Polycomb repressive complex 2 (PRC2) is the epigenetic regulator that induces histone H3
lysine 27 methylation (H3K27me3) and silences specific gene transcription. Enhancer of
zeste homolog 2 (EZH2) is an enzymatic subunit of PRC2, and evidence shows that EZH2
plays an essential role in cancer initiation, development, progression, metastasis, and drug
resistance. EZH2 expression is indeed regulated by various oncogenic transcription factors,
tumor suppressor miRNAs, and cancer-associated non-coding RNA. EZH2 activity is also
controlled by post-translational modifications, which are deregulated in cancer. The canonical
role of EZH2 is gene silencing through H3K27me3, but accumulating evidence shows
that EZH2 methlyates substrates other than histone and has methylase-independent
functions. These non-canonical functions of EZH2 are shown to play a role in cancer
progression. In this review, we summarize current information on the regulation and roles
of EZH2 in cancer. We also discuss various therapeutic approaches to targeting EZH2.
Citations
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Cancer Stem Cell Plasticity – A Deadly Deal Archana P. Thankamony, Kritika Saxena, Reshma Murali, Mohit Kumar Jolly, Radhika Nair Frontiers in Molecular Biosciences.2020;[Epub] CrossRef
Acquired resistance to DZNep-mediated apoptosis is associated with copy number gains of AHCY in a B-cell lymphoma model Chidimma Agatha Akpa, Karsten Kleo, Elisabeth Oker, Nancy Tomaszewski, Clemens Messerschmidt, Cristina López, Rabea Wagener, Kathrin Oehl-Huber, Katja Dettmer, Anne Schoeler, Dido Lenze, Peter J. Oefner, Dieter Beule, Reiner Siebert, David Capper, Lora Di BMC Cancer.2020;[Epub] CrossRef
Long noncoding RNA ANRIL promotes the malignant progression of cholangiocarcinoma by epigenetically repressing ERRFI1 expression Yang Yu, Qiaoyu Chen, Xunlei Zhang, Jian Yang, Kaibo Lin, Congfei Ji, Aibing Xu, Lei Yang, Lin Miao Cancer Science.2020; 111(7): 2297. CrossRef
CAMK2A supported tumor initiating cells of lung adenocarcinoma by upregulating SOX2 through EZH2 phosphorylation Si-Qi Wang, Jing Liu, Jing Qin, Yun Zhu, Vicky Pui-Chi Tin, Judy Wai Ping Yam, Maria Pik Wong, Zhi-Jie Xiao Cell Death & Disease.2020;[Epub] CrossRef
INI-1 (SMARCB1)–Deficient Undifferentiated Sinonasal Carcinoma: Novel Paradigm of Molecular Testing in the Diagnosis and Management of Sinonasal Malignancies Khvaramze Shaverdashvili, Elham Azimi-Nekoo, Perry Cohen, Nadeem Akbar, Thomas J. Ow, Balazs Halmos, Enrico Castellucci The Oncologist.2020; 25(9): 738. CrossRef
Genomic profiling in renal cell carcinoma Nazli Dizman, Errol J. Philip, Sumanta K. Pal Nature Reviews Nephrology.2020; 16(8): 435. CrossRef
The Roles of the Histone Protein Modifier EZH2 in the Uterus and Placenta Ana M. Mesa, Cheryl S. Rosenfeld, Geetu Tuteja, Theresa I. Medrano, Paul S. Cooke Epigenomes.2020; 4(3): 20. CrossRef
FOXC1-mediated LINC00301 facilitates tumor progression and triggers an immune-suppressing microenvironment in non-small cell lung cancer by regulating the HIF1α pathway Cheng-Cao Sun, Wei Zhu, Shu-Jun Li, Wei Hu, Jian Zhang, Yue Zhuo, Han Zhang, Juan Wang, Yu Zhang, Shao-Xin Huang, Qi-Qiang He, De-Jia Li Genome Medicine.2020;[Epub] CrossRef
The long non‐coding RNA SNHG1 promotes bladder cancer progression by interacting with miR‐143‐3p and EZH2 Wei Xiang, Lei Lyu, Tao Huang, Fuxin Zheng, Jingdong Yuan, Chuanhua Zhang, Guosong Jiang Journal of Cellular and Molecular Medicine.2020; 24(20): 11858. CrossRef
Elevated expression of RUNX3 co-expressing with EZH2 in esophageal cancer patients from India Asad Ur Rehman, Mohammad Askandar Iqbal, Real Sumayya Abdul Sattar, Snigdha Saikia, Mohammad Kashif, Wasif Mohammad Ali, Subhash Medhi, Sundeep Singh Saluja, Syed Akhtar Husain Cancer Cell International.2020;[Epub] CrossRef
MicroRNA-33b Suppresses Epithelial–Mesenchymal Transition Repressing the MYC–EZH2 Pathway in HER2+ Breast Carcinoma Birlipta Pattanayak, Iris Garrido-Cano, Anna Adam-Artigues, Eduardo Tormo, Begoña Pineda, Paula Cabello, Elisa Alonso, Begoña Bermejo, Cristina Hernando, María Teresa Martínez, Ana Rovira, Joan Albanell, Federico Rojo, Octavio Burgués, Juan Miguel Cejalvo Frontiers in Oncology.2020;[Epub] CrossRef
