An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED
Qi, Wei, Zhao, Kehao, Gu, Justin, Huang, Ying, Wang, Youzhen, Zhang, Hailong, Zhang, Man, Zhang, Jeff, Yu, Zhengtian, Li, Ling, Teng, Lin, Chuai, Shannon, Zhang, Chao, Zhao, Mengxi, Chan, HoMan, Chen, Zijun, Fang, Douglas, Fei, Qi, Feng, Leying, Feng, Lijian, Gao, Yuan, Ge, Hui, Ge, Xinjian, Li, Guobin, Lingel, Andreas, Lin, Ying, Liu, Yueqin, Luo, Fangjun, Shi, Minlong, Wang, Long, Wang, Zhaofu, Yu, Yanyan, Zeng, Jue, Zeng, Chenhui, Zhang, Lijun, Zhang, Qiong, Zhou, Shaolian, Oyang, Counde, Atadja, Peter, Li, En
Published in Nature chemical biology (01.04.2017)
Published in Nature chemical biology (01.04.2017)
Get full text
Journal Article
Selective inhibition of Ezh2 by a small molecule inhibitor blocks tumor cells proliferation
Qi, Wei, Chan, HoMan, Tenga, Lin, Li, Ling, Chuai, Shannon, Zhang, Ruipeng, Zeng, Jue, Li, Min, Fan, Hong, Lin, Ying, Gu, Justin, Ardayfio, Ophelia, Zhang, Ji-Hu, Yan, Xiaoxia, Fang, Jialuo, Mi, Yuan, Zhang, Man, Zhou, Tao, Feng, Grace, Chen, Zijun, Li, Guobin, Yang, Teddy, Zhao, Kehao, Liu, Xianghui, Yu, Zhengtian, Lu, Chris X., Atadja, Peter, Li, En
Published in Proceedings of the National Academy of Sciences - PNAS (26.12.2012)
Published in Proceedings of the National Academy of Sciences - PNAS (26.12.2012)
Get full text
Journal Article
Histone Methylation by PRC2 Is Inhibited by Active Chromatin Marks
Schmitges, Frank W., Prusty, Archana B., Faty, Mahamadou, Stützer, Alexandra, Lingaraju, Gondichatnahalli M., Aiwazian, Jonathan, Sack, Ragna, Hess, Daniel, Li, Ling, Zhou, Shaolian, Bunker, Richard D., Wirth, Urs, Bouwmeester, Tewis, Bauer, Andreas, Ly-Hartig, Nga, Zhao, Kehao, Chan, Homan, Gu, Justin, Gut, Heinz, Fischle, Wolfgang, Müller, Jürg, Thomä, Nicolas H.
Published in Molecular cell (06.05.2011)
Published in Molecular cell (06.05.2011)
Get full text
Journal Article
473 LAE113, a novel TIGIT/PVRIG bispecific antibody for the treatment of cancer
Chen, Yan, Li, Xue, Jiang, Ling, Gu, Xiang-Ju Justin
Published in Journal for immunotherapy of cancer (01.11.2023)
Published in Journal for immunotherapy of cancer (01.11.2023)
Get full text
Journal Article
Structure-Guided Design of EED Binders Allosterically Inhibiting the Epigenetic Polycomb Repressive Complex 2 (PRC2) Methyltransferase
Lingel, Andreas, Sendzik, Martin, Huang, Ying, Shultz, Michael D, Cantwell, John, Dillon, Michael P, Fu, Xingnian, Fuller, John, Gabriel, Tobias, Gu, Justin, Jiang, Xiangqing, Li, Ling, Liang, Fang, McKenna, Maureen, Qi, Wei, Rao, Weijun, Sheng, Xijun, Shu, Wei, Sutton, James, Taft, Benjamin, Wang, Long, Zeng, Jue, Zhang, Hailong, Zhang, Maya, Zhao, Kehao, Lindvall, Mika, Bussiere, Dirksen E
Published in Journal of medicinal chemistry (12.01.2017)
Published in Journal of medicinal chemistry (12.01.2017)
Get full text
Journal Article
Discovery and Molecular Basis of a Diverse Set of Polycomb Repressive Complex 2 Inhibitors Recognition by EED
