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Theranostics 2023; 13(2):787-809. doi:10.7150/thno.78840 This issue Cite
Review
1. School of Pharmaceutical Sciences, Shenzhen Technology University, Shenzhen, 518118, China.
2. State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, Sichuan University, Chengdu 610041, China.
3. School of Pharmaceutical Sciences, Medical School, Shenzhen University, Shenzhen 518060, China.
#These authors contributed equally to this work.
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.
Keywords: ATPase family AAA domain-containing protein 2 (ATAD2), Epigenetic modification, Therapeutic target, Small-molecule inhibitor, Cancer therapy, Anticancer drug