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Discovery of MD-224 as a First-in-Class, Highly Potent, and Efficacious Proteolysis Targeting Chimera Murine Double Minute 2 Degrader Capable of Achieving Complete and Durable Tumor Regression.
Li Y, Yang J, Aguilar A, McEachern D, Przybranowski S, Liu L, Yang CY, Wang M, Han X, Wang S. Li Y, et al. Among authors: liu l. J Med Chem. 2019 Jan 24;62(2):448-466. doi: 10.1021/acs.jmedchem.8b00909. Epub 2018 Dec 10. J Med Chem. 2019. PMID: 30525597 Free PMC article.
A potent and highly efficacious Bcl-2/Bcl-xL inhibitor.
Aguilar A, Zhou H, Chen J, Liu L, Bai L, McEachern D, Yang CY, Meagher J, Stuckey J, Wang S. Aguilar A, et al. Among authors: liu l. J Med Chem. 2013 Apr 11;56(7):3048-3067. doi: 10.1021/jm4001105. Epub 2013 Mar 22. J Med Chem. 2013. PMID: 23448298 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. Among authors: liu l. 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.
Discovery of 4-((3'R,4'S,5'R)-6″-Chloro-4'-(3-chloro-2-fluorophenyl)-1'-ethyl-2″-oxodispiro[cyclohexane-1,2'-pyrrolidine-3',3″-indoline]-5'-carboxamido)bicyclo[2.2.2]octane-1-carboxylic Acid (AA-115/APG-115): A Potent and Orally Active Murine Double Minute 2 (MDM2) Inhibitor in Clinical Development.
Aguilar A, Lu J, Liu L, Du D, Bernard D, McEachern D, Przybranowski S, Li X, Luo R, Wen B, Sun D, Wang H, Wen J, Wang G, Zhai Y, Guo M, Yang D, Wang S. Aguilar A, et al. Among authors: liu l. J Med Chem. 2017 Apr 13;60(7):2819-2839. doi: 10.1021/acs.jmedchem.6b01665. Epub 2017 Mar 24. J Med Chem. 2017. PMID: 28339198 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: liu l. 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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