Li, Ling, Zhang, Hailong, Zhang, Man, Zhao, Mengxi, Feng, Lijian, Luo, Xiao, Gao, Zhenting, Huang, Ying, Ardayfio, Ophelia, Zhang, Ji-Hu, Lin, Ying, Fan, Hong, Mi, Yuan, Li, Guobin, Liu, Lei, Feng, Leying, Luo, Fangjun, Teng, Lin, Qi, Wei, Ottl, Johannes, Lingel, Andreas, Bussiere, Dirksen E, Yu, Zhengtian, Atadja, Peter, Lu, Chris, Li, En, Gu, Justin, Zhao, Kehao
Published in PloS one (10.01.2017)
Published in PloS one (10.01.2017)
Get full text
Journal Article
NSD2 Is Recruited through Its PHD Domain to Oncogenic Gene Loci to Drive Multiple Myeloma
ZHENG HUANG, HAIPING WU, GU, Justin, MAN ZHANG, YANG, Teddy, KEHAO ZHAO, YANYAN YU, JINGQUAN DAI, WEI YI, SHAOLIAN ZHOU, QIAN LI, JING WU, SHANNON CHUAI, JUN LIU, XU WU, CHAN, Homan, LU, Chris, ATADJA, Peter, EN LI, YAN WANG, MIN HU, FIONA XU, FENG YAN, ENGLUND, Nathan, ZHAOFU WANG, HAILONG ZHANG, MING FANG, YOUZHEN WANG
Published in Cancer research (Chicago, Ill.) (15.10.2013)
Published in Cancer research (Chicago, Ill.) (15.10.2013)
Get full text
Journal Article
Split luciferase-based biosensors for characterizing EED binders
Li, Ling, Feng, Lijian, Shi, Minlong, Zeng, Jue, Chen, Zijun, Zhong, Li, Huang, Li, Guo, Weihui, Huang, Ying, Qi, Wei, Lu, Chris, Li, En, Zhao, Kehao, Gu, Justin
Published in Analytical biochemistry (01.04.2017)
Published in Analytical biochemistry (01.04.2017)
Get full text
Journal Article
Detecting S-adenosyl-l-methionine-induced conformational change of a histone methyltransferase using a homogeneous time-resolved fluorescence-based binding assay
Lin, Ying, Fan, Hong, Frederiksen, Mathias, Zhao, Kehao, Jiang, Lei, Wang, Zhaofu, Zhou, Shaolian, Guo, Weihui, Gao, Jun, Li, Shu, Harrington, Edmund, Meier, Peter, Scheufler, Clemens, Xu, Yao-Chang, Atadja, Peter, Lu, Chris, Li, En, Justin Gu, X.
Published in Analytical biochemistry (01.04.2012)
Published in Analytical biochemistry (01.04.2012)
Get full text
Journal Article
A liquid chromatography/mass spectrometry-based generic detection method for biochemical assay and hit discovery of histone methyltransferases
Li, Shu, Gu, X. Justin, Hao, Qin, Fan, Hong, Li, Ling, Zhou, Shaolian, Zhao, Kehao, Chan, Ho Man, Wang, Y. Karen
Published in Analytical biochemistry (15.12.2013)
Published in Analytical biochemistry (15.12.2013)
Get full text
Journal Article
Disordered methionine metabolism in MTAP/CDKN2A-deleted cancers leads to dependence on PRMT5
Mavrakis, Konstantinos J., McDonald, E. Robert, Schlabach, Michael R., Billy, Eric, Hoffman, Gregory R., deWeck, Antoine, Ruddy, David A., Venkatesan, Kavitha, Yu, Jianjun, McAllister, Gregg, Stump, Mark, deBeaumont, Rosalie, Ho, Samuel, Yue, Yingzi, Liu, Yue, Yan-Neale, Yan, Yang, Guizhi, Lin, Fallon, Yin, Hong, Gao, Hui, Kipp, D. Randal, Zhao, Songping, McNamara, Joshua T., Sprague, Elizabeth R., Zheng, Bing, Lin, Ying, Cho, Young Shin, Gu, Justin, Crawford, Kenneth, Ciccone, David, Vitari, Alberto C., Lai, Albert, Capka, Vladimir, Hurov, Kristen, Porter, Jeffery A., Tallarico, John, Mickanin, Craig, Lees, Emma, Pagliarini, Raymond, Keen, Nicholas, Schmelzle, Tobias, Hofmann, Francesco, Stegmeier, Frank, Sellers, William R.
