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Guoquan Wan, Huan Feng, Chang Su, Yongxia Zhu, Lidan Zhang, Qiangsheng Zhang & Luoting Yu. (2023) A patent review of EZH2 inhibitors from 2017 and beyond. Expert Opinion on Therapeutic Patents 33:4, pages 293-308.
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Milly Dockerill, Clare Gregson & Daniel H. O’ Donovan. (2021) Targeting PRC2 for the treatment of cancer: an updated patent review (2016 - 2020). Expert Opinion on Therapeutic Patents 31:2, pages 119-135.
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Nitya Gulati, Wendy Béguelin & Lisa Giulino-Roth. (2018) Enhancer of zeste homolog 2 (EZH2) inhibitors. Leukemia & Lymphoma 59:7, pages 1574-1585.
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Articles from other publishers (31)
Sunkyu Kim, Natalie Barkey, Onur Atasoylu & Dashyant Dhanak. 2023. Epigenetic Cancer Therapy. Epigenetic Cancer Therapy
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Margarita E. Neganova, Sergey G. Klochkov, Yulia R. Aleksandrova & Gjumrakch Aliev. (2022) Histone modifications in epigenetic regulation of cancer: Perspectives and achieved progress. Seminars in Cancer Biology 83, pages 452-471.
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Samir H. Barghout, Raquel Arminda Carvalho Machado & Dalia Barsyte-Lovejoy. (2022) Chemical biology and pharmacology of histone lysine methylation inhibitors. Biochimica et Biophysica Acta (BBA) - Gene Regulatory Mechanisms 1865:6, pages 194840.
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Juan Xia, Jingyi Li, Lei Tian, Xiaodong Ren, Chang Liu & Chengyuan Liang. (2022) Targeting Enhancer of Zeste Homolog 2 for the Treatment of Hematological Malignancies and Solid Tumors: Candidate Structure–Activity Relationships Insights and Evolution Prospects. Journal of Medicinal Chemistry 65:10, pages 7016-7043.
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Sepideh Mirzaei, Mohammad Hossein Gholami, Kiavash Hushmandi, Farid Hashemi, Amirhossein Zabolian, Israel Canadas, Ali Zarrabi, Noushin Nabavi, Amir Reza Aref, Francesco Crea, Yuzhuo Wang, Milad Ashrafizadeh & Alan Prem Kumar. (2022) The long and short non-coding RNAs modulating EZH2 signaling in cancer. Journal of Hematology & Oncology 15:1.
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Kai-Lu Liu, Kongkai Zhu & Hua Zhang. (2022) An overview of the development of EED inhibitors to disable the PRC2 function. RSC Medicinal Chemistry 13:1, pages 39-53.
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Shasha Cheng, Guan-Jun Yang, Wanhe Wang, Ying-Qi Song, Chung-Nga Ko, Quanbin Han, Dik-Lung Ma & Chung-Hang Leung. (2022) Identification of a cytisine-based EED-EZH2 protein-protein interaction inhibitor preventing metastasis in triple-negative breast cancer cells. Acta Materia Medica 1:2.
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Ruhul Amin, Anjali Shukla, Jacqueline Jufen Zhu, Sohyoung Kim, Ping Wang, Simon Zhongyuan Tian, Andy D. Tran, Debasish Paul, Steven D. Cappell, Sandra Burkett, Huaitian Liu, Maxwell P. Lee, Michael J. Kruhlak, Jennifer E. Dwyer, R. Mark Simpson, Gordon L. Hager, Yijun Ruan & Kent W. Hunter. (2021) Nuclear pore protein NUP210 depletion suppresses metastasis through heterochromatin-mediated disruption of tumor cell mechanical response. Nature Communications 12:1.
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Sharan K. Bagal, Clare Gregson, Daniel H. O’ Donovan, Kurt G. Pike, Andrew Bloecher, Peter Barton, Alexandra Borodovsky, Erin Code, Shaun M. Fillery, Jessie Hao-Ru Hsu, Sameer P. Kawatkar, Chengzhi Li, David Longmire, Youfeng Nai, Samuel C. Nash, Andrew Pike, James Robinson, Jon A. Read, Phillip B. Rawlins, Minhui Shen, Jia Tang, Peng Wang, Haley Woods & Beth Williamson. (2021) Diverse, Potent, and Efficacious Inhibitors That Target the EED Subunit of the Polycomb Repressive Complex 2 Methyltransferase. Journal of Medicinal Chemistry 64:23, pages 17146-17183.