Inhibition of EZH2 via the STAT3/HOTAIR signalling axis contributes to cell cycle arrest and apoptosis induced by polyphyllin I in human non-small cell lung cancer cells Hok Shing Li, Yao Xu Steroids.2020; 164: 108729. CrossRef
EZH2 overexpression dampens tumor-suppressive signals via an EGR1 silencer to drive breast tumorigenesis Xiaowen Guan, Houliang Deng, Un Lam Choi, Zhengfeng Li, Yiqi Yang, Jianming Zeng, Yunze Liu, Xuanjun Zhang, Gang Li Oncogene.2020; 39(48): 7127. CrossRef
RETRACTED: Exosome-Delivered LncHEIH Promotes Gastric Cancer Progression by Upregulating EZH2 and Stimulating Methylation of the GSDME Promoter Yan Lu, Kaiqing Hou, Mengsen Li, Xiaobin Wu, Shaochun Yuan Frontiers in Cell and Developmental Biology.2020;[Epub] CrossRef
Impact of the Tumor Microenvironment on Tumor Heterogeneity and Consequences for Cancer Cell Plasticity and Stemness Ralf Hass, Juliane von der Ohe, Hendrik Ungefroren Cancers.2020; 12(12): 3716. CrossRef
The EZH2–PHACTR2–AS1–Ribosome Axis induces Genomic Instability and Promotes Growth and Metastasis in Breast Cancer Wenhui Chu, Xi Zhang, Lihua Qi, Yenan Fu, Peng Wang, Wei Zhao, Juan Du, Jing Zhang, Jun Zhan, Yunling Wang, Wei-Guo Zhu, Yu Yu, Hongquan Zhang Cancer Research.2020; 80(13): 2737. CrossRef
Inhibition of EZH2 Enhances the Antitumor Efficacy of Metformin in Prostate Cancer Yifan Kong, Yanquan Zhang, Fengyi Mao, Zhuangzhuang Zhang, Zhiguo Li, Ruixin Wang, Jinghui Liu, Xiaoqi Liu Molecular Cancer Therapeutics.2020; 19(12): 2490. CrossRef
Aberrant differential expression of EZH2 and H3K27me3 in extranodal NK/T-cell lymphoma, nasal type, is associated with disease progression and prognosis Jumei Liu, Li Liang, Sixia Huang, Lin Nong, Dong Li, Bo Zhang, Ting Li Human Pathology.2019; 83: 166. CrossRef
Retracted: Long noncoding RNA TALNEC2 plays an oncogenic role in breast cancer by binding to EZH2 to target p57KIP2 and involving in p‐p38 MAPK and NF‐κB pathways Enqi Qiao, Daobao Chen, Qinglin Li, Weiliang Feng, Xingfei Yu, Xiping Zhang, Liang Xia, Ju Jin, Hongjian Yang Journal of Cellular Biochemistry.2019; 120(3): 3978. CrossRef
Interaction of EZH2 and P65 is involved in the arsenic trioxide-induced anti-angiogenesis in human triple-negative breast cancer cells Fei Jiang, Yuan Li, Lu Si, Zengli Zhang, Zhong Li Cell Biology and Toxicology.2019; 35(4): 361. CrossRef
lncRNA SNHG6 regulates EZH2 expression by sponging miR-26a/b and miR-214 in colorectal cancer Mu Xu, Xiaoxiang Chen, Kang Lin, Kaixuan Zeng, Xiangxiang Liu, Xueni Xu, Bei Pan, Tao Xu, Li Sun, Bangshun He, Yuqin Pan, Huiling Sun, Shukui Wang Journal of Hematology & Oncology.2019;[Epub] CrossRef
Genome-wide expression analysis reveals six contravened targets of EZH2 associated with breast cancer patient survival Kanchan Kumari, Biswajit Das, Amit K. Adhya, Arabinda K. Rath, Sandip K. Mishra Scientific Reports.2019;[Epub] CrossRef
LncRNA ADAMTS9-AS2 promotes tongue squamous cell carcinoma proliferation, migration and EMT via the miR-600/EZH2 axis Yingru Li, Quan Wan, Weiwei Wang, Lianxi Mai, Liujuan Sha, Mubarak Mashrah, Zhaoyu Lin, Chaobin Pan Biomedicine & Pharmacotherapy.2019; 112: 108719. CrossRef
New directions in treating peripheral T-cell lymphomas (PTCL): leveraging epigenetic modifiers alone and in combination Helen Ma, Owen A. O’Connor, Enrica Marchi Expert Review of Hematology.2019; 12(3): 137. CrossRef
iPS-Cell Technology and the Problem of Genetic Instability—Can It Ever Be Safe for Clinical Use? Stephen W. Attwood, Michael J. Edel Journal of Clinical Medicine.2019; 8(3): 288. CrossRef
Protein dynamics analysis reveals that missense mutations in cancer‐related genes appear frequently on hinge‐neighboring residues Jan Fehmi Sayılgan, Türkan Haliloğlu, Mehmet Gönen Proteins: Structure, Function, and Bioinformatics.2019; 87(6): 512. CrossRef
Enhancer of Zeste 2 Polycomb Repressive Complex 2 Subunit Is Required for Uterine Epithelial Integrity Xin Fang, Nan Ni, John P. Lydon, Ivan Ivanov, Kayla J. Bayless, Monique Rijnkels, Qinglei Li The American Journal of Pathology.2019; 189(6): 1212. CrossRef
Prolactin Receptor Signaling Regulates a Pregnancy-Specific Transcriptional Program in Mouse Islets Mark E Pepin, Hayden H Bickerton, Maigen Bethea, Chad S Hunter, Adam R Wende, Ronadip R Banerjee Endocrinology.2019; 160(5): 1150. CrossRef
