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Updated: Aug 14, 2025

ATAC-Seq Optimization for Cancer Epigenetics Research
Published on: June 30, 2022
ATPase family AAA domain-containing protein 2 (ATAD2): From an epigenetic modulator to cancer therapeutic target
Jiahui Fu1,2, Jin Zhang3, Xiya Chen1,3
1School of Pharmaceutical Sciences, Shenzhen Technology University, Shenzhen, 518118, China.
Abstract:
ATPase family AAA domain-containing protein 2 (ATAD2) has been widely reported to be a new emerging oncogene that is closely associated with epigenetic modifications in human cancers. As a coactivator of transcription factors, ATAD2 can participate in epigenetic modifications and regulate the expression of downstream oncogenes or tumor suppressors, which may be supported by the enhancer of zeste homologue 2. Moreover, the dominant structure (AAA + ATPase and bromine domains) can make ATAD2 a potential therapeutic target in cancer, and some relevant small-molecule inhibitors, such as GSK8814 and AZ13824374, have also been discovered. Thus, in this review, we focus on summarizing the structural features and biological functions of ATAD2 from an epigenetic modulator to a cancer therapeutic target, and further discuss the existing small-molecule inhibitors targeting ATAD2 to improve potential cancer therapy. Together, these inspiring findings would shed new light on ATAD2 as a promising druggable target in cancer and provide a clue on the development of candidate anticancer drugs.
Insights
ATPase family AAA domain-containing protein 2 (ATAD2) is an emerging oncogene involved in epigenetic modifications and cancer. This review highlights ATAD2
Area of Science:
- Molecular Biology
- Epigenetics
- Oncology
Background:
- ATPase family AAA domain-containing protein 2 (ATAD2) is an emerging oncogene implicated in human cancers.
- ATAD2 functions as a transcriptional coactivator involved in epigenetic modifications.
- Its role in regulating oncogenes and tumor suppressors is linked to enhancer of zeste homologue 2 (EZH2).
Purpose of the Study:
- To review the structural features and biological functions of ATAD2.
- To discuss ATAD2's role as an epigenetic modulator and a cancer therapeutic target.
- To summarize small-molecule inhibitors targeting ATAD2 for improved cancer therapy.
Main Methods:
- Literature review summarizing existing research on ATAD2.
- Analysis of ATAD2's structural domains (AAA+ ATPase and bromine domains).
- Discussion of identified small-molecule inhibitors (e.g., GSK8814, AZ13824374).
Main Results:
- ATAD2's structure makes it a viable therapeutic target in cancer.
- Several small-molecule inhibitors targeting ATAD2 have been identified.
- ATAD2's function as an epigenetic modulator is crucial in cancer development.
Conclusions:
- ATAD2 is a promising druggable target for cancer therapy.
- Targeting ATAD2 with small-molecule inhibitors could lead to novel anticancer drugs.
- Further research into ATAD2 inhibitors may improve potential cancer treatments.
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