Related Experiment Video

Updated: Aug 19, 2026

A Bilingual Computational Workflow for Identifying Potential PLK1 Inhibitors in American Sign Language and English
14:34

A Bilingual Computational Workflow for Identifying Potential PLK1 Inhibitors in American Sign Language and English

Published on: April 3, 2026

ON01910, a non-ATP-competitive small molecule inhibitor of Plk1, is a potent anticancer agent

Kiranmai Gumireddy1, M V Ramana Reddy, Stephen C Cosenza

  • 1Fels Institute for Cancer Research and Molecular Biology, Temple University School of Medicine, 3307 N. Broad Street, Philadelphia, Pennsylvania 19140, USA.

Cancer Cell
|March 16, 2005
PubMed

Insights

ON01910, a polo-like kinase 1 (Plk1) inhibitor, effectively halts tumor cell division and induces apoptosis. This novel compound shows potent anti-tumor effects in vivo without significant toxicity and synergizes with chemotherapy.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Polo-like kinase 1 (Plk1) is overexpressed in numerous human cancers.
  • Inhibiting Plk1 activity leads to mitotic arrest and apoptosis in tumor cells.

Purpose of the Study:

  • To characterize ON01910, a novel small molecule inhibitor of Plk1.
  • To evaluate the anti-tumor efficacy and safety profile of ON01910.

Main Methods:

  • In vitro assays to determine the mechanism of Plk1 inhibition.
  • In vivo studies using xenograft nude mouse models.
  • Evaluation of synergistic effects with chemotherapeutic agents.

Main Results:

  • ON01910 inhibits Plk1 activity by competing for the substrate binding site, not the ATP-binding site.
  • The compound induces mitotic arrest and apoptosis in tumor cells via spindle abnormalities.
  • ON01910 demonstrated potent tumor growth inhibition in vivo without significant hematotoxicity, liver damage, or neurotoxicity.
  • Significant synergy was observed between ON01910 and various chemotherapeutic agents, leading to complete tumor regression in some cases.

Conclusions:

  • ON01910 is a potent Plk1 inhibitor with a favorable safety profile.
  • ON01910 exhibits significant anti-tumor activity and synergistic potential with chemotherapy, warranting further clinical investigation.

More Related Videos

Through the Looking Glass: Time-lapse Microscopy and Longitudinal Tracking of Single Cells to Study Anti-cancer Therapeutics06:00

Through the Looking Glass: Time-lapse Microscopy and Longitudinal Tracking of Single Cells to Study Anti-cancer Therapeutics

Published on: May 14, 2016

Related Concept Videos

Inhibition of Cdk Activity02:34

Inhibition of Cdk Activity

The orderly progression of the cell cycle depends on the activation of Cdk protein by binding to its cyclin partner. However, the cell cycle must be restricted when undergoing abnormal changes. Most cancers correlate to the deregulated cell cycle, and since Cdks are a central component of the cell cycle, Cdk inhibitors are extensively studied to develop anticancer agents. For instance, cyclin D associates with several Cdks, such as Cdk 4/6, to form an active complex. The cyclin D-Cdk4/6 complex...
Inhibition of CDK Activity02:34

Inhibition of CDK Activity

The orderly progression of the cell cycle depends on the activation of Cdk protein by binding to its cyclin partner. However, the cell cycle must be restricted when undergoing abnormal changes. Most cancers correlate to the deregulated cell cycle, and since Cdks are a central component of the cell cycle, Cdk inhibitors are extensively studied to develop anticancer agents. For instance, cyclin D associates with several Cdks, such as Cdk 4/6, to form an active complex. The cyclin D-Cdk4/6 complex...
Negative Regulator Molecules01:23

Negative Regulator Molecules

Positive regulators allow a cell to advance through cell cycle checkpoints. Negative regulators have an equally important role as they terminate a cell’s progression through the cell cycle—or pause it—until the cell meets specific criteria.
M-Cdk Drives Transition Into Mitosis02:15

M-Cdk Drives Transition Into Mitosis

Checkpoints throughout the cell cycle serve as safeguards and gatekeepers, allowing the cell cycle to progress in favorable conditions and slow or halt it in problematic ones. This regulation is known as the cell cycle control system.
Cyclin-dependent kinases, or Cdks, work in concert with cyclins to control cell cycle transitions. M-Cdk, a complex of Cdk1 bound to M cyclin, is a well-known example of this coordinated control that drives the transition from the G2 to the M phase.
M cyclin...
Drugs that Destabilize Microtubules01:10

Drugs that Destabilize Microtubules

Microtubules are dynamic structures and can be regulated by microtubule targeting agents (MTAs). Microtubule destabilizing drugs are a class of MTAs that destabilize and prevent microtubules' polymerization. Both natural and synthetic chemicals can be found under this class of drugs. Vincristine and vinblastine, two vinca alkaloids, and colchicine were among the first to be discovered. These drugs can affect cells in various ways, either by inducing a change in cell morphology, preventing...
DNA Damage can Stall the Cell Cycle02:36

DNA Damage can Stall the Cell Cycle

In response to DNA damage, cells can pause the cell cycle to assess and repair the breaks. However, the cell must check the DNA at certain critical stages during the cell cycle. If the cell cycle pauses before DNA replication, the cells will contain twice the amount of DNA. On the other hand, if cells arrest after DNA replication but before mitosis, they will contain four times the normal amount of DNA. With a host of specialized proteins at their disposal,cells must use the right protein at...