Targeting EZH2 histone methyltransferase activity alleviates experimental intestinal inflammation Jie Zhou, Shuo Huang, Zhongyu Wang, Jiani Huang, Liang Xu, Xuefeng Tang, Yisong Y. Wan, Qi-jing Li, Alistair L. J. Symonds, Haixia Long, Bo Zhu Nature Communications.2019;[Epub] CrossRef
Silencing of microRNA-708 promotes cell growth and epithelial-to-mesenchymal transition by activating the SPHK2/AKT/β-catenin pathway in glioma Yan Chen, Xubin Deng, Weiquan Chen, Pengwei Shi, Mei Lian, Hongxiao Wang, Kewan Wang, Dadi Qian, Dong Xiao, Hao Long Cell Death & Disease.2019;[Epub] CrossRef
EZH2 upregulates the PI3K/AKT pathway through IGF1R and MYC in clinically aggressive chronic lymphocytic leukaemia Subazini Thankaswamy Kosalai, Mohammad Hamdy Abdelrazak Morsy, Nikos Papakonstantinou, Larry Mansouri, Niki Stavroyianni, Chandrasekhar Kanduri, Kostas Stamatopoulos, Richard Rosenquist, Meena Kanduri Epigenetics.2019; 14(11): 1125. CrossRef
Current state of melanoma diagnosis and treatment Lauren E. Davis, Sara C. Shalin, Alan J. Tackett Cancer Biology & Therapy.2019; 20(11): 1366. CrossRef
DZNep-mediated apoptosis in B-cell lymphoma is independent of the lymphoma type, EZH2 mutation status and MYC, BCL2 or BCL6 translocations Chidimma Agatha Akpa, Karsten Kleo, Dido Lenze, Elisabeth Oker, Lora Dimitrova, Michael Hummel, Francesco Bertolini PLOS ONE.2019; 14(8): e0220681. CrossRef
HO-1 promotes resistance to an EZH2 inhibitor through the pRB-E2F pathway: correlation with the progression of myelodysplastic syndrome into acute myeloid leukemia Zhengchang He, Siyu Zhang, Dan Ma, Qin Fang, Liping Yang, Shaoxian Shen, Ying Chen, Lingli Ren, Jishi Wang Journal of Translational Medicine.2019;[Epub] CrossRef
Hematopoietic Differentiation of Human Pluripotent Stem Cells: HOX and GATA Transcription Factors as Master Regulators Khaled Alsayegh, Lorena V. Cortés-Medina, Gerardo Ramos-Mandujano, Heba Badraiq, Mo Li Current Genomics.2019; 20(6): 438. CrossRef
Long non‐coding small nucleolar RNA host genes in digestive cancers Huan Yang, Zheng Jiang, Shuang Wang, Yongbing Zhao, Xiaomei Song, Yufeng Xiao, Shiming Yang Cancer Medicine.2019; 8(18): 7693. CrossRef
Aberrant Expression of EZH2 in Pediatric Patients with Myelodysplastic Syndrome: A Potential Biomarker of Leukemic Evolution Teresa de Souza Fernandez, Tatiana Fonseca Alvarenga, Elaiza Almeida Antônio de Kós, Viviane Lamim Lovatel, Rita de Cássia Tavares, Elaine Sobral da Costa, Cecília de Souza Fernandez, Eliana Abdelhay BioMed Research International.2019; 2019: 1. CrossRef
Epigenetics of Bladder Cancer: Where Biomarkers and Therapeutic Targets Meet Victor G. Martinez, Ester Munera-Maravilla, Alejandra Bernardini, Carolina Rubio, Cristian Suarez-Cabrera, Cristina Segovia, Iris Lodewijk, Marta Dueñas, Mónica Martínez-Fernández, Jesus Maria Paramio Frontiers in Genetics.2019;[Epub] CrossRef
Cigarette smoke affects the onco-suppressor DAB2IP expression in bronchial epithelial cells of COPD patients Giulia Anzalone, Giuseppe Arcoleo, Fabio Bucchieri, Angela M. Montalbano, Roberto Marchese, Giusy D. Albano, Caterina Di Sano, Monica Moscato, Rosalia Gagliardo, Fabio L. M. Ricciardolo, Mirella Profita Scientific Reports.2019;[Epub] CrossRef
Stratifying nonfunctional pituitary adenomas into two groups distinguished by macrophage subtypes Garima Yagnik, Martin J. Rutowski, Sumedh S. Shah, Manish K. Aghi Oncotarget.2019; 10(22): 2212. CrossRef
Genome‑wide analysis reveals the emerging roles of long non‑coding RNAs in cancer (Review) Xiaoxia Ren Oncology Letters.2019;[Epub] CrossRef
EZH2 contributes to the response to PARP inhibitors through its PARP-mediated poly-ADP ribosylation in breast cancer H Yamaguchi, Y Du, K Nakai, M Ding, S-S Chang, J L Hsu, J Yao, Y Wei, L Nie, S Jiao, W-C Chang, C-H Chen, Y Yu, G N Hortobagyi, M-C Hung Oncogene.2018; 37(2): 208. CrossRef
Optimization of Orally Bioavailable Enhancer of Zeste Homolog 2 (EZH2) Inhibitors Using Ligand and Property-Based Design Strategies: Identification of Development Candidate (R)-5,8-Dichloro-7-(methoxy(oxetan-3-yl)methyl)-2-((4-methoxy-6-methyl-2-oxo-1,2-d Pei-Pei Kung, Patrick Bingham, Alexei Brooun, Michael Collins, Ya-Li Deng, Dac Dinh, Connie Fan, Ketan S. Gajiwala, Rita Grantner, Hovhannes J. Gukasyan, Wenyue Hu, Buwen Huang, Robert Kania, Susan E. Kephart, Cody Krivacic, Robert A. Kumpf, Penney Khamph Journal of Medicinal Chemistry.2018; 61(3): 650. CrossRef
