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An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED.
Qi W, Zhao K, Gu J, Huang Y, Wang Y, Zhang H, Zhang M, Zhang J, Yu Z, Li L, Teng L, Chuai S, Zhang C, Zhao M, Chan H, Chen Z, Fang D, Fei Q, Feng L, Feng L, Gao Y, Ge H, Ge X, Li G, Lingel A, Lin Y, Liu Y, Luo F, Shi M, Wang L, Wang Z, Yu Y, Zeng J, Zeng C, Zhang L, Zhang Q, Zhou S, Oyang C, Atadja P, Li E. Qi W, et al. Among authors: zhang l, zhang m, zhang c, zhang q, zhang j, zhang h. Nat Chem Biol. 2017 Apr;13(4):381-388. doi: 10.1038/nchembio.2304. Epub 2017 Jan 30. Nat Chem Biol. 2017. PMID: 28135235
A Selective FGFR1/2 PROTAC Degrader with Antitumor Activity.
Kong Y, Zhao X, Wang Z, Yuan S, Chen S, Lou S, Ma S, Li Y, Wang X, Ge Y, Li G, Yang H, Zhao M, Li D, Zhang H, Tan W, Wang J. Kong Y, et al. Among authors: zhang h. Mol Cancer Ther. 2024 Jun 10:OF1-OF11. doi: 10.1158/1535-7163.MCT-23-0719. Online ahead of print. Mol Cancer Ther. 2024. PMID: 38853423
Discovery and Molecular Basis of a Diverse Set of Polycomb Repressive Complex 2 Inhibitors Recognition by EED.
Li L, Zhang H, Zhang M, Zhao M, Feng L, Luo X, Gao Z, Huang Y, Ardayfio O, Zhang JH, Lin Y, Fan H, Mi Y, Li G, Liu L, Feng L, Luo F, Teng L, Qi W, Ottl J, Lingel A, Bussiere DE, Yu Z, Atadja P, Lu C, Li E, Gu J, Zhao K. Li L, et al. Among authors: zhang m, zhang jh, zhang h. PLoS One. 2017 Jan 10;12(1):e0169855. doi: 10.1371/journal.pone.0169855. eCollection 2017. PLoS One. 2017. PMID: 28072869 Free PMC article.
Discovery of the Clinical Candidate MAK683: An EED-Directed, Allosteric, and Selective PRC2 Inhibitor for the Treatment of Advanced Malignancies.
Huang Y, Sendzik M, Zhang J, Gao Z, Sun Y, Wang L, Gu J, Zhao K, Yu Z, Zhang L, Zhang Q, Blanz J, Chen Z, Dubost V, Fang D, Feng L, Fu X, Kiffe M, Li L, Luo F, Luo X, Mi Y, Mistry P, Pearson D, Piaia A, Scheufler C, Terranova R, Weiss A, Zeng J, Zhang H, Zhang J, Zhao M, Dillon MP, Jeay S, Qi W, Moggs J, Pissot-Soldermann C, Li E, Atadja P, Lingel A, Oyang C. Huang Y, et al. Among authors: zhang l, zhang q, zhang j, zhang h. J Med Chem. 2022 Apr 14;65(7):5317-5333. doi: 10.1021/acs.jmedchem.1c02148. Epub 2022 Mar 30. J Med Chem. 2022. PMID: 35352560
NSD2 is recruited through its PHD domain to oncogenic gene loci to drive multiple myeloma.
Huang Z, Wu H, Chuai S, Xu F, Yan F, Englund N, Wang Z, Zhang H, Fang M, Wang Y, Gu J, Zhang M, Yang T, Zhao K, Yu Y, Dai J, Yi W, Zhou S, Li Q, Wu J, Liu J, Wu X, Chan H, Lu C, Atadja P, Li E, Wang Y, Hu M. Huang Z, et al. Among authors: zhang m, zhang h. Cancer Res. 2013 Oct 15;73(20):6277-88. doi: 10.1158/0008-5472.CAN-13-1000. Epub 2013 Aug 26. Cancer Res. 2013. PMID: 23980095
Discovery of First-in-Class, Potent, and Orally Bioavailable Embryonic Ectoderm Development (EED) Inhibitor with Robust Anticancer Efficacy.
Huang Y, Zhang J, Yu Z, Zhang H, Wang Y, Lingel A, Qi W, Gu J, Zhao K, Shultz MD, Wang L, Fu X, Sun Y, Zhang Q, Jiang X, Zhang J, Zhang C, Li L, Zeng J, Feng L, Zhang C, Liu Y, Zhang M, Zhang L, Zhao M, Gao Z, Liu X, Fang D, Guo H, Mi Y, Gabriel T, Dillon MP, Atadja P, Oyang C. Huang Y, et al. Among authors: zhang l, zhang m, zhang c, zhang q, zhang j, zhang h. J Med Chem. 2017 Mar 23;60(6):2215-2226. doi: 10.1021/acs.jmedchem.6b01576. Epub 2017 Feb 6. J Med Chem. 2017. PMID: 28092155
Activation loop dynamics are controlled by conformation-selective inhibitors of ERK2.
Pegram LM, Liddle JC, Xiao Y, Hoh M, Rudolph J, Iverson DB, Vigers GP, Smith D, Zhang H, Wang W, Moffat JG, Ahn NG. Pegram LM, et al. Among authors: zhang h. Proc Natl Acad Sci U S A. 2019 Jul 30;116(31):15463-15468. doi: 10.1073/pnas.1906824116. Epub 2019 Jul 16. Proc Natl Acad Sci U S A. 2019. PMID: 31311868 Free PMC article.
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