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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.
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.
Reduced asymmetric dimethylarginine accumulation through inhibition of the type I protein arginine methyltransferases promotes renal fibrosis in obstructed kidneys.
Wu M, Lin P, Li L, Chen D, Yang X, Xu L, Zhou B, Wang C, Zhang Y, Luo C, Ye C. Wu M, et al. Among authors: zhou b. FASEB J. 2019 Jun;33(6):6948-6956. doi: 10.1096/fj.201802585RR. Epub 2019 Mar 6. FASEB J. 2019. PMID: 30840839
Finally, we conclude that ADMA has an antifibrotic effect in obstructed kidneys, and future application of type I PRMT inhibitor should be done cautiously for patients with CKD.-Wu, M., Lin, P., Li, L., Chen, D., Yang, X., Xu, L., Zhou, B., Wang, C., Zhang, Y., Luo, …
Finally, we conclude that ADMA has an antifibrotic effect in obstructed kidneys, and future application of type I PRMT inhibitor should be d …
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