Nicotine associated breast cancer in smokers is mediated through high level of EZH2 expression which can be reversed by methyltransferase inhibitor DZNepA Kanchan Kumari, Biswajit Das, Amit Adhya, Sanjib Chaudhary, Shantibhusan Senapati, Sandip K. Mishra Cell Death & Disease.2018;[Epub] CrossRef
Long noncoding RNA GAS5 promotes bladder cancer cells apoptosis through inhibiting EZH2 transcription Miao Wang, Chen Guo, Liang Wang, Gang Luo, Chao Huang, Yawei Li, Dong Liu, Fuqing Zeng, Guosong Jiang, Xingyuan Xiao Cell Death & Disease.2018;[Epub] CrossRef
Valproic Acid Promotes Apoptosis and Cisplatin Sensitivity Through Downregulation of H19 Noncoding RNA in Ovarian A2780 Cells Zahre Sajadpoor, Zeinab Amini-Farsani, Hossein Teimori, Mehdi Shamsara, Mohammad Hossein Sangtarash, Payam Ghasemi-Dehkordi, Farrokh Yadollahi Applied Biochemistry and Biotechnology.2018; 185(4): 1132. CrossRef
Epigenetic dysregulation of key developmental genes in radiation‐induced rat mammary carcinomas Kazuhiro Daino, Mayumi Nishimura, Tatsuhiko Imaoka, Masaru Takabatake, Takamitsu Morioka, Yukiko Nishimura, Yoshiya Shimada, Shizuko Kakinuma International Journal of Cancer.2018; 143(2): 343. CrossRef
The role of enhancer of zeste homolog 2: From viral epigenetics to the carcinogenesis of hepatocellular carcinoma Luca Sanna, Irene Marchesi, Mariarosa A. B. Melone, Luigi Bagella Journal of Cellular Physiology.2018; 233(9): 6508. CrossRef
Decreased expression of microRNA-26b in locally advanced and inflammatory breast cancer Qingqing Ding, Yan Wang, Zhuang Zuo, Yun Gong, Savitri Krishnamurthy, Chia-Wei Li, Yun-Ju Lai, Wei Wei, Jing Wang, Ganiraju C. Manyam, Lixia Diao, Xinna Zhang, Feng Lin, William F. Symmans, Li Sun, Chang-Gong Liu, Xiuping Liu, Bisrat G. Debeb, Naoto T. Ue Human Pathology.2018; 77: 121. CrossRef
EZH2 induces the expression of miR-1301 as a negative feedback control mechanism in triple negative breast cancer Qiuju Wu, Zekun Chen, Guihua Zhang, Wenhui Zhou, You Peng, Rong Liu, Ceshi Chen, Jing Feng Acta Biochimica et Biophysica Sinica.2018; 50(7): 693. CrossRef
Impact of OGT deregulation on EZH2 target genes FOXA1 and FOXC1 expression in breast cancer cells Ewa Forma, Paweł Jóźwiak, Piotr Ciesielski, Agnieszka Zaczek, Katarzyna Starska, Magdalena Bryś, Anna Krześlak, Gokul M. Das PLOS ONE.2018; 13(6): e0198351. CrossRef
Anti-tumor and anti-metastasis activities of honey bee larvae powder by suppressing the expression of EZH2 Masakatsu Kageyama, Kejuan Li, Shuang Sun, Guoqing Xing, Ran Gao, Zhongfang Lei, Zhenya Zhang Biomedicine & Pharmacotherapy.2018; 105: 690. CrossRef
Epigenetic silencing of tumor suppressor gene CDKN1A by oncogenic long non-coding RNA SNHG1 in cholangiocarcinoma Yang Yu, Mingjiong Zhang, Ni Wang, Quanpeng Li, Jian Yang, Shuai Yan, Xuezhi He, Guozhong Ji, Lin Miao Cell Death & Disease.2018;[Epub] CrossRef
Emerging roles of Myc in stem cell biology and novel tumor therapies Go J. Yoshida Journal of Experimental & Clinical Cancer Research.2018;[Epub] CrossRef
The long noncoding RNA SNHG1 regulates colorectal cancer cell growth through interactions with EZH2 and miR-154-5p Mu Xu, Xiaoxiang Chen, Kang Lin, Kaixuan Zeng, Xiangxiang Liu, Bei Pan, Xueni Xu, Tao Xu, Xiuxiu Hu, Li Sun, Bangshun He, Yuqin Pan, Huiling Sun, Shukui Wang Molecular Cancer.2018;[Epub] CrossRef
Long noncoding RNA PCAT6 functions as an oncogene by binding to EZH2 and suppressing LATS2 in non-small-cell lung cancer Xuefei Shi, Zhili Liu, Zhicong Liu, Xueren Feng, Feng Hua, Xixian Hu, Bin Wang, Kaihua Lu, Fengqi Nie EBioMedicine.2018; 37: 177. CrossRef
DUXAP8, a pseudogene derived lncRNA, promotes growth of pancreatic carcinoma cells by epigenetically silencing CDKN1A and KLF2 Yifan Lian, Jiebin Yang, Yikai Lian, Chuangxing Xiao, Xuezhen Hu, Hongzhi Xu Cancer Communications.2018; 38(1): 1. CrossRef
EZH2, HIF-1, and Their Inhibitors: An Overview on Pediatric Cancers Marco Papale, Elisabetta Ferretti, Giuseppe Battaglia, Diana Bellavia, Antonello Mai, Marco Tafani Frontiers in Pediatrics.2018;[Epub] CrossRef
