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Items: 32

1.

Efficacy of oral tenofovir alafenamide/emtricitabine combination or single agent tenofovir alafenamide against vaginal SHIV infection in macaques.

Massud I, Cong ME, Ruone S, Holder A, Dinh C, Nishiura K, Khalil G, Pan Y, Lipscomb J, Johnson R, Deyounks F, Rooney JF, Babusis D, Park Y, McCallister S, Callebaut C, Heneine W, García-Lerma JG.

J Infect Dis. 2019 Jul 31. pii: jiz383. doi: 10.1093/infdis/jiz383. [Epub ahead of print]

PMID:
31362305
2.

Nucleotide Prodrug Containing a Nonproteinogenic Amino Acid To Improve Oral Delivery of a Hepatitis C Virus Treatment.

Feng JY, Wang T, Park Y, Babusis D, Birkus G, Xu Y, Voitenleitner C, Fenaux M, Yang H, Eng S, Tirunagari N, Kirschberg T, Cho A, Ray AS.

Antimicrob Agents Chemother. 2018 Jul 27;62(8). pii: e00620-18. doi: 10.1128/AAC.00620-18. Print 2018 Aug.

3.

Sofosbuvir and Ribavirin Liver Pharmacokinetics in Patients Infected with Hepatitis C Virus.

Babusis D, Curry MP, Kirby B, Park Y, Murakami E, Wang T, Mathias A, Afdhal N, McHutchison JG, Ray AS.

Antimicrob Agents Chemother. 2018 Apr 26;62(5). pii: e02587-17. doi: 10.1128/AAC.02587-17. Print 2018 May.

4.

Broad-spectrum antiviral GS-5734 inhibits both epidemic and zoonotic coronaviruses.

Sheahan TP, Sims AC, Graham RL, Menachery VD, Gralinski LE, Case JB, Leist SR, Pyrc K, Feng JY, Trantcheva I, Bannister R, Park Y, Babusis D, Clarke MO, Mackman RL, Spahn JE, Palmiotti CA, Siegel D, Ray AS, Cihlar T, Jordan R, Denison MR, Baric RS.

Sci Transl Med. 2017 Jun 28;9(396). pii: eaal3653. doi: 10.1126/scitranslmed.aal3653.

5.

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.

Bioorg Med Chem Lett. 2017 Apr 15;27(8):1840-1847. doi: 10.1016/j.bmcl.2017.02.037. Epub 2017 Feb 20.

PMID:
28274633
6.

Viability of primary osteoblasts after treatment with tenofovir alafenamide: Lack of cytotoxicity at clinically relevant drug concentrations.

Callebaut C, Liu Y, Babusis D, Ray A, Miller M, Kitrinos K.

PLoS One. 2017 Feb 9;12(2):e0169948. doi: 10.1371/journal.pone.0169948. eCollection 2017.

7.

Tenofovir alafenamide (TAF) does not deplete mitochondrial DNA in human T-cell lines at intracellular concentrations exceeding clinically relevant drug exposures.

Stray KM, Park Y, Babusis D, Callebaut C, Cihlar T, Ray AS, Perron M.

Antiviral Res. 2017 Apr;140:116-120. doi: 10.1016/j.antiviral.2017.01.014. Epub 2017 Jan 26.

PMID:
28131805
8.

Chemoprophylaxis With Oral Emtricitabine and Tenofovir Alafenamide Combination Protects Macaques From Rectal Simian/Human Immunodeficiency Virus Infection.

Massud I, Mitchell J, Babusis D, Deyounks F, Ray AS, Rooney JF, Heneine W, Miller MD, García-Lerma JG.

J Infect Dis. 2016 Oct 1;214(7):1058-62. doi: 10.1093/infdis/jiw312. Epub 2016 Jul 27.

PMID:
27465645
9.

Therapeutic efficacy of the small molecule GS-5734 against Ebola virus in rhesus monkeys.

