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Toll-Like Receptor 8 Agonist GS-9688 Induces Sustained Efficacy in the Woodchuck Model of Chronic Hepatitis B.
Daffis S, Balsitis S, Chamberlain J, Zheng J, Santos R, Rowe W, Ramakrishnan D, Pattabiraman D, Spurlock S, Chu R, Kang D, Mish M, Ramirez R, Li L, Li B, Ma S, Hung M, Voitenleitner C, Yon C, Suresh M, Menne S, Cote P, Delaney WE 4th, Mackman R, Fletcher SP. Daffis S, et al. Among authors: mackman r. Hepatology. 2021 Jan;73(1):53-67. doi: 10.1002/hep.31255. Epub 2020 Nov 27. Hepatology. 2021. PMID: 32246499 Free PMC article.
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. 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: mackman r. 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-9688 (Selgantolimod) as a Potent and Selective Oral Toll-Like Receptor 8 Agonist for the Treatment of Chronic Hepatitis B.
Mackman RL, Mish M, Chin G, Perry JK, Appleby T, Aktoudianakis V, Metobo S, Pyun P, Niu C, Daffis S, Yu H, Zheng J, Villasenor AG, Zablocki J, Chamberlain J, Jin H, Lee G, Suekawa-Pirrone K, Santos R, Delaney WE 4th, Fletcher SP. Mackman RL, et al. J Med Chem. 2020 Sep 24;63(18):10188-10203. doi: 10.1021/acs.jmedchem.0c00100. Epub 2020 Jun 3. J Med Chem. 2020. PMID: 32407112
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. Among authors: mackman r. 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.
Oral GS-5806 activity in a respiratory syncytial virus challenge study.
DeVincenzo JP, Whitley RJ, Mackman RL, Scaglioni-Weinlich C, Harrison L, Farrell E, McBride S, Lambkin-Williams R, Jordan R, Xin Y, Ramanathan S, O'Riordan T, Lewis SA, Li X, Toback SL, Lin SL, Chien JW. DeVincenzo JP, et al. Among authors: mackman rl. N Engl J Med. 2014 Aug 21;371(8):711-22. doi: 10.1056/NEJMoa1401184. N Engl J Med. 2014. PMID: 25140957 Free article. Clinical Trial.
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. 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.
71 results