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Discovery of GS-7682, a Novel 4'-Cyano-Modified C-Nucleoside Prodrug with Broad Activity against Pneumo- and Picornaviruses and Efficacy in RSV-Infected African Green Monkeys.
Siegel DS, Hui HC, Pitts J, Vermillion MS, Ishida K, Rautiola D, Keeney M, Irshad H, Zhang L, Chun K, Chin G, Goyal B, Doerffler E, Yang H, Clarke MO, Palmiotti C, Vijjapurapu A, Riola NC, Stray K, Murakami E, Ma B, Wang T, Zhao X, Xu Y, Lee G, Marchand B, Seung M, Nayak A, Tomkinson A, Kadrichu N, Ellis S, Barauskas O, Feng JY, Perry JK, Perron M, Bilello JP, Kuehl PJ, Subramanian R, Cihlar T, Mackman RL. Siegel DS, et al. Among authors: xu y. J Med Chem. 2024 Aug 8;67(15):12945-12968. doi: 10.1021/acs.jmedchem.4c00899. Epub 2024 Jul 17. J Med Chem. 2024. PMID: 39018526
Discovery and Synthesis of a Phosphoramidate Prodrug of a Pyrrolo[2,1-f][triazin-4-amino] Adenine C-Nucleoside (GS-5734) for the Treatment of Ebola and Emerging Viruses.
Siegel D, Hui HC, Doerffler E, Clarke MO, Chun K, Zhang L, Neville S, Carra E, Lew W, Ross B, Wang Q, Wolfe L, Jordan R, Soloveva V, Knox J, Perry J, Perron M, Stray KM, Barauskas O, Feng JY, Xu Y, Lee G, Rheingold AL, Ray AS, Bannister R, Strickley R, Swaminathan S, Lee WA, Bavari S, Cihlar T, Lo MK, Warren TK, Mackman RL. Siegel D, et al. Among authors: xu y. J Med Chem. 2017 Mar 9;60(5):1648-1661. doi: 10.1021/acs.jmedchem.6b01594. Epub 2017 Feb 14. J Med Chem. 2017. PMID: 28124907
Discovery of GS-5245 (Obeldesivir), an Oral Prodrug of Nucleoside GS-441524 That Exhibits Antiviral Efficacy in SARS-CoV-2-Infected African Green Monkeys.
Mackman RL, Kalla RV, Babusis D, Pitts J, Barrett KT, Chun K, Du Pont V, Rodriguez L, Moshiri J, Xu Y, Lee M, Lee G, Bleier B, Nguyen AQ, O'Keefe BM, Ambrosi A, Cook M, Yu J, Dempah KE, Bunyan E, Riola NC, Lu X, Liu R, Davie A, Hsiang TY, Dearing J, Vermillion M, Gale M Jr, Niedziela-Majka A, Feng JY, Hedskog C, Bilello JP, Subramanian R, Cihlar T. Mackman RL, et al. Among authors: xu y. J Med Chem. 2023 Sep 14;66(17):11701-11717. doi: 10.1021/acs.jmedchem.3c00750. Epub 2023 Aug 19. J Med Chem. 2023. PMID: 37596939 Free PMC article.
Therapeutic efficacy of the small molecule GS-5734 against Ebola virus in rhesus monkeys.
Warren TK, Jordan R, Lo MK, Ray AS, Mackman RL, Soloveva V, Siegel D, Perron M, Bannister R, Hui HC, Larson N, Strickley R, Wells J, Stuthman KS, Van Tongeren SA, Garza NL, Donnelly G, Shurtleff AC, Retterer CJ, Gharaibeh D, Zamani R, Kenny T, Eaton BP, Grimes E, Welch LS, Gomba L, Wilhelmsen CL, Nichols DK, Nuss JE, Nagle ER, Kugelman JR, Palacios G, Doerffler E, Neville S, Carra E, Clarke MO, Zhang L, Lew W, Ross B, Wang Q, Chun K, Wolfe L, Babusis D, Park Y, Stray KM, Trancheva I, Feng JY, Barauskas O, Xu Y, Wong P, Braun MR, Flint M, McMullan LK, Chen SS, Fearns R, Swaminathan S, Mayers DL, Spiropoulou CF, Lee WA, Nichol ST, Cihlar T, Bavari S. Warren TK, et al. Among authors: xu y. Nature. 2016 Mar 17;531(7594):381-5. doi: 10.1038/nature17180. Epub 2016 Mar 2. Nature. 2016. PMID: 26934220 Free PMC article.
Inhibition of hepatitis C virus replication by GS-6620, a potent C-nucleoside monophosphate prodrug.
Feng JY, Cheng G, Perry J, Barauskas O, Xu Y, Fenaux M, Eng S, Tirunagari N, Peng B, Yu M, Tian Y, Lee YJ, Stepan G, Lagpacan LL, Jin D, Hung M, Ku KS, Han B, Kitrinos K, Perron M, Birkus G, Wong KA, Zhong W, Kim CU, Carey A, Cho A, Ray AS. Feng JY, et al. Among authors: xu y. Antimicrob Agents Chemother. 2014;58(4):1930-42. doi: 10.1128/AAC.02351-13. Epub 2014 Jan 13. Antimicrob Agents Chemother. 2014. PMID: 24419349 Free PMC article.
Key Metabolic Enzymes Involved in Remdesivir Activation in Human Lung Cells.
Li R, Liclican A, Xu Y, Pitts J, Niu C, Zhang J, Kim C, Zhao X, Soohoo D, Babusis D, Yue Q, Ma B, Murray BP, Subramanian R, Xie X, Zou J, Bilello JP, Li L, Schultz BE, Sakowicz R, Smith BJ, Shi PY, Murakami E, Feng JY. Li R, et al. Among authors: xu y. Antimicrob Agents Chemother. 2021 Aug 17;65(9):e0060221. doi: 10.1128/AAC.00602-21. Epub 2021 Aug 17. Antimicrob Agents Chemother. 2021. PMID: 34125594 Free PMC article.
Nucleotide Prodrug Containing a Nonproteinogenic Amino Acid To Improve Oral Delivery of a Hepatitis C Virus Treatment.
Feng JY, Wang T, Park Y, Babusis D, Birkus G, Xu Y, Voitenleitner C, Fenaux M, Yang H, Eng S, Tirunagari N, Kirschberg T, Cho A, Ray AS. Feng JY, et al. Among authors: xu y. Antimicrob Agents Chemother. 2018 Jul 27;62(8):e00620-18. doi: 10.1128/AAC.00620-18. Print 2018 Aug. Antimicrob Agents Chemother. 2018. PMID: 29866875 Free PMC article.
Preclinical characterization of a non-peptidomimetic HIV protease inhibitor with improved metabolic stability.
Mulato A, Lansdon E, Aoyama R, Voigt J, Lee M, Liclican A, Lee G, Singer E, Stafford B, Gong R, Murray B, Chan J, Lee J, Xu Y, Ahmadyar S, Gonzalez A, Cho A, Stepan GJ, Schmitz U, Schultz B, Marchand B, Brumshtein B, Wang R, Yu H, Cihlar T, Xu L, Yant SR. Mulato A, et al. Among authors: xu l, xu y. Antimicrob Agents Chemother. 2024 Apr 3;68(4):e0137323. doi: 10.1128/aac.01373-23. Epub 2024 Feb 21. Antimicrob Agents Chemother. 2024. PMID: 38380945 Free PMC article.
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