Warren TK, Jordan R, Lo MK, Ray AS, Mackman RL, Soloveva V, Siegel D, Perron M, Bannister R, Hui HC, Larson N, Strickley R, Wells J, Stuthman KS, Van Tongeren SA, Garza NL, Donnelly G, Shurtleff AC, Retterer CJ, Gharaibeh D, Zamani R, Kenny T, Eaton BP, Grimes E, Welch LS, Gomba L, Wilhelmsen CL, Nichols DK, Nuss JE, Nagle ER, Kugelman JR, Palacios G, Doerffler E, Neville S, Carra E, Clarke MO, Zhang L, Lew W, Ross B, Wang Q, Chun K, Wolfe L, Babusis D, Park Y, Stray KM, Trancheva I, Feng JY, Barauskas O, Xu Y, Wong P, Braun MR, Flint M, McMullan LK, Chen SS, Fearns R, Swaminathan S, Mayers DL, Spiropoulou CF, Lee WA, Nichol ST, Cihlar T, Bavari S.

Nature. 2016 Mar 17;531(7594):381-5. doi: 10.1038/nature17180. Epub 2016 Mar 2. Erratum in: ACS Chem Biol. 2016 May 20;11(5):1463.

10.

Role of Mitochondrial RNA Polymerase in the Toxicity of Nucleotide Inhibitors of Hepatitis C Virus.

Feng JY, Xu Y, Barauskas O, Perry JK, Ahmadyar S, Stepan G, Yu H, Babusis D, Park Y, McCutcheon K, Perron M, Schultz BE, Sakowicz R, Ray AS.

Antimicrob Agents Chemother. 2015 Nov 23;60(2):806-17. doi: 10.1128/AAC.01922-15. Print 2016 Feb.

11.

Implications of efficient hepatic delivery by tenofovir alafenamide (GS-7340) for hepatitis B virus therapy.

Murakami E, Wang T, Park Y, Hao J, Lepist EI, Babusis D, Ray AS.

Antimicrob Agents Chemother. 2015;59(6):3563-9. doi: 10.1128/AAC.00128-15. Epub 2015 Apr 13.

12.

Synthesis and characterization of 1'-C-cyano-2'-fluoro-2'-C-methyl pyrimidine nucleosides as HCV polymerase inhibitors.

Kirschberg TA, Mish MR, Zhang L, Squires NH, Wang KY, Cho A, Feng JY, Fenaux M, Babusis D, Park Y, Ray AS, Kim CU.

Bioorg Med Chem Lett. 2015 Mar 1;25(5):1040-3. doi: 10.1016/j.bmcl.2015.01.021. Epub 2015 Jan 17.

PMID:
25650256
13.

Preparation and biological evaluation of 1'-cyano-2'-C-methyl pyrimidine nucleosides as HCV NS5B polymerase inhibitors.

Mish MR, Cho A, Kirschberg T, Xu J, Zonte CS, Fenaux M, Park Y, Babusis D, Feng JY, Ray AS, Kim CU.

Bioorg Med Chem Lett. 2014 Jul 15;24(14):3092-5. doi: 10.1016/j.bmcl.2014.05.015. Epub 2014 May 22.

PMID:
24907145
14.

Metabolism and antiretroviral activity of tenofovir alafenamide in CD4+ T-cells and macrophages from demographically diverse donors.

Bam RA, Birkus G, Babusis D, Cihlar T, Yant SR.

Antivir Ther. 2014;19(7):669-77. doi: 10.3851/IMP2767. Epub 2014 Mar 14.

PMID:
24625459
15.

GS-9219/VDC-1101--a prodrug of the acyclic nucleotide PMEG has antitumor activity in spontaneous canine multiple myeloma.

Thamm DH, Vail DM, Kurzman ID, Babusis D, Ray AS, Sousa-Powers N, Tumas DB.

BMC Vet Res. 2014 Jan 25;10:30. doi: 10.1186/1746-6148-10-30.

16.

Metabolism and pharmacokinetics of the anti-hepatitis C virus nucleotide prodrug GS-6620.

Murakami E, Wang T, Babusis D, Lepist EI, Sauer D, Park Y, Vela JE, Shih R, Birkus G, Stefanidis D, Kim CU, Cho A, Ray AS.

