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Discovery of an oral respiratory syncytial virus (RSV) fusion inhibitor (GS-5806) and clinical proof of concept in a human RSV challenge study.
Mackman RL, Sangi M, Sperandio D, Parrish JP, Eisenberg E, Perron M, Hui H, Zhang L, Siegel D, Yang H, Saunders O, Boojamra C, Lee G, Samuel D, Babaoglu K, Carey A, Gilbert BE, Piedra PA, Strickley R, Iwata Q, Hayes J, Stray K, Kinkade A, Theodore D, Jordan R, Desai M, Cihlar T. Mackman RL, et al. Among authors: yang h. J Med Chem. 2015 Feb 26;58(4):1630-43. doi: 10.1021/jm5017768. Epub 2015 Jan 27. J Med Chem. 2015. PMID: 25574686 Clinical Trial.
Discovery of a Potent and Orally Bioavailable Cyclophilin Inhibitor Derived from the Sanglifehrin Macrocycle.
Mackman RL, Steadman VA, Dean DK, Jansa P, Poullennec KG, Appleby T, Austin C, Blakemore CA, Cai R, Cannizzaro C, Chin G, Chiva JC, Dunbar NA, Fliri H, Highton AJ, Hui H, Ji M, Jin H, Karki K, Keats AJ, Lazarides L, Lee YJ, Liclican A, Mish M, Murray B, Pettit SB, Pyun P, Sangi M, Santos R, Sanvoisin J, Schmitz U, Schrier A, Siegel D, Sperandio D, Stepan G, Tian Y, Watt GM, Yang H, Schultz BE. Mackman RL, et al. Among authors: yang h. J Med Chem. 2018 Nov 8;61(21):9473-9499. doi: 10.1021/acs.jmedchem.8b00802. Epub 2018 Aug 22. J Med Chem. 2018. PMID: 30074795
Structure-guided discovery of a novel, potent, and orally bioavailable 3,5-dimethylisoxazole aryl-benzimidazole BET bromodomain inhibitor.
Sperandio D, Aktoudianakis V, Babaoglu K, Chen X, Elbel K, Chin G, Corkey B, Du J, Jiang B, Kobayashi T, Mackman R, Martinez R, Yang H, Zablocki J, Kusam S, Jordan K, Webb H, Bates JG, Lad L, Mish M, Niedziela-Majka A, Metobo S, Sapre A, Hung M, Jin D, Fung W, Kan E, Eisenberg G, Larson N, Newby ZER, Lansdon E, Tay C, Neve RM, Shevick SL, Breckenridge DG. Sperandio D, et al. Among authors: yang h. Bioorg Med Chem. 2019 Feb 1;27(3):457-469. doi: 10.1016/j.bmc.2018.11.020. Epub 2018 Nov 15. Bioorg Med Chem. 2019. PMID: 30606676
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: yang h. 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
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