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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: pitts j. 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
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: pitts j. 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
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: pitts j. 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.
Inhaled remdesivir reduces viral burden in a nonhuman primate model of SARS-CoV-2 infection.
Vermillion MS, Murakami E, Ma B, Pitts J, Tomkinson A, Rautiola D, Babusis D, Irshad H, Seigel D, Kim C, Zhao X, Niu C, Yang J, Gigliotti A, Kadrichu N, Bilello JP, Ellis S, Bannister R, Subramanian R, Smith B, Mackman RL, Lee WA, Kuehl PJ, Hartke J, Cihlar T, Porter DP. Vermillion MS, et al. Among authors: pitts j. Sci Transl Med. 2022 Feb 23;14(633):eabl8282. doi: 10.1126/scitranslmed.abl8282. Epub 2022 Feb 23. Sci Transl Med. 2022. PMID: 34968150 Free PMC article.
Intravenous delivery of GS-441524 is efficacious in the African green monkey model of SARS-CoV-2 infection.
Pitts J, Babusis D, Vermillion MS, Subramanian R, Barrett K, Lye D, Ma B, Zhao X, Riola N, Xie X, Kajon A, Lu X, Bannister R, Shi PY, Toteva M, Porter DP, Smith BJ, Cihlar T, Mackman R, Bilello JP. Pitts J, et al. Antiviral Res. 2022 Jul;203:105329. doi: 10.1016/j.antiviral.2022.105329. Epub 2022 May 5. Antiviral Res. 2022. PMID: 35525335 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: pitts j. 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.
Remdesivir and GS-441524 Retain Antiviral Activity against Delta, Omicron, and Other Emergent SARS-CoV-2 Variants.
Pitts J, Li J, Perry JK, Du Pont V, Riola N, Rodriguez L, Lu X, Kurhade C, Xie X, Camus G, Manhas S, Martin R, Shi PY, Cihlar T, Porter DP, Mo H, Maiorova E, Bilello JP. Pitts J, et al. Antimicrob Agents Chemother. 2022 Jun 21;66(6):e0022222. doi: 10.1128/aac.00222-22. Epub 2022 May 9. Antimicrob Agents Chemother. 2022. PMID: 35532238 Free PMC article.
Remdesivir Inhibits SARS-CoV-2 in Human Lung Cells and Chimeric SARS-CoV Expressing the SARS-CoV-2 RNA Polymerase in Mice.
Pruijssers AJ, George AS, Schäfer A, Leist SR, Gralinksi LE, Dinnon KH 3rd, Yount BL, Agostini ML, Stevens LJ, Chappell JD, Lu X, Hughes TM, Gully K, Martinez DR, Brown AJ, Graham RL, Perry JK, Du Pont V, Pitts J, Ma B, Babusis D, Murakami E, Feng JY, Bilello JP, Porter DP, Cihlar T, Baric RS, Denison MR, Sheahan TP. Pruijssers AJ, et al. Among authors: pitts j. Cell Rep. 2020 Jul 21;32(3):107940. doi: 10.1016/j.celrep.2020.107940. Epub 2020 Jul 7. Cell Rep. 2020. PMID: 32668216 Free PMC article.
Remdesivir potently inhibits SARS-CoV-2 in human lung cells and chimeric SARS-CoV expressing the SARS-CoV-2 RNA polymerase in mice.
Pruijssers AJ, George AS, Schäfer A, Leist SR, Gralinksi LE, Dinnon KH, Yount BL, Agostini ML, Stevens LJ, Chappell JD, Lu X, Hughes TM, Gully K, Martinez DR, Brown AJ, Graham RL, Perry JK, Du Pont V, Pitts J, Ma B, Babusis D, Murakami E, Feng JY, Bilello JP, Porter DP, Cihlar T, Baric RS, Denison MR, Sheahan TP. Pruijssers AJ, et al. Among authors: pitts j. bioRxiv [Preprint]. 2020 Apr 27:2020.04.27.064279. doi: 10.1101/2020.04.27.064279. bioRxiv. 2020. Update in: Cell Rep. 2020 Jul 21;32(3):107940. doi: 10.1016/j.celrep.2020.107940 PMID: 32511392 Free PMC article. Updated. Preprint.
412 results