Related Experiment Video
Updated: Jun 17, 2026

A Bilingual Computational Workflow for Identifying Potential PLK1 Inhibitors in American Sign Language and English
Published on: April 3, 2026
Polo-like kinase inhibitors: an emerging opportunity for cancer therapeutics
Puneet Chopra1, Gautam Sethi, Sunanda G Dastidar
1New Drug Discovery Research, Department of Pharmacology, Ranbaxy Research Laboratories, Gurgaon-122001-Haryana, India. p.chopra@ranbaxy.com
Importance Of The Field:
The Polo-like kinase (Plk) family has emerged as an important regulator in cell cycle progression. Plks belong to a family of serine/threonine kinases and exist in four isoforms Plk1- 4. However, only one of these isoforms, Plk1, is shown to be involved in the activation of Cdc2, chromosome segregation, centrosome maturation, bipolar spindle formation and execution of cytokinesis. The activity of Plk1 is elevated in tissues and cells with a high mitotic index. In patients, Plk1 is overexpressed in tumors including those derived from lung, breast, colon, pancreas, prostate and ovary. Plk1 depletion is associated with the decrease in cell viability and induction of apoptosis in various cancerous cells. Several Plk1 inhibitors are in different phases of clinical development for anticancer therapy.
Areas Covered In This Review:
The focus of present review is to highlight Plk1 as a promising therapeutic approach for the treatment of cancer. The review discusses the role of Plk1 in cancer and the current status of Plk1 inhibitors, as well as highlighting the possible beneficial effect of inhibition of Plk1 as compared to other mitotic targets.
What The Reader Will Gain:
Readers will get a comprehensive overview of Plk1 as a novel anticancer drug target. This review will also update readers about the progress made in the field of Plk1 inhibitors.
Take Home Message:
The current literature about Plk1 inhibitors and knockout studies favor Plk1 inhibition as a potential antitumor therapy.
Insights
Polo-like kinase 1 (Plk1) is crucial for cell division and is overexpressed in many cancers. Inhibiting Plk1 shows promise as an effective anticancer therapy, with several Plk1 inhibitors in clinical development.
Area of Science:
- Cell Biology
- Molecular Oncology
- Drug Discovery
Background:
- Polo-like kinase (Plk) family regulates cell cycle progression.
- Plk1 isoform is critical for mitosis, including chromosome segregation and cytokinesis.
- Plk1 is overexpressed in various human cancers, correlating with high mitotic index.
Purpose of the Study:
- To review the role of Plk1 in cancer.
- To highlight Plk1 as a potential therapeutic target for cancer treatment.
- To discuss the current status and benefits of Plk1 inhibitors compared to other mitotic targets.
Main Methods:
- Literature review focusing on Plk1's role in cancer.
- Analysis of current Plk1 inhibitors in clinical development.
- Comparison of Plk1 inhibition with other mitotic targets.
Main Results:
- Plk1 is a promising novel drug target for anticancer therapy.
- Significant progress has been made in the development of Plk1 inhibitors.
- Plk1 inhibition demonstrates potential for decreasing cancer cell viability and inducing apoptosis.
Conclusions:
- Plk1 inhibition is a potential antitumor strategy.
- Knockout studies and existing literature support Plk1 inhibition for cancer therapy.
- Plk1 inhibitors represent a developing class of anticancer agents.
Related Concept Videos
Targeted Cancer Therapies
There are several types of targeted therapies against specific...
Targeted Cancer Therapies
There are several types of targeted therapies against specific...
Inhibition of Cdk Activity
Inhibition of CDK Activity
Combination Therapies and Personalized Medicine
The combination of the drug acetazolamide and sulforaphane is a good example of combination therapy to treat cancer. The cells in the interior of a large tumor often die due to the hypoxic and...
mTOR Signaling and Cancer Progression
The mTOR pathway or the...