Antimicrob Agents Chemother. 2014;58(4):1943-51. doi: 10.1128/AAC.02350-13. Epub 2014 Jan 13.

17.

Pomalidomide shows significant therapeutic activity against CNS lymphoma with a major impact on the tumor microenvironment in murine models.

Li Z, Qiu Y, Personett D, Huang P, Edenfield B, Katz J, Babusis D, Tang Y, Shirely MA, Moghaddam MF, Copland JA, Tun HW.

PLoS One. 2013 Aug 5;8(8):e71754. doi: 10.1371/journal.pone.0071754. Print 2013.

18.

Evaluation of 2'-α-fluorine modified nucleoside phosphonates as potential inhibitors of HCV polymerase.

Parrish JP, Lee SK, Boojamra CG, Hui H, Babusis D, Brown B, Shih IH, Feng JY, Ray AS, Mackman RL.

Bioorg Med Chem Lett. 2013 Jun 1;23(11):3354-7. doi: 10.1016/j.bmcl.2013.03.095. Epub 2013 Apr 2.

PMID:
23639543
19.

Discovery of the first C-nucleoside HCV polymerase inhibitor (GS-6620) with demonstrated antiviral response in HCV infected patients.

Cho A, Zhang L, Xu J, Lee R, Butler T, Metobo S, Aktoudianakis V, Lew W, Ye H, Clarke M, Doerffler E, Byun D, Wang T, Babusis D, Carey AC, German P, Sauer D, Zhong W, Rossi S, Fenaux M, McHutchison JG, Perry J, Feng J, Ray AS, Kim CU.

J Med Chem. 2014 Mar 13;57(5):1812-25. doi: 10.1021/jm400201a. Epub 2013 May 1.

PMID:
23547794
20.

Isosteric analogs of lenalidomide and pomalidomide: synthesis and biological activity.

Ruchelman AL, Man HW, Zhang W, Chen R, Capone L, Kang J, Parton A, Corral L, Schafer PH, Babusis D, Moghaddam MF, Tang Y, Shirley MA, Muller GW.

Bioorg Med Chem Lett. 2013 Jan 1;23(1):360-5. doi: 10.1016/j.bmcl.2012.10.071. Epub 2012 Oct 27.

PMID:
23168019
21.

Sensitivity of mitochondrial transcription and resistance of RNA polymerase II dependent nuclear transcription to antiviral ribonucleosides.

Arnold JJ, Sharma SD, Feng JY, Ray AS, Smidansky ED, Kireeva ML, Cho A, Perry J, Vela JE, Park Y, Xu Y, Tian Y, Babusis D, Barauskus O, Peterson BR, Gnatt A, Kashlev M, Zhong W, Cameron CE.

PLoS Pathog. 2012;8(11):e1003030. doi: 10.1371/journal.ppat.1003030. Epub 2012 Nov 15.

22.

Compared to subcutaneous tenofovir, oral tenofovir disoproxyl fumarate administration preferentially concentrates the drug into gut-associated lymphoid cells in simian immunodeficiency virus-infected macaques.

Van Rompay KK, Babusis D, Abbott Z, Geng Y, Jayashankar K, Johnson JA, Lipscomb J, Heneine W, Abel K, Ray AS.

Antimicrob Agents Chemother. 2012 Sep;56(9):4980-4. doi: 10.1128/AAC.01095-12. Epub 2012 Jul 9.

23.

Mechanism for effective lymphoid cell and tissue loading following oral administration of nucleotide prodrug GS-7340.

Babusis D, Phan TK, Lee WA, Watkins WJ, Ray AS.

Mol Pharm. 2013 Feb 4;10(2):459-66. doi: 10.1021/mp3002045. Epub 2012 Jul 12.

PMID:
22738467
24.

Synthesis and characterization of 2'-C-Me branched C-nucleosides as HCV polymerase inhibitors.

Cho A, Zhang L, Xu J, Babusis D, Butler T, Lee R, Saunders OL, Wang T, Parrish J, Perry J, Feng JY, Ray AS, Kim CU.

