Health, Frontiers Science Center for Disease-related Molecular Network, Joint Research Institution of Altitude Health, National Clinical Research Center for Geriatrics, West China Hospital, Sichuan University, Chengdu 610041, Sichuan, China.

Journal of Medicinal Chemistry
|July 25, 2022
PubMed

Insights

Polo-like kinase 1 (PLK1) inhibitors show promise as cancer treatments. Newer, more selective inhibitors offer improved potency and drug properties, advancing antitumor therapies.

Area of Science:

  • Oncology
  • Molecular Biology
  • Drug Discovery

Background:

  • Polo-like kinase 1 (PLK1) is crucial for cell division and is overexpressed in many cancers.
  • PLK1 is a validated target for cancer therapy due to its role in proliferation and poor prognosis.

Purpose of the Study:

  • To review the structure-activity relationships (SARs) of Polo-like kinase 1 inhibitors (PLK1i).
  • To provide insights into the development of novel PLK1-targeting drugs for clinical application.

Main Methods:

  • Review of existing literature on PLK1 inhibitors.
  • Analysis of structure-activity relationships (SARs) for PLK1i.
  • Evaluation of drug properties including selectivity, potency, and ADME characteristics.

Main Results:

  • Several PLK1 inhibitors have entered clinical trials, with some showing promise.
  • Early kinase domain (KD) inhibitors faced challenges with specificity and toxicity.
  • Recent PLK1i exhibit enhanced selectivity, potency, and favorable ADME profiles.

Conclusions:

  • PLK1 remains a significant target for anticancer drug development.
  • Advances in inhibitor design are overcoming previous limitations, leading to more effective therapies.
  • Understanding SARs is key to developing next-generation PLK1 inhibitors for clinical use.

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