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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
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
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
Fragment-Based Drug Discovery of Inhibitors of Phosphopantetheine Adenylyltransferase from Gram-Negative Bacteria.
Moreau RJ, Skepper CK, Appleton BA, Blechschmidt A, Balibar CJ, Benton BM, Drumm JE 3rd, Feng BY, Geng M, Li C, Lindvall MK, Lingel A, Lu Y, Mamo M, Mergo W, Polyakov V, Smith TM, Takeoka K, Uehara K, Wang L, Wei JR, Weiss AH, Xie L, Xu W, Zhang Q, de Vicente J. Moreau RJ, et al. Among authors: zhang q. J Med Chem. 2018 Apr 26;61(8):3309-3324. doi: 10.1021/acs.jmedchem.7b01691. Epub 2018 Apr 9. J Med Chem. 2018. PMID: 29498517
Discovery and Optimization of Phosphopantetheine Adenylyltransferase Inhibitors with Gram-Negative Antibacterial Activity.
Skepper CK, Moreau RJ, Appleton BA, Benton BM, Drumm JE 3rd, Feng BY, Geng M, Hu C, Li C, Lingel A, Lu Y, Mamo M, Mergo W, Mostafavi M, Rath CM, Steffek M, Takeoka KT, Uehara K, Wang L, Wei JR, Xie L, Xu W, Zhang Q, de Vicente J. Skepper CK, et al. Among authors: zhang q. J Med Chem. 2018 Apr 26;61(8):3325-3349. doi: 10.1021/acs.jmedchem.7b01861. Epub 2018 Apr 13. J Med Chem. 2018. PMID: 29551072
Imidazo[1,2-a]pyridin-6-yl-benzamide analogs as potent RAF inhibitors.
Smith A, Ni ZJ, Poon D, Huang Z, Chen Z, Zhang Q, Tandeske L, Merritt H, Shoemaker K, Chan J, Kaufman S, Huh K, Murray J, Appleton BA, Cowan-Jacob SW, Scheufler C, Kanazawa T, Jansen JM, Stuart D, Shafer CM. Smith A, et al. Among authors: zhang q. Bioorg Med Chem Lett. 2017 Dec 1;27(23):5221-5224. doi: 10.1016/j.bmcl.2017.10.047. Epub 2017 Oct 20. Bioorg Med Chem Lett. 2017. PMID: 29107542
In vivo incorporation of unnatural amino acids to probe structure, dynamics, and ligand binding in a large protein by nuclear magnetic resonance spectroscopy.
Cellitti SE, Jones DH, Lagpacan L, Hao X, Zhang Q, Hu H, Brittain SM, Brinker A, Caldwell J, Bursulaya B, Spraggon G, Brock A, Ryu Y, Uno T, Schultz PG, Geierstanger BH. Cellitti SE, et al. Among authors: zhang q. J Am Chem Soc. 2008 Jul 23;130(29):9268-81. doi: 10.1021/ja801602q. Epub 2008 Jun 25. J Am Chem Soc. 2008. PMID: 18576636 Free PMC article.
Site-specific labeling of proteins with NMR-active unnatural amino acids.
Jones DH, Cellitti SE, Hao X, Zhang Q, Jahnz M, Summerer D, Schultz PG, Uno T, Geierstanger BH. Jones DH, et al. Among authors: zhang q. J Biomol NMR. 2010 Jan;46(1):89-100. doi: 10.1007/s10858-009-9365-4. Epub 2009 Aug 9. J Biomol NMR. 2010. PMID: 19669620 Review.
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