Bioorg Med Chem Lett. 2012 Jun 15;22(12):4127-32. doi: 10.1016/j.bmcl.2012.04.065. Epub 2012 Apr 20.

PMID:
22578461
25.

Metabolic activation of the anti-hepatitis C virus nucleotide prodrug PSI-352938.

Niu C, Tolstykh T, Bao H, Park Y, Babusis D, Lam AM, Bansal S, Du J, Chang W, Reddy PG, Zhang HR, Woolley J, Wang LQ, Chao PB, Ray AS, Otto MJ, Sofia MJ, Furman PA, Murakami E.

Antimicrob Agents Chemother. 2012 Jul;56(7):3767-75. doi: 10.1128/AAC.00530-12. Epub 2012 Apr 23.

26.

Intracellular nucleotide levels during coadministration of tenofovir disoproxil fumarate and didanosine in HIV-1-infected patients.

Hawkins T, Veikley W, Durand-Gasselin L, Babusis D, Reddy YS, Flaherty JF, Ray AS.

Antimicrob Agents Chemother. 2011 Apr;55(4):1549-55. doi: 10.1128/AAC.00910-10. Epub 2011 Jan 31.

27.

Assessment of GS-9219 in a pet dog model of non-Hodgkin's lymphoma.

Vail DM, Thamm DH, Reiser H, Ray AS, Wolfgang GH, Watkins WJ, Babusis D, Henne IN, Hawkins MJ, Kurzman ID, Jeraj R, Vanderhoek M, Plaza S, Anderson C, Wessel MA, Robat C, Lawrence J, Tumas DB.

Clin Cancer Res. 2009 May 15;15(10):3503-10. doi: 10.1158/1078-0432.CCR-08-3113. Epub 2009 May 5.

28.

Discovery of (S)-N-[2-[1-(3-ethoxy-4-methoxyphenyl)-2-methanesulfonylethyl]-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl] acetamide (apremilast), a potent and orally active phosphodiesterase 4 and tumor necrosis factor-alpha inhibitor.

Man HW, Schafer P, Wong LM, Patterson RT, Corral LG, Raymon H, Blease K, Leisten J, Shirley MA, Tang Y, Babusis DM, Chen R, Stirling D, Muller GW.

J Med Chem. 2009 Mar 26;52(6):1522-4. doi: 10.1021/jm900210d.

PMID:
19256507
29.

Synthesis, anti-HIV activity, and resistance profiles of ribose modified nucleoside phosphonates.

Mackman RL, Boojamra CG, Prasad V, Zhang L, Lin KY, Petrakovsky O, Babusis D, Chen J, Douglas J, Grant D, Hui HC, Kim CU, Markevitch DY, Vela J, Ray A, Cihlar T.

Bioorg Med Chem Lett. 2007 Dec 15;17(24):6785-9. Epub 2007 Oct 17.

PMID:
18029175
30.

Effects of human immunodeficiency virus protease inhibitors on the intestinal absorption of tenofovir disoproxil fumarate in vitro.

Tong L, Phan TK, Robinson KL, Babusis D, Strab R, Bhoopathy S, Hidalgo IJ, Rhodes GR, Ray AS.

Antimicrob Agents Chemother. 2007 Oct;51(10):3498-504. Epub 2007 Jul 30.

31.

Effects of the preservative purite on the bioavailability of brimonidine in the aqueous humor of rabbits.

Dong JQ, Babusis DM, Welty DF, Acheampong AA, Tang-Liu D, Whitcup SM.

J Ocul Pharmacol Ther. 2004 Aug;20(4):285-92.

PMID:
15321023
32.

Pharmacological characterization of a novel antiglaucoma agent, Bimatoprost (AGN 192024).

Woodward DF, Krauss AH, Chen J, Liang Y, Li C, Protzman CE, Bogardus A, Chen R, Kedzie KM, Krauss HA, Gil DW, Kharlamb A, Wheeler LA, Babusis D, Welty D, Tang-Liu DD, Cherukury M, Andrews SW, Burk RM, Garst ME.

J Pharmacol Exp Ther. 2003 May;305(2):772-85. Epub 2003 Jan 24.

PMID:
12606640

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