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Yusuke Aoki, Yasunori Tome, Qinghong Han, Jun Yamamoto, Kazuyuki Hamada, Noriyuki Masaki, Michael Bouvet, Kotaro Nishida & Robert M. Hoffman. (2021) Histone H3 lysine-trimethylation markers are decreased by recombinant methioninase and increased by methotrexate at concentrations which inhibit methionine-addicted osteosarcoma cell proliferation. Biochemistry and Biophysics Reports 28, pages 101177.
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Yuko Kusakabe, Tetsuhiro Chiba, Motohiko Oshima, Shuhei Koide, Ola Rizq, Kazumasa Aoyama, Junjie Ao, Tatsuya Kaneko, Hiroaki Kanzaki, Kengo Kanayama, Takahiro Maeda, Tomoko Saito, Ryo Nakagawa, Kazufumi Kobayashi, Soichiro Kiyono, Masato Nakamura, Sadahisa Ogasawara, Eiichiro Suzuki, Shingo Nakamoto, Shin Yasui, Rintaro Mikata, Ryosuke Muroyama, Tatsuo Kanda, Hitoshi Maruyama, Jun Kato, Naoya Mimura, Anqi Ma, Jian Jin, Yoh Zen, Masayuki Otsuka, Atsushi Kaneda, Atsushi Iwama & Naoya Kato. (2021) EZH1/2 inhibition augments the anti-tumor effects of sorafenib in hepatocellular carcinoma. Scientific Reports 11:1.
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Yang Li, Gaoxia Yang, Chengcan Yang, Pan Tang, Juncheng Chen, Jifa Zhang, Jie Liu & Liang Ouyang. (2021) Targeting Autophagy-Related Epigenetic Regulators for Cancer Drug Discovery. Journal of Medicinal Chemistry 64:16, pages 11798-11815.
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Jie Zhou, Yang Yang, Yi-Ling Wang, Yue Zhao, Wen-Jing Ye, Si-Yao Deng, Jin-Yi Lang & Shun Lu. (2021) Enhancer of zeste homolog 2 contributes to apoptosis by inactivating janus kinase 2/ signal transducer and activator of transcription signaling in inflammatory bowel disease. World Journal of Gastroenterology 27:22, pages 3073-3084.
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Yong Shang, Chenggui Wu, Qianwen Gao, Chang Liu, Lisha Li, Xinping Zhang, Hong-Gang Cheng, Shanshan Liu & Qianghui Zhou. (2021) Diversity-oriented functionalization of 2-pyridones and uracils. Nature Communications 12:1.
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Daniel H. O' Donovan, Clare Gregson, Martin J. Packer, Ryan Greenwood, Kurt G. Pike, Sameer Kawatkar, Andrew Bloecher, James Robinson, Jon Read, Erin Code, Jessie Hao-Ru Hsu, Minhui Shen, Haley Woods, Peter Barton, Shaun Fillery, Beth Williamson, Philip B. Rawlins & Sharan K. Bagal. (2021) Free energy perturbation in the design of EED ligands as inhibitors of polycomb repressive complex 2 (PRC2) methyltransferase. Bioorganic & Medicinal Chemistry Letters 39, pages 127904.
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Jacob I. Stuckey, Nico R. Cantone, Alexandre Côté, Shilpi Arora, Valerie Vivat, Ashwin Ramakrishnan, Jennifer A. Mertz, Avinash Khanna, Jehrod Brenneman, Victor S. Gehling, Ludivine Moine, Robert J. SimsIIIIII, James E. Audia, Patrick Trojer, Julian R. Levell & Richard T. Cummings. (2021) Identification and characterization of second-generation EZH2 inhibitors with extended residence times and improved biological activity. Journal of Biological Chemistry 296, pages 100349.
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Yan Zhou, Dao‐Hai Du, Jia Wang, Xiao‐Qing Cai, Alicia X. Deng, Olivier Nosjean, Jean A. Boutin, Pierre Renard, De‐Hua Yang, Cheng Luo & Ming‐Wei Wang. (2020) Identification of catalytic and non‐catalytic activity inhibitors against PRC2‐EZH2 complex through multiple high‐throughput screening campaigns. Chemical Biology & Drug Design 96:4, pages 1024-1051.
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Eswar Shankar, Daniel Franco, Omair Iqbal, Stephen Moreton, Rajnee Kanwal & Sanjay Gupta. (2020) Dual targeting of EZH2 and androgen receptor as a novel therapy for castration-resistant prostate cancer. Toxicology and Applied Pharmacology 404, pages 115200.
