Guobin Li
Novartis
6 Papers
Guobin Li is an academic researcher from Novartis. The author has contributed to research in topics: Biology & Gene. The author has an hindex of 3, co-authored 3 publications.
Chat about Author
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.
580
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
Abstract 4962: Discovery of cancer-specific E3 ligase ligands for targeted protein degradation
Zhao Wang,Mengxi Zhao,Guobin Li,Shichao Ma,Xinghao Wang,Ying Kong,Shen-Jue Chen,Hailong Zhang +7 more
TL;DR: Wang et al. as discussed by the authors used a high-throughput screen to discover cancer-specific E3 ligase ligands for targeted protein degradation and proposed a novel therapeutic approach against FBXW7 R465C mutant cancer.
Abstract 6271: Discovery of BR1733 for the treatment of SWI/SNF deficient or highly vascularized solid tumor
Xinghao Wang,Shichao Ma,Min Xie,Lele Wang,Yajun Wang,Shen-Jue Chen,Yongqi Zhou,Mengxi Zhao,Guobin Li,Xiao-Xia Fan,Hailong Zhang +10 more
TL;DR: Wang et al. as mentioned in this paper developed a potent, selective, and orally bioavailable EED inhibitor BR1733, which blocks the interaction between EED and H3K27me3, and inhibits catalytic activity of PRC2.
Discovery and Molecular Basis of a Diverse Set of Polycomb Repressive Complex 2 Inhibitors Recognition by EED
Ling Li,Hailong Zhang,Man Zhang,Mengxi Zhao,Lijian Feng,Xiao Luo,Zhenting Gao,Ying Huang,Ophelia Ardayfio,Ji-Hu Zhang,Ying Lin,Hong Fan,Yuan Mi,Guobin Li,Lei Liu,Leying Feng,Fangjun Luo,Lin Teng,Wei Qi,Johannes Ottl,Andreas Lingel,Dirksen E. Bussiere,Zhengtian Yu,Peter Atadja,Chris Lu,En Li,Justin Gu,Kehao Zhao +27 more
TL;DR: The identification and validation of four other EED binders along with EED162, the parental compound of EED226, revealed a common deep pocket induced by the binding of this diverse set of compounds, and provides structural insights for rational design of novel EED binder for the inhibition of PRC2 complex activity.