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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: zheng j. 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.
GS-9620, an oral agonist of Toll-like receptor-7, induces prolonged suppression of hepatitis B virus in chronically infected chimpanzees.
Lanford RE, Guerra B, Chavez D, Giavedoni L, Hodara VL, Brasky KM, Fosdick A, Frey CR, Zheng J, Wolfgang G, Halcomb RL, Tumas DB. Lanford RE, et al. Among authors: zheng j. Gastroenterology. 2013 Jun;144(7):1508-17, 1517.e1-10. doi: 10.1053/j.gastro.2013.02.003. Epub 2013 Feb 13. Gastroenterology. 2013. PMID: 23415804 Free PMC article.
Pharmacokinetic and pharmacodynamic properties of GS-9620, a novel Toll-like receptor 7 agonist, demonstrate interferon-stimulated gene induction without detectable serum interferon at low oral doses.
Fosdick A, Zheng J, Pflanz S, Frey CR, Hesselgesser J, Halcomb RL, Wolfgang G, Tumas DB. Fosdick A, et al. Among authors: zheng j. J Pharmacol Exp Ther. 2014 Jan;348(1):96-105. doi: 10.1124/jpet.113.207878. Epub 2013 Oct 16. J Pharmacol Exp Ther. 2014. PMID: 24133297
Sustained efficacy and seroconversion with the Toll-like receptor 7 agonist GS-9620 in the Woodchuck model of chronic hepatitis B.
Menne S, Tumas DB, Liu KH, Thampi L, AlDeghaither D, Baldwin BH, Bellezza CA, Cote PJ, Zheng J, Halcomb R, Fosdick A, Fletcher SP, Daffis S, Li L, Yue P, Wolfgang GH, Tennant BC. Menne S, et al. Among authors: zheng j. J Hepatol. 2015 Jun;62(6):1237-45. doi: 10.1016/j.jhep.2014.12.026. Epub 2015 Jan 2. J Hepatol. 2015. PMID: 25559326 Free PMC article.
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. Among authors: zheng j. 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.
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: zheng j. 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 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. Among authors: zheng j. 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
Long-acting capsid inhibitor protects macaques from repeat SHIV challenges.
Vidal SJ, Bekerman E, Hansen D, Lu B, Wang K, Mwangi J, Rowe W, Campigotto F, Zheng J, Kato D, Chandrashekar A, Barrett J, Patel S, Wan H, Anioke T, Mercado NB, Nkolola JP, Ferguson MJ, Rinaldi WJ, Callebaut C, Blair W, Cihlar T, Geleziunas R, Yant SR, Barouch DH. Vidal SJ, et al. Among authors: zheng j. Nature. 2022 Jan;601(7894):612-616. doi: 10.1038/s41586-021-04279-4. Epub 2021 Dec 7. Nature. 2022. PMID: 34875675 Free PMC article.
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