Z
Zhaofu Wang
Researcher at Novartis
Publications - 5
Citations - 583
Zhaofu Wang is an academic researcher from Novartis. The author has contributed to research in topics: Uncompetitive inhibitor & Allosteric regulation. The author has an hindex of 5, co-authored 5 publications receiving 465 citations.
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Journal ArticleDOI
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.
Journal ArticleDOI
Global chromatin profiling reveals NSD2 mutations in pediatric acute lymphoblastic leukemia
Jacob D. Jaffe,Yan Wang,Ho Man Chan,Jinghui Zhang,Robert Huether,Gregory V. Kryukov,Gregory V. Kryukov,Gregory V. Kryukov,Hyo-eun C. Bhang,Jordan E. Taylor,Min Hu,Nathan P. Englund,Feng Yan,Zhaofu Wang,E. Robert McDonald,Lei Wei,Jing Ma,John Easton,Zhengtian Yu,Rosalie deBeaumount,Veronica Gibaja,Kavitha Venkatesan,Robert Schlegel,William R. Sellers,Nicholas Keen,Jun Liu,Giordano Caponigro,Jordi Barretina,Vesselina G. Cooke,Charles G. Mullighan,Steven A. Carr,James R. Downing,Levi A. Garraway,Levi A. Garraway,Frank Stegmeier +34 more
TL;DR: In this article, a high-information-content mass spectrometry approach was developed to profile global histone modifications in human cancers. When applied to 115 lines from the Cancer Cell Line Encyclopedia1, this approach identified distinct molecular chromatin signatures.
Journal ArticleDOI
NSD2 Is Recruited through Its PHD Domain to Oncogenic Gene Loci to Drive Multiple Myeloma
Zheng Huang,Haiping Wu,Shannon Chuai,Fiona Xu,Feng Yan,Nathan P. Englund,Zhaofu Wang,Hailong Zhang,Ming Fang,Youzhen Wang,Justin Gu,Man Zhang,Teddy Yang,Kehao Zhao,Yanyan Yu,Jingquan Dai,Wei Yi,Shaolian Zhou,Qian Li,Jing Wu,Jun Liu,Xu Wu,Ho Man Chan,Chris Lu,Peter Atadja,En Li,Yan Wang,Min Hu +27 more
TL;DR: It is shown that N SD2 methyltransferase activity is crucial for clonogenicity, adherence, and proliferation of multiple myeloma cells on bone marrow stroma in vitro and that NSD2 is required for tumorigenesis of t(4;14)+ but not t( 4;14)- multiple myELoma cells in vivo.
Journal ArticleDOI
Upregulation of CD11b and CD86 through LSD1 inhibition promotes myeloid differentiation and suppresses cell proliferation in human monocytic leukemia cells
Jianwu Fang,Jianwu Fang,Haiyan Ying,Ting Mao,Yanjia Fang,Yuan Lu,He Wang,Irene Zang,Zhaofu Wang,Ying Lin,Mengxi Zhao,Xiao Luo,Zongyao Wang,Yan Zhang,Chao Zhang,Wei Xiao,Yan Wang,Wei Tan,Zhui Chen,Chris Lu,Peter Atadja,En Li,Kehao Zhao,Jianfeng Liu,Justin Gu +24 more
TL;DR: It is reported that small hairpin RNA mediated LSD1 inhibition causes a remarkable transcriptional activation of myeloid lineage marker genes (CD11b/ITGAM and CD86), reduction of cell proliferation and decrease of clonogenic ability of human AML cells.
Journal ArticleDOI
Detecting S-adenosyl-L-methionine-induced conformational change of a histone methyltransferase using a homogeneous time-resolved fluorescence-based binding assay.
Ying Lin,Hong Fan,Mathias Frederiksen,Kehao Zhao,Lei Jiang,Zhaofu Wang,Shaolian Zhou,Weihui Guo,Jun Gao,Shu Li,Edmund Harrington,Peter Meier,Clemens Scheufler,Yao-Chang Xu,Peter Atadja,Chris Lu,En Li,X. Justin Gu +17 more
TL;DR: The G9a-CJP702 binding assay not only can be used to characterize the peptide-pocket inhibitors but also can detect the subtle conformational differences induced by the binding of different SAM-pocket compounds.