Long Noncoding RNA ANRIL Supports Proliferation of Adult T-Cell Leukemia Cells through Cooperation with EZH2 Zaowen Song, Wencai Wu, Mengyun Chen, Wenzhao Cheng, Juntao Yu, Jinyong Fang, Lingling Xu, Jun-ichirou Yasunaga, Masao Matsuoka, Tiejun Zhao, Viviana Simon Journal of Virology.2018;[Epub] CrossRef
MET/ERK and MET/JNK Pathway Activation Is Involved in BCR-ABL Inhibitor-resistance in Chronic Myeloid Leukemia Masanobu Tsubaki YAKUGAKU ZASSHI.2018; 138(12): 1461. CrossRef
EZH2 inhibitors sensitize myeloma cell lines to panobinostat resulting in unique combinatorial transcriptomic changes Taylor Harding, Jessica Swanson, Brian Van Ness Oncotarget.2018; 9(31): 21930. CrossRef
The untold stories of the speech gene, the FOXP2 cancer gene Maria Jesus Herrero, Yorick Gitton Genes & Cancer.2018; 9(1-2): 11. CrossRef
SKP2 loss destabilizes EZH2 by promoting TRAF6-mediated ubiquitination to suppress prostate cancer W Lu, S Liu, B Li, Y Xie, M G Izban, B R Ballard, S A Sathyanarayana, S E Adunyah, R J Matusik, Z Chen Oncogene.2017; 36(10): 1364. CrossRef
Circ100284, via miR-217 regulation of EZH2, is involved in the arsenite-accelerated cell cycle of human keratinocytes in carcinogenesis Junchao Xue, Yang Liu, Fei Luo, Xiaolin Lu, Hui Xu, Xinlu Liu, Lu Lu, Qianlei Yang, Chao Chen, Weimin Fan, Qizhan Liu Biochimica et Biophysica Acta (BBA) - Molecular Basis of Disease.2017; 1863(3): 753. CrossRef
Regulation of cancer epigenomes with a histone-binding synthetic transcription factor David B. Nyer, Rene M. Daer, Daniel Vargas, Caroline Hom, Karmella A. Haynes npj Genomic Medicine.2017;[Epub] CrossRef
Metastatic biomarkers in synovial sarcoma Rosalia de Necochea-Campion, Lee M. Zuckerman, Hamid R. Mirshahidi, Shahrzad Khosrowpour, Chien-Shing Chen, Saied Mirshahidi Biomarker Research.2017;[Epub] CrossRef
Interplay of DNA methyltransferase 1 and EZH2 through inactivation of Stat3 contributes to β-elemene-inhibited growth of nasopharyngeal carcinoma cells JingJing Wu, Qing Tang, LiJuan Yang, YuQing Chen, Fang Zheng, Swei Sunny Hann Scientific Reports.2017;[Epub] CrossRef
Regulation of the JMJD3 (KDM6B) histone demethylase in glioblastoma stem cells by STAT3 Maureen M. Sherry-Lynes, Sejuti Sengupta, Shreya Kulkarni, Brent H. Cochran, Anita B. Hjelmeland PLOS ONE.2017; 12(4): e0174775. CrossRef
Modulation of HAT activity by the BRCA2 N372H variation is a novel mechanism of paclitaxel resistance in breast cancer cell lines Woo Sun Kwon, Sun Young Rha, Hei-Cheul Jeung, Tae Soo Kim, Hyun Cheol Chung Biochemical Pharmacology.2017; 138: 163. CrossRef
Expression and inhibition of BRD4, EZH2 and TOP2A in neurofibromas and malignant peripheral nerve sheath tumors Azadeh Amirnasr, Rob M. Verdijk, Patricia F. van Kuijk, Walter Taal, Stefan Sleijfer, Erik A. C. Wiemer, Marta M. Alonso PLOS ONE.2017; 12(8): e0183155. CrossRef
Morphoproteomics, E6/E7 in-situ hybridization, and biomedical analytics define the etiopathogenesis of HPV-associated oropharyngeal carcinoma and provide targeted therapeutic options Robert E. Brown, Syed Naqvi, Mary F. McGuire, Jamie Buryanek, Ron J. Karni Journal of Otolaryngology - Head & Neck Surgery.2017;[Epub] CrossRef
Epigenetic Silencing of miRNA-34a in Human Cholangiocarcinoma via EZH2 and DNA Methylation Hyunjoo Kwon, Kyoungsub Song, Chang Han, Jinqiang Zhang, Lu Lu, Weina Chen, Tong Wu The American Journal of Pathology.2017; 187(10): 2288. CrossRef
The role of EZH2 in overall survival of colorectal cancer: a meta-analysis Laura Vilorio-Marqués, Vicente Martín, Cristina Diez-Tascón, María Francisca González-Sevilla, Tania Fernández-Villa, Emiliano Honrado, Veronica Davila-Batista, Antonio J. Molina Scientific Reports.2017;[Epub] CrossRef
Identification of coexistence of BRAF V600E mutation and EZH2 gain specifically in melanoma as a promising target for combination therapy Huan Yu, Meng Ma, Junya Yan, Longwen Xu, Jiayi Yu, Jie Dai, Tianxiao Xu, Huan Tang, Xiaowen Wu, Siming Li, Bin Lian, Lili Mao, Zhihong Chi, Chuanliang Cui, Jun Guo, Yan Kong Journal of Translational Medicine.2017;[Epub] CrossRef
Decreased expression of JMJD3 predicts poor prognosis of patients with clear cell renal cell carcinoma Jiajun Wang, Li Liu, Qilai Long, Qi Bai, Yu Xia, Wei Xi, Jiejie Xu, Jianming Guo Oncology Letters.2017; 14(2): 1550. CrossRef