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Seok-Jin Kang & Taehoon Chun. (2020) Structural heterogeneity of the mammalian polycomb repressor complex in immune regulation. Experimental & Molecular Medicine 52:7, pages 1004-1015.
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Hope S. Rugo, Ira Jacobs, Shikhar Sharma, Frank Scappaticci, Thomas A. Paul, Kristen Jensen-Pergakes & Gabriel G. Malouf. (2020) The Promise for Histone Methyltransferase Inhibitors for Epigenetic Therapy in Clinical Oncology: A Narrative Review. Advances in Therapy 37:7, pages 3059-3082.
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Shinji Yamazaki, Hovhannes J. Gukasyan, Hui Wang, Sean Uryu & Shikhar Sharma. (2020) Translational Pharmacokinetic-Pharmacodynamic Modeling for an Orally Available Novel Inhibitor of Epigenetic Regulator Enhancer of Zeste Homolog 2. Journal of Pharmacology and Experimental Therapeutics 373:2, pages 220-229.
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Dading Huang, Shuaizhen Tian, Yifei Qi & John Z. H. Zhang. (2020) Binding Modes of Small‐Molecule Inhibitors to the EED Pocket of PRC2. ChemPhysChem 21:3, pages 263-271.
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Daniela Tomaselli, Alessia Lucidi, Dante Rotili & Antonello Mai. (2019) Epigenetic polypharmacology: A new frontier for epi‐drug discovery. Medicinal Research Reviews 40:1, pages 190-244.
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Kanchan Kumari, Biswajit Das, Amit K. Adhya, Arabinda K. Rath & Sandip K. Mishra. (2019) Genome-wide expression analysis reveals six contravened targets of EZH2 associated with breast cancer patient survival. Scientific Reports 9:1.
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Sofia Genta, Maria Cristina Pirosa & Anastasios Stathis. (2019) BET and EZH2 Inhibitors: Novel Approaches for Targeting Cancer. Current Oncology Reports 21:2.
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Giulia Stazi, Clemens Zwergel & Sergio Valente. 2020. Chemical Epigenetics. Chemical Epigenetics
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Gan Zhang, Flavia Barragan, Khadija Wilson, Nissim Levy, Adam Herskovits, Milana Sapozhnikov, Yoel Rodríguez, Leutrim Kelmendi, Haleem Alkasimi, Hunter Korsmo, Maisha Chowdhury & Guillermo Gerona‐Navarro. (2018) A Solid‐Phase Approach to Accessing Bisthioether‐Stapled Peptides Resulting in a Potent Inhibitor of PRC2 Catalytic Activity. Angewandte Chemie International Edition 57:52, pages 17073-17078.
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Gan Zhang, Flavia Barragan, Khadija Wilson, Nissim Levy, Adam Herskovits, Milana Sapozhnikov, Yoel Rodríguez, Leutrim Kelmendi, Haleem Alkasimi, Hunter Korsmo, Maisha Chowdhury & Guillermo Gerona‐Navarro. (2018) A Solid‐Phase Approach to Accessing Bisthioether‐Stapled Peptides Resulting in a Potent Inhibitor of PRC2 Catalytic Activity. Angewandte Chemie 130:52, pages 17319-17324.
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Andrea Di Pietro & Kim L. Good-Jacobson. (2018) Disrupting the Code: Epigenetic Dysregulation of Lymphocyte Function during Infectious Disease and Lymphoma Development. The Journal of Immunology 201:4, pages 1109-1118.
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David Roquis, Aaron Taudt, Kathrin K. Geyer, Gilda Padalino, Karl F. Hoffmann, Nancy Holroyd, Matt Berriman, Benoît Aliaga, Cristian Chaparro, Christoph Grunau & Ronaldo de Carvalho Augusto. (2018) Histone methylation changes are required for life cycle progression in the human parasite Schistosoma mansoni. PLOS Pathogens 14:5, pages e1007066.
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Biao Lu, Xiaodong Shen, Lei Zhang, Dong Liu, Caihua Zhang, Jingsong Cao, Ru Shen, Jiayin Zhang, Dan Wang, Hong Wan, Zhibin Xu, Ming-Hsun Ho, Minsheng Zhang, Lianshan Zhang, Feng He & Weikang Tao. (2018) Discovery of EBI-2511: A Highly Potent and Orally Active EZH2 Inhibitor for the Treatment of Non-Hodgkin’s Lymphoma. ACS Medicinal Chemistry Letters 9:2, pages 98-102.
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