Related Experiment Video
Updated: Nov 20, 2025
Toxicological Assays for Testing Effects of an Epigenetic Drug on Development, Fecundity and Survivorship of Malaria Mosquitoes
Published on: January 16, 2015
Targeting EZH2 as cancer therapy
Shunsuke Hanaki1, Midori Shimada1
1Department of Biochemistry, Joint Faculty of Veterinary Science, Yamaguchi University, 1677-1 Yoshida, Yamaguchi 753-8511, Japan.
Abstract:
Enhancer of zeste homolog 2 (EZH2) is the catalytic subunit of polycomb repressive complex 2 (PRC2) that mediate repression of target genes by trimethylation of Lys27 in histone 3 (H3K27me3). Given the reported roles of EZH2 in cancer, it is perhaps not surprising that targeting EZH2 in cancer therapy has become a hot research topic. Indeed, different types of EZH2 inhibitors are currently under development and are being evaluated by clinical trials. Recently, Murashima et al. identified NPD13668, a novel EZH2 inhibitor, by using a cell-based high-throughput screening assay. NPD13668 inhibited EZH2 methyltransferase activity, and repressed cell growth in multiple cancer cell lines, indicating a potential role for this compound in cancer treatment. In this review, we will focus on the current knowledge regarding the biological significance of PRC2 and H3K27me, and the recent advances in developing and testing drugs that target PRC2.
Insights
A novel Enhancer of zeste homolog 2 (EZH2) inhibitor, NPD13668, shows promise for cancer therapy by blocking EZH2 activity and inhibiting cancer cell growth. This review covers PRC2, H3K27me, and emerging EZH2-targeted drugs.
Area of Science:
- Epigenetics and Molecular Biology
- Cancer Research
- Pharmacology
Background:
- Enhancer of zeste homolog 2 (EZH2) is the catalytic subunit of Polycomb Repressive Complex 2 (PRC2).
- PRC2 mediates gene repression through histone H3 Lysine 27 trimethylation (H3K27me3).
- EZH2 plays a significant role in various cancers, making it a therapeutic target.
Purpose of the Study:
- To review the biological significance of PRC2 and H3K27me.
- To highlight recent advances in developing drugs targeting PRC2.
- To introduce NPD13668, a novel EZH2 inhibitor.
Main Methods:
- High-throughput screening assay to identify EZH2 inhibitors.
- In vitro assays to assess EZH2 methyltransferase activity.
- Cell-based assays to evaluate cell growth inhibition in cancer lines.
Main Results:
- Identification of NPD13668 as a novel EZH2 inhibitor.
- NPD13668 demonstrated inhibition of EZH2 methyltransferase activity.
- NPD13668 repressed proliferation in multiple cancer cell lines.
Conclusions:
- NPD13668 shows potential as a therapeutic agent for cancer treatment.
- Targeting EZH2 is a promising strategy in oncology.
- Further development and clinical evaluation of EZH2 inhibitors are warranted.
More Related Videos
07:48Utilizing Functional Genomics Screening to Identify Potentially Novel Drug Targets in Cancer Cell Spheroid Cultures
Published on: December 26, 2016
10:27Testing Targeted Therapies in Cancer using Structural DNA Alteration Analysis and Patient-Derived Xenografts
Published on: July 25, 2020
Related Concept Videos
02:57Targeted Cancer Therapies
There are several types of targeted therapies against...
02:38Mitogens and the Cell Cycle
02:49Cancer Therapies
However, cancer treatments can pose several challenges, as therapies used to kill cancer cells are generally also toxic to normal cells. Moreover, cancer cells mutate rapidly and can develop resistance to chemical agents or radiation therapy. Besides, all types of cancer cells may not respond to the same therapy. Some cancer cells respond to one...
02:50Combination 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...
02:34Inhibition of Cdk Activity