Contributions of MET activation to BCR-ABL1 tyrosine kinase inhibitor resistance in chronic myeloid leukemia cells Masanobu Tsubaki, Tomoya Takeda, Toshiki Kino, Kazuko Sakai, Tatsuki Itoh, Motohiro Imano, Takashi Nakayama, Kazuto Nishio, Takao Satou, Shozo Nishida Oncotarget.2017; 8(24): 38717. CrossRef
Methylation-mediated silencing of microRNA-211 promotes cell growth and epithelial to mesenchymal transition through activation of the AKT/β-catenin pathway in GBM Weidong Li, Xiaobo Miao, Lingling Liu, Yue Zhang, Xuejun Jin, Xiaojun Luo, Hai Gao, Xubin Deng Oncotarget.2017; 8(15): 25167. CrossRef
Inhibition of enhancer of zeste homolog 2 increases the expression of p16 and suppresses the proliferation and migration of ovarian carcinoma cells in�vitro and in�vivo Fangfang Lu, Hong Xu, Qi Wang, Meiyi Li, Jiahua Meng, Yan Kuang Oncology Letters.2017;[Epub] CrossRef
miR-202 Diminishes TGFβ Receptors and Attenuates TGFβ1-Induced EMT in Pancreatic Cancer Hardik R. Mody, Sau Wai Hung, Rakesh K. Pathak, Jazmine Griffin, Zobeida Cruz-Monserrate, Rajgopal Govindarajan Molecular Cancer Research.2017; 15(8): 1029. CrossRef
TET-Mediated Sequestration of miR-26 Drives EZH2 Expression and Gastric Carcinogenesis Min Deng, Ruixin Zhang, Zhengxi He, Qinwei Qiu, Xihong Lu, Jiang Yin, Hao Liu, Xiaoting Jia, Zhimin He Cancer Research.2017; 77(22): 6069. CrossRef
The role of the polycomb repressive complex pathway in T and NK cell lymphoma: biological and prognostic implications Soo Hee Kim, Woo Ick Yang, Yoo Hong Min, Young Hyeh Ko, Sun Och Yoon Tumor Biology.2016; 37(2): 2037. CrossRef
Interference with endogenous EZH2 reverses the chemotherapy drug resistance in cervical cancer cells partly by up-regulating Dicer expression Liqiong Cai, Zehua Wang, Denghua Liu Tumor Biology.2016; 37(5): 6359. CrossRef
The Ezh2 polycomb group protein drives an aggressive phenotype in melanoma cancer stem cells and is a target of diet derived sulforaphane Matthew L. Fisher, Gautam Adhikary, Dan Grun, David M. Kaetzel, Richard L. Eckert Molecular Carcinogenesis.2016; 55(12): 2024. CrossRef
Problems of glioblastoma multiforme drug resistance A. A. Stavrovskaya, S. S. Shushanov, E. Yu. Rybalkina Biochemistry (Moscow).2016; 81(2): 91. CrossRef
High EZH2 Protein Expression Is Associated with Poor Overall Survival in Patients with Luminal A Breast Cancer Si-Hyong Jang, Jong Eun Lee, Mee-Hye Oh, Ji-Hye Lee, Hyun Deuk Cho, Kyung-Ju Kim, Sung Yong Kim, Sun Wook Han, Han Jo Kim, Sang Byung Bae, Hyun Ju Lee Journal of Breast Cancer.2016; 19(1): 53. CrossRef
Expression of Mirna-26B in the Diagnosis and Prognosis of Patients with Non-Small-Cell Lung Cancer Li-Peng Jiang, Zhi-Tu Zhu, Chun-Yan He Future Oncology.2016; 12(9): 1105. CrossRef
Targeting NK Cells for Anticancer Immunotherapy: Clinical and Preclinical Approaches Sebastian Carotta Frontiers in Immunology.2016;[Epub] CrossRef
Role of EZH2 histone methyltrasferase in melanoma progression and metastasis Fade Mahmoud, Bradley Shields, Issam Makhoul, Laura F. Hutchins, Sara C. Shalin, Alan J. Tackett Cancer Biology & Therapy.2016; 17(6): 579. CrossRef
Prognostic value of UTX expression in patients with clear cell renal cell carcinoma Jiajun Wang, Li Liu, Wei Xi, Qilai Long, Yiwei Wang, Qi Bai, Yu Xia, Jiejie Xu, Jianming Guo Urologic Oncology: Seminars and Original Investigations.2016; 34(8): 338.e19. CrossRef
Squamous Cell Cancers: A Unified Perspective on Biology and Genetics G. Paolo Dotto, Anil K. Rustgi Cancer Cell.2016; 29(5): 622. CrossRef
Genomic and Epigenomic Alterations in Cancer Balabhadrapatruni V.S.K. Chakravarthi, Saroj Nepal, Sooryanarayana Varambally The American Journal of Pathology.2016; 186(7): 1724. CrossRef
Epigenetic mechanisms of cell adhesion-mediated drug resistance in multiple myeloma Yusuke Furukawa, Jiro Kikuchi International Journal of Hematology.2016; 104(3): 281. CrossRef
Down-Regulation of TSLP After EZH2 Silencing in ESCC Cell Line Gholamreza Karami Madani, Abolfazl Rad, Mohammad Mahdi Forghanifard Journal of Biomedicine.2016;[Epub] CrossRef
