Embryonic Ectoderm Development (EED) as a Novel Target for Cancer Treatment

Nicholas       Cook; Jianping       Chen; Jia       Zhou; Daqing       Wu

doi:10.2174/1568026621666210920154942

Abstract

The polycomb repressive complex 2 (PRC2) can methylate at lysine 27 of histone H3 at the trimethylation level (H3K27me3). This leads to gene silencing and is known to be dysregulated in many cancers. PRC2 is made up of three core subunits: EZH2, SUZ12, and EED. EED is essential for the regulation of PRC2 function by binding to H3K27me3. Targeting the allosteric site within EED offers new strategies to disrupt the PRC2 activity. In this minireview, we summarize some of the recent developments in small molecules that target EED and its interaction with other core proteins in the PRC2 complex.

Keywords: PRC2, EED, EZH2, Cancer, Inhibitor, Degrader.

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Current Topics in Medicinal Chemistry

Title:Embryonic Ectoderm Development (EED) as a Novel Target for Cancer Treatment

Volume: 21 Issue: 31

Author(s): Nicholas Cook, Jianping Chen, Jia Zhou and Daqing Wu*

Affiliation:

Department of Biological Sciences, Center for Cancer Research and Therapeutic Development, Clark Atlanta University, Atlanta, GA 30314,United States

Keywords: PRC2, EED, EZH2, Cancer, Inhibitor, Degrader.

Abstract: The polycomb repressive complex 2 (PRC2) can methylate at lysine 27 of histone H3 at the trimethylation level (H3K27me3). This leads to gene silencing and is known to be dysregulated in many cancers. PRC2 is made up of three core subunits: EZH2, SUZ12, and EED. EED is essential for the regulation of PRC2 function by binding to H3K27me3. Targeting the allosteric site within EED offers new strategies to disrupt the PRC2 activity. In this minireview, we summarize some of the recent developments in small molecules that target EED and its interaction with other core proteins in the PRC2 complex.

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Cook Nicholas , Chen Jianping , Zhou Jia and Wu Daqing*, Embryonic Ectoderm Development (EED) as a Novel Target for Cancer Treatment, Current Topics in Medicinal Chemistry 2021; 21 (31) . https://dx.doi.org/10.2174/1568026621666210920154942

DOI https://dx.doi.org/10.2174/1568026621666210920154942	Print ISSN 1568-0266
Publisher Name Bentham Science Publisher	Online ISSN 1873-4294