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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: kalla r. 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: kalla r. 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: kalla rv. 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
Discovery of triazolopyridine GS-458967, a late sodium current inhibitor (Late INai) of the cardiac NaV 1.5 channel with improved efficacy and potency relative to ranolazine.
Koltun DO, Parkhill EQ, Elzein E, Kobayashi T, Notte GT, Kalla R, Jiang RH, Li X, Perry TD, Avila B, Wang WQ, Smith-Maxwell C, Dhalla AK, Rajamani S, Stafford B, Tang J, Mollova N, Belardinelli L, Zablocki JA. Koltun DO, et al. Among authors: kalla r. Bioorg Med Chem Lett. 2016 Jul 1;26(13):3202-3206. doi: 10.1016/j.bmcl.2016.03.101. Epub 2016 Mar 30. Bioorg Med Chem Lett. 2016. PMID: 27080178
189 results