High EZH2 expression is correlated to metastatic disease in pediatric soft tissue sarcomas Maria Ramaglia, Velia D’Angelo, Adriana Iannotta, Daniela Di Pinto, Elvira Pota, Maria Carmen Affinita, Vittoria Donofrio, Maria Elena Errico, Angela Lombardi, Cristiana Indolfi, Fiorina Casale, Michele Caraglia Cancer Cell International.2016;[Epub] CrossRef
DNA-PK-mediated phosphorylation of EZH2 regulates the DNA damage-induced apoptosis to maintain T-cell genomic integrity Y Wang, H Sun, J Wang, H Wang, L Meng, C Xu, M Jin, B Wang, Y Zhang, Y Zhang, T Zhu Cell Death & Disease.2016; 7(7): e2316. CrossRef
Significance of EZH2 expression in canine mammary tumors Hyun-Ji Choi, Sungwoong Jang, Jae-Eun Ryu, Hyo-Ju Lee, Han-Byul Lee, Woo-Sung Ahn, Hye-Jin Kim, Hyo-Jin Lee, Hee Jin Lee, Gyung-Yub Gong, Woo-Chan Son BMC Veterinary Research.2016;[Epub] CrossRef
Identification of (R)-N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide (CPI-1205), a Potent and Selective Inhibitor of Histone Methyltransferase EZH2, Suitabl Rishi G. Vaswani, Victor S. Gehling, Les A. Dakin, Andrew S. Cook, Christopher G. Nasveschuk, Martin Duplessis, Priyadarshini Iyer, Srividya Balasubramanian, Feng Zhao, Andrew C. Good, Robert Campbell, Christina Lee, Nico Cantone, Richard T. Cummings, Emm Journal of Medicinal Chemistry.2016; 59(21): 9928. CrossRef
MiR-101 Targets the EZH2/Wnt/β-Catenin the Pathway to Promote the Osteogenic Differentiation of Human Bone Marrow-Derived Mesenchymal Stem Cells Hongrui Wang, Yake Meng, Quanjun Cui, Fujun Qin, Haisong Yang, Yu Chen, Yajun Cheng, Jiangang Shi, Yongfei Guo Scientific Reports.2016;[Epub] CrossRef
EZH2 mediates lidamycin-induced cellular senescence through regulating p21 expression in human colon cancer cells Ming-Quan Sha, Xiao-Li Zhao, Liang Li, Li-Hui Li, Yi Li, Tian-Geng Dong, Wei-Xin Niu, Li-Jun Jia, Rong-Guang Shao, Yong-Su Zhen, Zhen Wang Cell Death & Disease.2016; 7(11): e2486. CrossRef
Marginal zone lymphoma-derived interfollicular diffuse large B-cell lymphoma harboring 20q12 chromosomal deletion and missense mutation of BIRC3 gene: a case report Joseph Hatem, April M. Schrank-Hacker, Christopher D. Watt, Jennifer J. D. Morrissette, Adam I. Rubin, Ellen J. Kim, Sunita D. Nasta, Mariusz A. Wasik, Agata M. Bogusz Diagnostic Pathology.2016;[Epub] CrossRef
Expression Profile and Function Analysis of LncRNAs during Priming Phase of Rat Liver Regeneration Jun Li, Wei Jin, Yanli Qin, Weiming Zhao, Cuifang Chang, Cunshuan Xu, Klaus Roemer PLOS ONE.2016; 11(6): e0156128. CrossRef
Non-Canonical EZH2 Transcriptionally Activates RelB in Triple Negative Breast Cancer Cortney L. Lawrence, Albert S. Baldwin, Aamir Ahmad PLOS ONE.2016; 11(10): e0165005. CrossRef
Identification of Polycomb Group Protein EZH2-Mediated DNA Mismatch Repair Gene MSH2 in Human Uterine Fibroids Qiwei Yang, Archana Laknaur, Lelyand Elam, Nahed Ismail, Larisa Gavrilova-Jordan, John Lue, Michael P. Diamond, Ayman Al-Hendy Reproductive Sciences.2016; 23(10): 1314. CrossRef
The relationship between EZH2 expression and microRNA-31 in colorectal cancer and the role in evolution of the serrated pathway Hiroyoshi Kurihara, Reo Maruyama, Kazuya Ishiguro, Shinichi Kanno, Itaru Yamamoto, Keisuke Ishigami, Kei Mitsuhashi, Hisayoshi Igarashi, Miki Ito, Tokuma Tanuma, Yasutaka Sukawa, Kenji Okita, Tadashi Hasegawa, Kohzoh Imai, Hiroyuki Yamamoto, Yasuhisa Shin Oncotarget.2016; 7(11): 12704. CrossRef
The histone methyltransferase EZH2 as a novel prosurvival factor in clinically aggressive chronic lymphocytic leukemia Nikos Papakonstantinou, Stavroula Ntoufa, Elisavet Chartomatsidou, Konstantia Kotta, Andreas Agathangelidis, Lefki Giassafaki, Tzeni Karamanli, Panagiota Bele, Theodoros Moysiadis, Panagiotis Baliakas, Lesley Ann Sutton, Niki Stavroyianni, Achilles Anagno Oncotarget.2016; 7(24): 35946. CrossRef
Proximal and distal regulation of the HYAL1 gene cluster by the estrogen receptor α in breast cancer cells Lydia Edjekouane, Samira Benhadjeba, Maïka Jangal, Hubert Fleury, Nicolas Gévry, Euridice Carmona, André Tremblay Oncotarget.2016; 7(47): 77276. CrossRef
Overexpression of EZH2 is associated with the poor prognosis in osteosarcoma and function analysis indicates a therapeutic potential Ranran Sun, Jacson Shen, Yan Gao, Yubing Zhou, Zujiang Yu, Francis Hornicek, Quancheng Kan, Zhenfeng Duan Oncotarget.2016; 7(25): 38333. CrossRef
