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Novel Pyrrolopyridone Bromodomain and Extra-Terminal Motif (BET) Inhibitors Effective in Endocrine-Resistant ER+ Breast Cancer with Acquired Resistance to Fulvestrant and Palbociclib.
Li Y, Zhao J, Gutgesell LM, Shen Z, Ratia K, Dye K, Dubrovskyi O, Zhao H, Huang F, Tonetti DA, Thatcher GRJ, Xiong R. Li Y, et al. J Med Chem. 2020 Jul 9;63(13):7186-7210. doi: 10.1021/acs.jmedchem.0c00456. Epub 2020 Jun 15. J Med Chem. 2020. PMID: 32453591 Free PMC article.
Design and Synthesis of Basic Selective Estrogen Receptor Degraders for Endocrine Therapy Resistant Breast Cancer.
Lu Y, Gutgesell LM, Xiong R, Zhao J, Li Y, Rosales CI, Hollas M, Shen Z, Gordon-Blake J, Dye K, Wang Y, Lee S, Chen H, He D, Dubrovyskyii O, Zhao H, Huang F, Lasek AW, Tonetti DA, Thatcher GRJ. Lu Y, et al. Among authors: li y. J Med Chem. 2019 Dec 26;62(24):11301-11323. doi: 10.1021/acs.jmedchem.9b01580. Epub 2019 Dec 10. J Med Chem. 2019. PMID: 31746603 Free PMC article.
XP-524 is a dual-BET/EP300 inhibitor that represses oncogenic KRAS and potentiates immune checkpoint inhibition in pancreatic cancer.
Principe DR, Xiong R, Li Y, Pham TND, Kamath SD, Dubrovskyi O, Ratia K, Huang F, Zhao J, Shen Z, Thummuri D, Daohong Z, Underwood PW, Trevino J, Munshi HG, Thatcher GRJ, Rana A. Principe DR, et al. Among authors: li y. Proc Natl Acad Sci U S A. 2022 Jan 25;119(4):e2116764119. doi: 10.1073/pnas.2116764119. Proc Natl Acad Sci U S A. 2022. PMID: 35064087 Free PMC article.
Evidence for distinct mechanisms of small molecule inhibitors of filovirus entry.
Schafer A, Xiong R, Cooper L, Nowar R, Lee H, Li Y, Ramirez BE, Peet NP, Caffrey M, Thatcher GRJ, Saphire EO, Cheng H, Rong L. Schafer A, et al. Among authors: li y. PLoS Pathog. 2021 Feb 4;17(2):e1009312. doi: 10.1371/journal.ppat.1009312. eCollection 2021 Feb. PLoS Pathog. 2021. PMID: 33539432 Free PMC article.
Potent, Novel SARS-CoV-2 PLpro Inhibitors Block Viral Replication in Monkey and Human Cell Cultures.
Shen Z, Ratia K, Cooper L, Kong D, Lee H, Kwon Y, Li Y, Alqarni S, Huang F, Dubrovskyi O, Rong L, Thatcher GR, Xiong R. Shen Z, et al. Among authors: li y. bioRxiv [Preprint]. 2021 Feb 15:2021.02.13.431008. doi: 10.1101/2021.02.13.431008. bioRxiv. 2021. Update in: J Med Chem. 2022 Feb 24;65(4):2940-2955. doi: 10.1021/acs.jmedchem.1c01307 PMID: 33594371 Free PMC article. Updated. Preprint.
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