PreprintCited by 897Epigenetics and DNA MethylationChromatin Remodeling and CancerGenomics and Chromatin Dynamics

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Pharmacologic disruption of Polycomb-repressive complex 2-mediated gene repression selectively induces apoptosis in cancer cells

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Tan, Jing, Yang, Xiaojing, Zhuang, Li, Jiang, Xia, Chen, Wei, Lee, Puay Leng, Karuturi, R.K. Murthy, Tan, Patrick Boon Ooi, Liu, Edison T., Yu, Qiang·2007·Genes & Development

DOI 10.1101/gad.1524107PMC PMC1855231

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Abstract

Polycomb-repressive complex 2 (PRC2)-mediated histone methylation plays an important role in aberrant cancer gene silencing and is a potential target for cancer therapy. Here we show that S-adenosylhomocysteine hydrolase inhibitor 3-Deazaneplanocin A (DZNep) induces efficient apoptotic cell death in cancer cells but not in normal cells. We found that DZNep effectively depleted cellular levels of PRC2 components EZH2, SUZ12, and EED and inhibited associated histone H3 Lys 27 methylation (but not H3 Lys 9 methylation). By integrating RNA interference (RNAi), genome-wide expression analysis, and chromatin immunoprecipitation (ChIP) studies, we have identified a prominent set of genes selectively repressed by PRC2 in breast cancer that can be reactivated by DZNep. We further demonstrate that the preferential reactivation of a set of these genes by DZNep, including a novel apoptosis affector, FBXO32 , contributes to DZNep-induced apoptosis in breast cancer cells. Our results demonstrate the unique feature of DZNep as a novel chromatin remodeling compound and suggest that pharmacologic reversal of PRC2-mediated gene repression by DZNep may constitute a novel approach for cancer therapy.

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1 retracted

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“In contrast, histone H3 trimethylation at Lys 9 (H3-K9me3)—which is mediated by another histone MTase, Suv39h1 (Rea et al. 2000; Peters et al. 2001; Lehnertz et al. 2003)—was not affected by DZNep treatment.”
Background
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Self-citation

Authors: Tan, J., Yang, X., Zhuang, L., Jiang, X., Chen, W., Lee, P. L., Karuturi, R. K. M., Tan, P. B. O., Liu, E. T., & Yu, Q.
Affiliations: Genome Institute of Singapore (SG)
Chinese Academy of Medical Sciences & Peking Union Medical College (CN)
Duke-NUS Medical School (SG)
ORCID: Tan, Jing
Yang, Xiaojing
Zhuang, Li
Jiang, Xia
Chen, Wei
Lee, Puay Leng
Karuturi, R.K. Murthy
Liu, Edison T.
Yu, Qiang
Venue: Genes & Development
Publisher: Cold Spring Harbor Laboratory
Published: 2007-04-16
Volume: 21
Issue: 9
Pages: 1050-1063
ISSN: 0890-9369 (ISSN-L)
1549-5477
DOI: 10.1101/gad.1524107
PMC: PMC1855231
OpenAlex: W2113634596
Cited by: 895
References: 68
Citations by year: 2026: 12 · 2025: 16 · 2024: 18 · 2023: 35 · 2022: 21 · 2021: 35 · 2020: 39 · 2019: 37 · 2018: 44 · 2017: 65 · 2016: 55 · 2015: 65 · 2014: 98 · 2013: 77 · 2012: 70
Type: posted content
Language: en
Open access: bronze
doi.org
Locations: Genes & Development (publishedVersion)
PubMed Central (publishedVersion)
PubMed (publishedVersion)
National University of Singapore (submittedVersion)
Funders: Agency for Science, Technology and Research
National Cancer Institute
Topics: Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Epigenetics and DNA Methylation
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Chromatin Remodeling and Cancer
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Genomics and Chromatin Dynamics
Keywords: polycomb repressive complex 2, DZNep, EZH2, SUZ12, EED, histone H3 lysine 27 methylation, gene silencing, apoptosis, breast cancer, atrogin-1, chromatin remodeling, cancer therapy
MeSH terms: Adenosine, Base Sequence, Breast Neoplasms, Enzyme Inhibitors, Female, Histones, Humans, Methylation, Promoter Regions, Genetic, Repressor Proteins, RNA Polymerase II, Apoptosis, RNA Interference, RNA, Small Interfering, Chromatin Assembly and Disassembly, Adenosylhomocysteinase, Epigenesis, Genetic, Cell Line, Tumor, Chromatin Immunoprecipitation, Polycomb-Group Proteins

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Pharmacologic disruption of Polycomb-repressive complex 2-mediated gene repression selectively induces apoptosis in cancer cells

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