GSK3β inactivation promotes the oncogenic functions of EZH2 and enhances methylation of H3K27 in human breast cancers How-Wen Ko, Heng-Huan Lee, Longfei Huo, Weiya Xia, Cheng-Chieh Yang, Jennifer L. Hsu, Long-Yuan Li, Chien-Chen Lai, Li-Chuan Chan, Chien-Chia Cheng, Adam M. Labaff, Hsin-Wei Liao, Seung-Oe Lim, Chia-Wei Li, Yongkun Wei, Lei Nie, Hirohito Yamaguchi, Mien-C Oncotarget.2016; 7(35): 57131. CrossRef
Upregulation of the long noncoding RNA TUG1 promotes proliferation and migration of esophageal squamous cell carcinoma Youtao Xu, Jie Wang, Mantang Qiu, Lei Xu, Ming Li, Feng Jiang, Rong Yin, Lin Xu Tumor Biology.2015; 36(3): 1643. CrossRef
Role of the ubiquitin proteasome system in hematologic malignancies Anagh A. Sahasrabuddhe, Kojo S. J. Elenitoba‐Johnson Immunological Reviews.2015; 263(1): 224. CrossRef
The roles of chromatin-remodelers and epigenetic modifiers in kidney cancer Lili Liao, Joseph R. Testa, Haifeng Yang Cancer Genetics.2015; 208(5): 206. CrossRef
The role of aberrant proteolysis in lymphomagenesis Anagh A. Sahasrabuddhe, Kojo S.J. Elenitoba-Johnson Current Opinion in Hematology.2015; 22(4): 369. CrossRef
Small Molecule Inhibitors of EZH2: the Emerging Translational Landscape Heike Keilhack, Jesse J Smith Epigenomics.2015; 7(3): 337. CrossRef
Enhancer of zeste homolog 2 silencing inhibits tumor growth and lung metastasis in osteosarcoma Yang-Fan Lv, Guang-Ning Yan, Gang Meng, Xi Zhang, Qiao-Nan Guo Scientific Reports.2015;[Epub] CrossRef
Characterization and pharmacologic targeting of EZH2, a fetal retinal protein and epigenetic regulator, in human retinoblastoma Mehnaz Khan, Laura L Walters, Qiang Li, Dafydd G Thomas, Jason M L Miller, Qitao Zhang, Andrew P Sciallis, Yu Liu, Brian J Dlouhy, Patrice E Fort, Steven M Archer, Hakan Demirci, Yali Dou, Rajesh C Rao Laboratory Investigation.2015; 95(11): 1278. CrossRef
Methyltransferase expression and tumor suppressor gene methylation in sporadic and familial colorectal cancer Emmi I. Joensuu, Taina T. Nieminen, Johanna E. Lotsari, Walter Pavicic, Wael M. Abdel‐Rahman, Päivi Peltomäki Genes, Chromosomes and Cancer.2015; 54(12): 776. CrossRef
Phosphorylation-mediated EZH2 inactivation promotes drug resistance in multiple myeloma Jiro Kikuchi, Daisuke Koyama, Taeko Wada, Tohru Izumi, Peter O. Hofgaard, Bjarne Bogen, Yusuke Furukawa Journal of Clinical Investigation.2015; 125(12): 4375. CrossRef
Overexpression of enhancer of zeste homolog 2 (EZH2) characterizes an aggressive subset of prostate cancers and predicts patient prognosis independently from pre- and postoperatively assessed clinicopathological parameters Nathaniel Melling, Erik Thomsen, Maria Christina Tsourlakis, Martina Kluth, Claudia Hube-Magg, Sarah Minner, Christina Koop, Markus Graefen, Hans Heinzer, Corinna Wittmer, Guido Sauter, Waldemar Wilczak, Hartwig Huland, Ronald Simon, Thorsten Schlomm, Ste Carcinogenesis.2015; 36(11): 1333. CrossRef
EZH2 in Bladder Cancer, a Promising Therapeutic Target Mónica Martínez-Fernández, Carolina Rubio, Cristina Segovia, Fernando López-Calderón, Marta Dueñas, Jesús Paramio International Journal of Molecular Sciences.2015; 16(11): 27107. CrossRef
siRNA Silencing EZH2 Reverses Cisplatin-resistance of Human Non-small Cell Lung and Gastric Cancer Cells Wen Zhou, Jian Wang, Wang-Ying Man, Qing-Wei Zhang, Wen-Gui Xu Asian Pacific Journal of Cancer Prevention.2015; 16(6): 2425. CrossRef
H3K27me3 is an Epigenetic Mark of Relevance in Endometriosis Mariano Colón-Caraballo, Janice B. Monteiro, Idhaliz Flores Reproductive Sciences.2015; 22(9): 1134. CrossRef
A Gene Regulatory Program in Human Breast Cancer Renhua Li, John Campos, Joji Iida Genetics.2015; 201(4): 1341. CrossRef
MiR-101 reverses the hypomethylation of the LMO3 promoter in glioma cells Xiaoping Liu, Qianqian Lei, Zhibin Yu, Gang Xu, Hailin Tang, Wei Wang, Zeyou Wang, Guiyuan Li, Minghua Wu Oncotarget.2015; 6(10): 7930. CrossRef
Enhancer of zeste acts as a major developmental regulator ofCiona intestinalisembryogenesis Emilie Le Goff, Camille Martinand-Mari, Marianne Martin, Jérôme Feuillard, Yvan Boublik, Nelly Godefroy, Paul Mangeat, Stephen Baghdiguian, Giacomo Cavalli Biology Open.2015; 4(9): 1109. CrossRef