Related Experiment Video

Updated: Apr 21, 2026

Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays
13:22

Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays

Published on: October 23, 2019

8.5K

A new small-molecule Aurora B inhibitor shows antitumor activity in human cancer cell lines

Yuanyuan Wu1, Jie Li, Chenxiao Jiang

  • 1State Key Laboratory of Genetic Engineering, Institute of Genetics, School of Life Sciences, Fudan University, Shanghai, 200433, People's Republic of China, windapple@126.com.

Molecular Biology Reports
|October 29, 2014
PubMed

Insights

The small molecule S4 inhibits Aurora kinase, a key regulator of cell division. This Aurora kinase inhibition reduces cancer cell growth and triggers programmed cell death, offering a potential new cancer therapy.

Area of Science:

  • Molecular Biology
  • Cell Biology
  • Biochemistry

Background:

  • Aurora kinases are serine/threonine kinases crucial for cell cycle regulation.
  • These kinases are frequently overexpressed or amplified in various human tumors.
  • Targeting Aurora kinases presents a potential strategy for cancer therapy.

Purpose of the Study:

  • To investigate the inhibitory effects of the small molecule S4 on Aurora kinase.
  • To evaluate the impact of Aurora kinase inhibition by S4 on cancer cell proliferation and survival.

Main Methods:

  • Biochemical and cell-based assays were employed to assess S4's activity.
  • Inhibition of Aurora B was confirmed by monitoring Histone H3 phosphorylation.
  • Cell proliferation, colony formation, cell cycle progression, and apoptosis assays were performed.

Main Results:

  • S4 effectively inhibited Aurora kinase activity at both biochemical and cellular levels.
  • S4 treatment reduced cancer cell proliferation and colony formation capabilities.
  • S4 induced cell cycle arrest in pseudo G1 phase and promoted apoptotic cell death in a dose- and time-dependent manner.

Conclusions:

  • The small molecule S4 acts as an effective inhibitor of Aurora kinase.
  • S4 demonstrates significant anti-cancer effects by inhibiting cancer cell growth and inducing apoptosis.
  • S4 represents a promising candidate for further development as a cancer therapeutic agent.

More Related Videos

Real-Time Monitoring of Aurora kinase A Activation using Conformational FRET Biosensors in Live Cells06:29

Real-Time Monitoring of Aurora kinase A Activation using Conformational FRET Biosensors in Live Cells

Published on: July 30, 2020

3.4K
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

10.8K

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...
4.8K
Inhibition of CDK Activity02:34

Inhibition of CDK Activity

4.3K
Targeted Cancer Therapies02:57

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against...
6.9K
mTOR Signaling and Cancer Progression03:03

mTOR Signaling and Cancer Progression

The mammalian target of rapamycin or mTOR protein was discovered in 1994 due to its direct interaction with rapamycin. The protein gets its name from a yeast homolog called TOR. The mTOR protein complex in mammalian cells plays a major role in balancing anabolic processes such as the synthesis of proteins, lipids, and nucleotides and catabolic processes, such as autophagy in response to environmental cues, such as availability of nutrients and growth factors.
The mTOR pathway or the...
3.6K
PI3K/mTOR/AKT Signaling Pathway01:22

PI3K/mTOR/AKT Signaling Pathway

The mammalian target of rapamycin  (mTOR) is a serine/threonine kinase that regulates growth, proliferation, and cell survival in response to hormones, growth factors, or nutrient availability. This kinase exists in two structurally and functionally distinct forms: mTOR complex 1  (mTORC1) and mTOR complex 2  (mTORC2). The first form (mTORC1) is composed of a rapamycin-sensitive Raptor and proline-rich Akt substrate, PRAS40. In contrast,  mTORC2 consists of a...
5.1K
Combination Therapies and Personalized Medicine02:50

Combination Therapies and Personalized Medicine

Combining two or more treatment methods increases the life span of cancer patients while reducing damage to vital organs or tissue from the overuse of a single treatment. Combination therapy also targets different cancer-inducing pathways, thus reducing the chances of developing resistance to treatment.
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...
4.8K