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Prodrugs of a 1'-CN-4-Aza-7,9-dideazaadenosine C-Nucleoside Leading to the Discovery of Remdesivir (GS-5734) as a Potent Inhibitor of Respiratory Syncytial Virus with Efficacy in the African Green Monkey Model of RSV.
Mackman RL, Hui HC, Perron M, Murakami E, Palmiotti C, Lee G, Stray K, Zhang L, Goyal B, Chun K, Byun D, Siegel D, Simonovich S, Du Pont V, Pitts J, Babusis D, Vijjapurapu A, Lu X, Kim C, Zhao X, Chan J, Ma B, Lye D, Vandersteen A, Wortman S, Barrett KT, Toteva M, Jordan R, Subramanian R, Bilello JP, Cihlar T. Mackman RL, et al. Among authors: chun k. J Med Chem. 2021 Apr 22;64(8):5001-5017. doi: 10.1021/acs.jmedchem.1c00071. Epub 2021 Apr 9. J Med Chem. 2021. PMID: 33835812
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: chun k. Nature. 2016 Mar 17;531(7594):381-5. doi: 10.1038/nature17180. Epub 2016 Mar 2. Nature. 2016. PMID: 26934220 Free PMC article.
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: chun k. 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
Therapeutic efficacy of an oral nucleoside analog of remdesivir against SARS-CoV-2 pathogenesis in mice.
Schäfer A, Martinez DR, Won JJ, Moreira FR, Brown AJ, Gully KL, Kalla R, Chun K, Du Pont V, Babusis D, Tang J, Murakami E, Subramanian R, Barrett KT, Bleier BJ, Bannister R, Feng JY, Bilello JP, Cihlar T, Mackman RL, Montgomery SA, Baric RS, Sheahan TP. Schäfer A, et al. Among authors: chun k. bioRxiv [Preprint]. 2021 Sep 17:2021.09.13.460111. doi: 10.1101/2021.09.13.460111. bioRxiv. 2021. Update in: Sci Transl Med. 2022 May 4;14(643):eabm3410. doi: 10.1126/scitranslmed.abm3410 PMID: 34545367 Free PMC article. Updated. Preprint.
Oral prodrug of remdesivir parent GS-441524 is efficacious against SARS-CoV-2 in ferrets.
Cox RM, Wolf JD, Lieber CM, Sourimant J, Lin MJ, Babusis D, DuPont V, Chan J, Barrett KT, Lye D, Kalla R, Chun K, Mackman RL, Ye C, Cihlar T, Martinez-Sobrido L, Greninger AL, Bilello JP, Plemper RK. Cox RM, et al. Among authors: chun k. Nat Commun. 2021 Nov 5;12(1):6415. doi: 10.1038/s41467-021-26760-4. Nat Commun. 2021. PMID: 34741049 Free PMC article.
Therapeutic treatment with an oral prodrug of the remdesivir parental nucleoside is protective against SARS-CoV-2 pathogenesis in mice.
Schäfer A, Martinez DR, Won JJ, Meganck RM, Moreira FR, Brown AJ, Gully KL, Zweigart MR, Conrad WS, May SR, Dong S, Kalla R, Chun K, Du Pont V, Babusis D, Tang J, Murakami E, Subramanian R, Barrett KT, Bleier BJ, Bannister R, Feng JY, Bilello JP, Cihlar T, Mackman RL, Montgomery SA, Baric RS, Sheahan TP. Schäfer A, et al. Among authors: chun k. Sci Transl Med. 2022 May 4;14(643):eabm3410. doi: 10.1126/scitranslmed.abm3410. Epub 2022 May 4. Sci Transl Med. 2022. PMID: 35315683 Free PMC article.
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: chun k. 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.
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: chun k. 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
Pulsed Field Ablation as First-line Therapy for Atrial Fibrillation: A Substudy of the EU-PORIA Registry.
Füting A, Neven K, Bordignon S, Reichlin T, Blaauw Y, Hansen J, Adelino R, Ouss A, Roten L, Mulder BA, Ruwald MH, Mené R, van der Voort P, Reinsch N, Kueffer T, Boveda S, Albrecht EM, Raybuck JD, Sutton B, Chun KRJ, Schmidt B. Füting A, et al. Among authors: chun krj. Circ Arrhythm Electrophysiol. 2024 Nov 27:e013088. doi: 10.1161/CIRCEP.124.013088. Online ahead of print. Circ Arrhythm Electrophysiol. 2024. PMID: 39601122
1,236 results