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Page 1
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. 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.
A highly potent long-acting small-molecule HIV-1 capsid inhibitor with efficacy in a humanized mouse model.
Yant SR, Mulato A, Hansen D, Tse WC, Niedziela-Majka A, Zhang JR, Stepan GJ, Jin D, Wong MH, Perreira JM, Singer E, Papalia GA, Hu EY, Zheng J, Lu B, Schroeder SD, Chou K, Ahmadyar S, Liclican A, Yu H, Novikov N, Paoli E, Gonik D, Ram RR, Hung M, McDougall WM, Brass AL, Sundquist WI, Cihlar T, Link JO. Yant SR, et al. Nat Med. 2019 Sep;25(9):1377-1384. doi: 10.1038/s41591-019-0560-x. Epub 2019 Sep 9. Nat Med. 2019. PMID: 31501601 Free PMC article.
New class of HIV-1 integrase (IN) inhibitors with a dual mode of action.
Tsiang M, Jones GS, Niedziela-Majka A, Kan E, Lansdon EB, Huang W, Hung M, Samuel D, Novikov N, Xu Y, Mitchell M, Guo H, Babaoglu K, Liu X, Geleziunas R, Sakowicz R. Tsiang M, et al. J Biol Chem. 2012 Jun 15;287(25):21189-203. doi: 10.1074/jbc.M112.347534. Epub 2012 Apr 25. J Biol Chem. 2012. PMID: 22535962 Free PMC article.
Impact of primary elvitegravir resistance-associated mutations in HIV-1 integrase on drug susceptibility and viral replication fitness.
Abram ME, Hluhanich RM, Goodman DD, Andreatta KN, Margot NA, Ye L, Niedziela-Majka A, Barnes TL, Novikov N, Chen X, Svarovskaia ES, McColl DJ, White KL, Miller MD. Abram ME, et al. Antimicrob Agents Chemother. 2013 Jun;57(6):2654-63. doi: 10.1128/AAC.02568-12. Epub 2013 Mar 25. Antimicrob Agents Chemother. 2013. PMID: 23529738 Free PMC article.
2,4,6-Triaminopyrimidine as a Novel Hinge Binder in a Series of PI3Kδ Selective Inhibitors.
Patel L, Chandrasekhar J, Evarts J, Haran AC, Ip C, Kaplan JA, Kim M, Koditek D, Lad L, Lepist EI, McGrath ME, Novikov N, Perreault S, Puri KD, Somoza JR, Steiner BH, Stevens KL, Therrien J, Treiberg J, Villaseñor AG, Yeung A, Phillips G. Patel L, et al. J Med Chem. 2016 Apr 14;59(7):3532-48. doi: 10.1021/acs.jmedchem.6b00213. Epub 2016 Mar 29. J Med Chem. 2016. PMID: 26980109
20 results