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21 results

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Page 1
Characterization of a KDM5 small molecule inhibitor with antiviral activity against hepatitis B virus.
Gilmore SA, Tam D, Cheung TL, Snyder C, Farand J, Dick R, Matles M, Feng JY, Ramirez R, Li L, Yu H, Xu Y, Barnes D, Czerwieniec G, Brendza KM, Appleby TC, Birkus G, Willkom M, Kobayashi T, Paoli E, Labelle M, Boesen T, Tay CH, Delaney WE 4th, Notte GT, Schmitz U, Feierbach B. Gilmore SA, et al. Among authors: appleby tc. PLoS One. 2022 Dec 7;17(12):e0271145. doi: 10.1371/journal.pone.0271145. eCollection 2022. PLoS One. 2022. PMID: 36477212 Free PMC article.
Structural basis for substrate selection by the SARS-CoV-2 replicase.
Malone BF, Perry JK, Olinares PDB, Lee HW, Chen J, Appleby TC, Feng JY, Bilello JP, Ng H, Sotiris J, Ebrahim M, Chua EYD, Mendez JH, Eng ET, Landick R, Götte M, Chait BT, Campbell EA, Darst SA. Malone BF, et al. Among authors: appleby tc. Nature. 2023 Feb;614(7949):781-787. doi: 10.1038/s41586-022-05664-3. Epub 2023 Feb 1. Nature. 2023. PMID: 36725929 Free PMC article.
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: appleby tc. 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.
Discovery of a 2'-fluoro-2'-C-methyl C-nucleotide HCV polymerase inhibitor and a phosphoramidate prodrug with favorable properties.
Kirschberg TA, Metobo S, Clarke MO, Aktoudianakis V, Babusis D, Barauskas O, Birkus G, Butler T, Byun D, Chin G, Doerffler E, Edwards TE, Fenaux M, Lee R, Lew W, Mish MR, Murakami E, Park Y, Squires NH, Tirunagari N, Wang T, Whitcomb M, Xu J, Yang H, Ye H, Zhang L, Appleby TC, Feng JY, Ray AS, Cho A, Kim CU. Kirschberg TA, et al. Among authors: appleby tc. Bioorg Med Chem Lett. 2017 Apr 15;27(8):1840-1847. doi: 10.1016/j.bmcl.2017.02.037. Epub 2017 Feb 20. Bioorg Med Chem Lett. 2017. PMID: 28274633
Discovery of Potent Cyclophilin Inhibitors Based on the Structural Simplification of Sanglifehrin A.
Steadman VA, Pettit SB, Poullennec KG, Lazarides L, Keats AJ, Dean DK, Stanway SJ, Austin CA, Sanvoisin JA, Watt GM, Fliri HG, Liclican AC, Jin D, Wong MH, Leavitt SA, Lee YJ, Tian Y, Frey CR, Appleby TC, Schmitz U, Jansa P, Mackman RL, Schultz BE. Steadman VA, et al. Among authors: appleby tc. J Med Chem. 2017 Feb 9;60(3):1000-1017. doi: 10.1021/acs.jmedchem.6b01329. Epub 2017 Jan 31. J Med Chem. 2017. PMID: 28075591
Preclinical characterization of GS-9669, a thumb site II inhibitor of the hepatitis C virus NS5B polymerase.
Fenaux M, Eng S, Leavitt SA, Lee YJ, Mabery EM, Tian Y, Byun D, Canales E, Clarke MO, Doerffler E, Lazerwith SE, Lew W, Liu Q, Mertzman M, Morganelli P, Xu L, Ye H, Zhang J, Matles M, Murray BP, Mwangi J, Zhang J, Hashash A, Krawczyk SH, Bidgood AM, Appleby TC, Watkins WJ. Fenaux M, et al. Among authors: appleby tc. Antimicrob Agents Chemother. 2013 Feb;57(2):804-10. doi: 10.1128/AAC.02052-12. Epub 2012 Nov 26. Antimicrob Agents Chemother. 2013. PMID: 23183437 Free PMC article. Clinical Trial.
21 results