Published in Science (American Association for the Advancement of Science) (11.03.2016)
Published in Science (American Association for the Advancement of Science) (11.03.2016)
Get full text
Journal Article
Discovery of First-in-Class, Potent, and Orally Bioavailable Embryonic Ectoderm Development (EED) Inhibitor with Robust Anticancer Efficacy
Huang, Ying, Zhang, Jeff, Yu, Zhengtian, Zhang, Hailong, Wang, Youzhen, Lingel, Andreas, Qi, Wei, Gu, Justin, Zhao, Kehao, Shultz, Michael D, Wang, Long, Fu, Xingnian, Sun, Yongfeng, Zhang, Qiong, Jiang, Xiangqing, Zhang, Jiangwei, Zhang, Chunye, Li, Ling, Zeng, Jue, Feng, Lijian, Zhang, Chao, Liu, Yueqin, Zhang, Man, Zhang, Lijun, Zhao, Mengxi, Gao, Zhenting, Liu, Xianghui, Fang, Douglas, Guo, Haibing, Mi, Yuan, Gabriel, Tobias, Dillon, Michael P, Atadja, Peter, Oyang, Counde
Published in Journal of medicinal chemistry (23.03.2017)
Published in Journal of medicinal chemistry (23.03.2017)
Get full text
Journal Article
Discovery of the Clinical Candidate MAK683: An EED-Directed, Allosteric, and Selective PRC2 Inhibitor for the Treatment of Advanced Malignancies
Huang, Ying, Sendzik, Martin, Zhang, Jeff, Gao, Zhenting, Sun, Yongfeng, Wang, Long, Gu, Justin, Zhao, Kehao, Yu, Zhengtian, Zhang, Lijun, Zhang, Qiong, Blanz, Joachim, Chen, Zijun, Dubost, Valérie, Fang, Douglas, Feng, Lijian, Fu, Xingnian, Kiffe, Michael, Li, Ling, Luo, Fangjun, Luo, Xiao, Mi, Yuan, Mistry, Prakash, Pearson, David, Piaia, Alessandro, Scheufler, Clemens, Terranova, Remi, Weiss, Andreas, Zeng, Jue, Zhang, Hailong, Zhang, Jiangwei, Zhao, Mengxi, Dillon, Michael P, Jeay, Sebastien, Qi, Wei, Moggs, Jonathan, Pissot-Soldermann, Carole, Li, En, Atadja, Peter, Lingel, Andreas, Oyang, Counde
Published in Journal of medicinal chemistry (14.04.2022)
Published in Journal of medicinal chemistry (14.04.2022)
Get full text
Journal Article
Abstract 7132: Preclinical characterization of LAE119, a novel PARP1 selective inhibitor and trapper
Li, Ming, Chen, Yan, Chen, Junyan, Jiang, Ling, Lin, Xiaofen, Gu, Justin
Published in Cancer research (Chicago, Ill.) (22.03.2024)
Published in Cancer research (Chicago, Ill.) (22.03.2024)
Get full text
Journal Article
Abstract 670: Preclinical candidate LAE120, a novel selective USP1 inhibitor shows effective anticancer and combination activity with PARP inhibitor
Wang, Jintao, Chen, Yan, Chen, Junyan, Jiang, Ling, Lin, Xiaofen, Cai, Chaojun, Zhang, Minhua, Li, Ming, Gu, Justin
