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Page 1
Discovery of Dihydrobenzoxazepinone (GS-6615) Late Sodium Current Inhibitor (Late INai), a Phase II Agent with Demonstrated Preclinical Anti-Ischemic and Antiarrhythmic Properties.
Zablocki JA, Elzein E, Li X, Koltun DO, Parkhill EQ, Kobayashi T, Martinez R, Corkey B, Jiang H, Perry T, Kalla R, Notte GT, Saunders O, Graupe M, Lu Y, Venkataramani C, Guerrero J, Perry J, Osier M, Strickley R, Liu G, Wang WQ, Hu L, Li XJ, El-Bizri N, Hirakawa R, Kahlig K, Xie C, Li CH, Dhalla AK, Rajamani S, Mollova N, Soohoo D, Lepist EI, Murray B, Rhodes G, Belardinelli L, Desai MC. Zablocki JA, et al. Among authors: graupe m. J Med Chem. 2016 Oct 13;59(19):9005-9017. doi: 10.1021/acs.jmedchem.6b00939. Epub 2016 Oct 3. J Med Chem. 2016. PMID: 27690427
Pharmacokinetics, Disposition, and Biotransformation of [14C]Lenacapavir, a Novel, First-in-Class, Selective Inhibitor of HIV-1 Capsid Function, in Healthy Participants Following a Single Intravenous Infusion.
Weber E, Subramanian R, Rowe W, Graupe M, Ling J, Shen G, Begley R, Sager J, Wolckenhauer S, Rhee M, Palaparthy R, Singh R. Weber E, et al. Among authors: graupe m. Clin Pharmacokinet. 2024 Feb;63(2):241-253. doi: 10.1007/s40262-023-01328-1. Epub 2024 Jan 18. Clin Pharmacokinet. 2024. PMID: 38236562
Phenotypic CD8 T cell profiling in chronic hepatitis B to predict HBV-specific CD8 T cell susceptibility to functional restoration in vitro.
Rossi M, Vecchi A, Tiezzi C, Barili V, Fisicaro P, Penna A, Montali I, Daffis S, Fletcher SP, Gaggar A, Medley J, Graupe M, Lad L, Loglio A, Soffredini R, Borghi M, Pollicino T, Musolino C, Alfieri A, Brillo F, Laccabue D, Massari M, Boarini C, Abbati G, Pedrazzi G, Missale G, Lampertico P, Ferrari C, Boni C. Rossi M, et al. Among authors: graupe m. Gut. 2023 Nov;72(11):2123-2137. doi: 10.1136/gutjnl-2022-327202. Epub 2023 Jan 30. Gut. 2023. PMID: 36717219 Free PMC article.
ASK1 contributes to fibrosis and dysfunction in models of kidney disease.
Liles JT, Corkey BK, Notte GT, Budas GR, Lansdon EB, Hinojosa-Kirschenbaum F, Badal SS, Lee M, Schultz BE, Wise S, Pendem S, Graupe M, Castonguay L, Koch KA, Wong MH, Papalia GA, French DM, Sullivan T, Huntzicker EG, Ma FY, Nikolic-Paterson DJ, Altuhaifi T, Yang H, Fogo AB, Breckenridge DG. Liles JT, et al. Among authors: graupe m. J Clin Invest. 2018 Oct 1;128(10):4485-4500. doi: 10.1172/JCI99768. Epub 2018 Jul 19. J Clin Invest. 2018. PMID: 30024858 Free PMC article.
Structure-guided design of peptide-based tryptase inhibitors.
McGrath ME, Sprengeler PA, Hirschbein B, Somoza JR, Lehoux I, Janc JW, Gjerstad E, Graupe M, Estiarte A, Venkataramani C, Liu Y, Yee R, Ho JD, Green MJ, Lee CS, Liu L, Tai V, Spencer J, Sperandio D, Katz BA. McGrath ME, et al. Among authors: graupe m. Biochemistry. 2006 May 16;45(19):5964-73. doi: 10.1021/bi060173m. Biochemistry. 2006. PMID: 16681368
Lenacapavir Exhibits Atropisomerism-Mechanistic Pharmacokinetics and Disposition Studies of Lenacapavir Reveal Intestinal Excretion as a Major Clearance Pathway.
Zheng J, Lu B, Carr G, Mwangi J, Wang K, Hao J, Staiger KM, Kozon N, Murray BP, Bashir M, Gohdes MA, Tse WC, Schroeder S, Graupe M, Link JO, Yoon J, Chiu A, Rowe W, Smith BJ, Subramanian R. Zheng J, et al. Among authors: graupe m. J Pharmacol Exp Ther. 2024 Sep 18;391(1):91-103. doi: 10.1124/jpet.124.002302. J Pharmacol Exp Ther. 2024. PMID: 39117460
Histone deacetylase inhibitor romidepsin induces HIV expression in CD4 T cells from patients on suppressive antiretroviral therapy at concentrations achieved by clinical dosing.
Wei DG, Chiang V, Fyne E, Balakrishnan M, Barnes T, Graupe M, Hesselgesser J, Irrinki A, Murry JP, Stepan G, Stray KM, Tsai A, Yu H, Spindler J, Kearney M, Spina CA, McMahon D, Lalezari J, Sloan D, Mellors J, Geleziunas R, Cihlar T. Wei DG, et al. Among authors: graupe m. PLoS Pathog. 2014 Apr 10;10(4):e1004071. doi: 10.1371/journal.ppat.1004071. eCollection 2014 Apr. PLoS Pathog. 2014. PMID: 24722454 Free PMC article. Clinical Trial.
Clinical targeting of HIV capsid protein with a long-acting small molecule.
Link JO, Rhee MS, Tse WC, Zheng J, Somoza JR, Rowe W, Begley R, Chiu A, Mulato A, Hansen D, Singer E, Tsai LK, Bam RA, Chou CH, Canales E, Brizgys G, Zhang JR, Li J, Graupe M, Morganelli P, Liu Q, Wu Q, Halcomb RL, Saito RD, Schroeder SD, Lazerwith SE, Bondy S, Jin D, Hung M, Novikov N, Liu X, Villaseñor AG, Cannizzaro CE, Hu EY, Anderson RL, Appleby TC, Lu B, Mwangi J, Liclican A, Niedziela-Majka A, Papalia GA, Wong MH, Leavitt SA, Xu Y, Koditek D, Stepan GJ, Yu H, Pagratis N, Clancy S, Ahmadyar S, Cai TZ, Sellers S, Wolckenhauer SA, Ling J, Callebaut C, Margot N, Ram RR, Liu YP, Hyland R, Sinclair GI, Ruane PJ, Crofoot GE, McDonald CK, Brainard DM, Lad L, Swaminathan S, Sundquist WI, Sakowicz R, Chester AE, Lee WE, Daar ES, Yant SR, Cihlar T. Link JO, et al. Among authors: graupe m. Nature. 2020 Aug;584(7822):614-618. doi: 10.1038/s41586-020-2443-1. Epub 2020 Jul 1. Nature. 2020. PMID: 32612233 Free PMC article. Clinical Trial.
27 results