Zijun Chen
Novartis
6 Papers
7 Citations
Zijun Chen is an academic researcher from Novartis. The author has contributed to research in topics: EZH2 & Allosteric regulation. The author has an hindex of 2, co-authored 5 publications.
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Papers
Selective inhibition of Ezh2 by a small molecule inhibitor blocks tumor cells proliferation
Wei Qi,Ho Man Chan,Lin Teng,Ling Li,Shannon Chuai,Ruipeng Zhang,Jue Zeng,Min Li,Hong Fan,Ying Lin,Justin Gu,Ophelia Ardayfio,Ji-Hu Zhang,Xiaoxia Yan,Jialuo Fang,Yuan Mi,Man Zhang,Tao Zhou,Grace Feng,Zijun Chen,Guobin Li,Teddy T.C. Yang,Kehao Zhao,Xianghui Liu,Zhengtian Yu,Chris Lu,Peter Atadja,En Li +27 more
TL;DR: A potent and selective small molecule inhibitor, EI1, is developed, which inhibits the enzymatic activity of Ezh2 through direct binding to the enzyme and competing with the methyl group donor S-Adenosyl methionine, providing strong validation of EzH2 as a potential therapeutic target for the treatment of cancer.
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An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED
Wei Qi,Kehao Zhao,Justin Gu,Ying Huang,Youzhen Wang,Hailong Zhang,Man Zhang,Jeff Zhang,Zhengtian Yu,Ling Li,Lin Teng,Shannon Chuai,Chao Zhang,Mengxi Zhao,Ho Man Chan,Zijun Chen,Douglas Fang,Qi Fei,Leying Feng,Lijian Feng,Yuan Gao,Hui Ge,Xinjian Ge,Guobin Li,Andreas Lingel,Ying Lin,Yueqin Liu,Fangjun Luo,Minlong Shi,Long Wang,Zhaofu Wang,Yanyan Yu,Jue Zeng,Chenhui Zeng,Lijun Zhang,Qiong Zhang,Shaolian Zhou,Counde Oyang,Peter Atadja,En Li +39 more
TL;DR: EED226 is reported, a potent and selective PRC2 inhibitor that directly binds to the H3K27me3 binding pocket of EED, and shows similar activity to SAM-competitive inhibitors in blocking H 3K27 methylation ofPRC2 target genes and inducing regression of human lymphoma xenograft tumors.
301
Discovery of the Clinical Candidate MAK683: An EED-Directed, Allosteric, and Selective PRC2 Inhibitor for the Treatment of Advanced Malignancies.
Ying Huang,Martin Sendzik,Jeff Zhang,Zhenting Gao,Yongfeng Sun,Long Wang,Justin Gu,Kehao Zhao,Zhengtian Yu,Lijun Zhang,Qiong Zhang,Joachim Blanz,Zijun Chen,Valerie Dubost,Douglas D. Fang,Li-Shi Feng,Xingnian Fu,Michael Kiffe,Ling Li,Fang Luo,Xiao Luo,Yuan Mi,Prakash Mistry,David Pearson,Alessandro Piaia,Clemens Scheufler,Rémi Terranova,Andreas Weiss,Jue Zeng,Hailong Zhang,Mengxi Zhao,Michael Patrick Dillon,Sébastien Jeay,Wei Qi,Jonathan G. Moggs,Carole Pissot-Soldermann,En Li,Peter Atadja,Andreas Lingel,Counde Oyang +39 more
TL;DR: The stepwise optimization of the tool compound EED226 toward the potent and selective EED inhibitor MAK683 (compound 22) and its subsequent preclinical characterization are reported, based on a balanced PK/PD profile, efficacy, and mitigated risk of forming reactive metabolites, which has been selected for clinical development.
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Split luciferase-based biosensors for characterizing EED binders.
Ling Li,Lijian Feng,Minlong Shi,Jue Zeng,Zijun Chen,Li Zhong,Li Huang,Weihui Guo,Ying Huang,Wei Qi,Chris Lu,En Li,Kehao Zhao,Justin Gu +13 more
TL;DR: Based on the crystal structure, the DSF data as well as the biosensor assay data, it's most likely that compound-induced increase in the luciferase activity of the EED[G255D] biosensor results from the decreased non-productive interactions between the Eed subdomain and other subdomains within the bios sensor construct.
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Patent
Antibodies targeting bone morphogenetic protein 9 (bmp9) and methods therefor
Zijun Chen,Sujun Deng,Yun He,Dagang Huang,Markus Kugler,Qian Li,Chris Lu,Xiao Luo,Yongqiang Shan,Kathrin Ulrike Tissot-Daguette,Jing Wu +10 more
- 26 May 2016
TL;DR: The present invention relates to isolated antibodies and antigen-binding fragments thereof which bind human BMP9 and compositions and methods of use thereof as mentioned in this paper, and is related to the present invention.
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