Published in Cancer research (Chicago, Ill.) (22.03.2024)
Published in Cancer research (Chicago, Ill.) (22.03.2024)
Get full text
Journal Article
Structure of Human SMYD2 Protein Reveals the Basis of p53 Tumor Suppressor Methylation
Wang, Li, Li, Ling, Zhang, Hailong, Luo, Xiao, Dai, Jingquan, Zhou, Shaolian, Gu, Justin, Zhu, Jidong, Atadja, Peter, Lu, Chris, Li, En, Zhao, Kehao
Published in The Journal of biological chemistry (04.11.2011)
Published in The Journal of biological chemistry (04.11.2011)
Get full text
Journal Article
Upregulation of CD11b and CD86 through LSD1 inhibition promotes myeloid differentiation and suppresses cell proliferation in human monocytic leukemia cells
Fang, Jianwu, Ying, Haiyan, Mao, Ting, Fang, Yanjia, Lu, Yuan, Wang, He, Zang, Irene, Wang, Zhaofu, Lin, Ying, Zhao, Mengxi, Luo, Xiao, Wang, Zongyao, Zhang, Yan, Zhang, Chao, Xiao, Wei, Wang, Yan, Tan, Wei, Chen, Zhui, Lu, Chris, Atadja, Peter, Li, En, Zhao, Kehao, Liu, Jianfeng, Gu, Justin
Published in Oncotarget (17.10.2017)
Published in Oncotarget (17.10.2017)
Get full text
Journal Article
Abstract LB-288: An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED
Qi, Wei, Zhao, Kehao, Gu, Justin, Huang, Ying, Wang, Youzhen, Zhang, Hailong, Zhang, Man, Zhang, Jeff, Yu, Zhengtian, Li, Ling, Teng, Lin, Chuai, Shannon, Zhang, Chao, Zhao, Mengxi, Chan, HoMan, Chen, Zijun, Fang, Douglas, Qi, Fei, Feng, Leying, Feng, Lijian, Gao, Yuan, Ge, Hui, Ge, Xinjian, Lingel, Andreas, Li, Guobin, Lin, Ying, Liu, Yueqin, Luo, Fangjun, Shi, Minlong, Wang, Long, Wang, Zhaofu, Yu, Yanyan, Zeng, Jue, Zeng, Chenhui, Zhang, Lijun, Zhang, Qiong, Zhou, Shaolian, Oyang, Counde, Atadja, Peter, Li, En
Published in Cancer research (Chicago, Ill.) (01.07.2017)
Published in Cancer research (Chicago, Ill.) (01.07.2017)
Get full text
Journal Article
Structure-Guided Design of EED Binders Allosterically Inhibiting the Epigenetic Polycomb Repressive Complex 2 (PRC2) Methyltransferase
Lingel, Andreas, Sendzik, Martin, Huang, Ying, Shultz, Michael D., Cantwell, John, Dillon, Michael P., Fu, Xingnian, Fuller, John, Gabriel, Tobias, Gu, Justin, Jiang, Xiangqing, Li, Ling, Liang, Fang, McKenna, Maureen, Qi, Wei, Rao, Weijun, Sheng, Xijun, Shu, Wei, Sutton, James, Taft, Benjamin, Wang, Long, Zeng, Jue, Zhang, Hailong, Zhang, Maya, Zhao, Kehao, Lindvall, Mika, Bussiere, Dirksen E.
Published in Journal of medicinal chemistry (19.12.2016)
Get full text
Published in Journal of medicinal chemistry (19.12.2016)
Journal Article