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Targeted Degradation of BET Proteins in Triple-Negative Breast Cancer.
Bai L, Zhou B, Yang CY, Ji J, McEachern D, Przybranowski S, Jiang H, Hu J, Xu F, Zhao Y, Liu L, Fernandez-Salas E, Xu J, Dou Y, Wen B, Sun D, Meagher J, Stuckey J, Hayes DF, Li S, Ellis MJ, Wang S. Bai L, et al. Among authors: zhou b. Cancer Res. 2017 May 1;77(9):2476-2487. doi: 10.1158/0008-5472.CAN-16-2622. Epub 2017 Feb 16. Cancer Res. 2017. PMID: 28209615 Free PMC article.
Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression.
Zhou B, Hu J, Xu F, Chen Z, Bai L, Fernandez-Salas E, Lin M, Liu L, Yang CY, Zhao Y, McEachern D, Przybranowski S, Wen B, Sun D, Wang S. Zhou B, et al. J Med Chem. 2018 Jan 25;61(2):462-481. doi: 10.1021/acs.jmedchem.6b01816. Epub 2017 Mar 24. J Med Chem. 2018. PMID: 28339196 Free PMC article.
Structure-Based Discovery of 4-(6-Methoxy-2-methyl-4-(quinolin-4-yl)-9H-pyrimido[4,5-b]indol-7-yl)-3,5-dimethylisoxazole (CD161) as a Potent and Orally Bioavailable BET Bromodomain Inhibitor.
Zhao Y, Bai L, Liu L, McEachern D, Stuckey JA, Meagher JL, Yang CY, Ran X, Zhou B, Hu Y, Li X, Wen B, Zhao T, Li S, Sun D, Wang S. Zhao Y, et al. Among authors: zhou b. J Med Chem. 2017 May 11;60(9):3887-3901. doi: 10.1021/acs.jmedchem.7b00193. Epub 2017 May 2. J Med Chem. 2017. PMID: 28463487 Free PMC article.
Structure-Based Discovery of CF53 as a Potent and Orally Bioavailable Bromodomain and Extra-Terminal (BET) Bromodomain Inhibitor.
Zhao Y, Zhou B, Bai L, Liu L, Yang CY, Meagher JL, Stuckey JA, McEachern D, Przybranowski S, Wang M, Ran X, Aguilar A, Hu Y, Kampf JW, Li X, Zhao T, Li S, Wen B, Sun D, Wang S. Zhao Y, et al. Among authors: zhou b. J Med Chem. 2018 Jul 26;61(14):6110-6120. doi: 10.1021/acs.jmedchem.8b00483. Epub 2018 Jul 17. J Med Chem. 2018. PMID: 30015487 Free PMC article.
Discovery of QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tumor Regression.
Qin C, Hu Y, Zhou B, Fernandez-Salas E, Yang CY, Liu L, McEachern D, Przybranowski S, Wang M, Stuckey J, Meagher J, Bai L, Chen Z, Lin M, Yang J, Ziazadeh DN, Xu F, Hu J, Xiang W, Huang L, Li S, Wen B, Sun D, Wang S. Qin C, et al. Among authors: zhou b. J Med Chem. 2018 Aug 9;61(15):6685-6704. doi: 10.1021/acs.jmedchem.8b00506. Epub 2018 Jul 18. J Med Chem. 2018. PMID: 30019901 Free PMC article.
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