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Items: 1 to 50 of 98

1.

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.

Nat Med. 2019 Sep;25(9):1377-1384. doi: 10.1038/s41591-019-0560-x. Epub 2019 Sep 9.

PMID:
31501601
2.

Broad spectrum antiviral remdesivir inhibits human endemic and zoonotic deltacoronaviruses with a highly divergent RNA dependent RNA polymerase.

Brown AJ, Won JJ, Graham RL, Dinnon KH 3rd, Sims AC, Feng JY, Cihlar T, Denison MR, Baric RS, Sheahan TP.

Antiviral Res. 2019 Sep;169:104541. doi: 10.1016/j.antiviral.2019.104541. Epub 2019 Jun 21.

PMID:
31233808
3.

Remdesivir (GS-5734) protects African green monkeys from Nipah virus challenge.

Lo MK, Feldmann F, Gary JM, Jordan R, Bannister R, Cronin J, Patel NR, Klena JD, Nichol ST, Cihlar T, Zaki SR, Feldmann H, Spiropoulou CF, de Wit E.

Sci Transl Med. 2019 May 29;11(494). pii: eaau9242. doi: 10.1126/scitranslmed.aau9242.

PMID:
31142680
4.

Identification of NK Cell Subpopulations That Differentiate HIV-Infected Subject Cohorts with Diverse Levels of Virus Control.

Pohlmeyer CW, Gonzalez VD, Irrinki A, Ramirez RN, Li L, Mulato A, Murry JP, Arvey A, Hoh R, Deeks SG, Kukolj G, Cihlar T, Pflanz S, Nolan GP, Min-Oo G.

J Virol. 2019 Mar 21;93(7). pii: e01790-18. doi: 10.1128/JVI.01790-18. Print 2019 Apr 1.

5.

TLR7 agonists induce transient viremia and reduce the viral reservoir in SIV-infected rhesus macaques on antiretroviral therapy.

Lim SY, Osuna CE, Hraber PT, Hesselgesser J, Gerold JM, Barnes TL, Sanisetty S, Seaman MS, Lewis MG, Geleziunas R, Miller MD, Cihlar T, Lee WA, Hill AL, Whitney JB.

Sci Transl Med. 2018 May 2;10(439). pii: eaao4521. doi: 10.1126/scitranslmed.aao4521.

6.

Coronavirus Susceptibility to the Antiviral Remdesivir (GS-5734) Is Mediated by the Viral Polymerase and the Proofreading Exoribonuclease.

Agostini ML, Andres EL, Sims AC, Graham RL, Sheahan TP, Lu X, Smith EC, Case JB, Feng JY, Jordan R, Ray AS, Cihlar T, Siegel D, Mackman RL, Clarke MO, Baric RS, Denison MR.

MBio. 2018 Mar 6;9(2). pii: e00221-18. doi: 10.1128/mBio.00221-18.

7.

Blood biomarkers of expressed and inducible HIV-1.

Cillo AR, Hong F, Tsai A, Irrinki A, Kaur J, Sloan DD, Follen M, Geleziunas R, Cihlar T, Win SS, Murry JP, Mellors JW.

AIDS. 2018 Mar 27;32(6):699-708. doi: 10.1097/QAD.0000000000001748.

8.

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.

9.

GS-5734 and its parent nucleoside analog inhibit Filo-, Pneumo-, and Paramyxoviruses.

Lo MK, Jordan R, Arvey A, Sudhamsu J, Shrivastava-Ranjan P, Hotard AL, Flint M, McMullan LK, Siegel D, Clarke MO, Mackman RL, Hui HC, Perron M, Ray AS, Cihlar T, Nichol ST, Spiropoulou CF.

Sci Rep. 2017 Mar 6;7:43395. doi: 10.1038/srep43395.

10.

Toll-Like Receptor 7 Agonist GS-9620 Induces HIV Expression and HIV-Specific Immunity in Cells from HIV-Infected Individuals on Suppressive Antiretroviral Therapy.

Tsai A, Irrinki A, Kaur J, Cihlar T, Kukolj G, Sloan DD, Murry JP.

J Virol. 2017 Mar 29;91(8). pii: e02166-16. doi: 10.1128/JVI.02166-16. Print 2017 Apr 15.

11.

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
12.

Discovery and Synthesis of a Phosphoramidate Prodrug of a Pyrrolo[2,1-f][triazin-4-amino] Adenine C-Nucleoside (GS-5734) for the Treatment of Ebola and Emerging Viruses.

Siegel D, Hui HC, Doerffler E, Clarke MO, Chun K, Zhang L, Neville S, Carra E, Lew W, Ross B, Wang Q, Wolfe L, Jordan R, Soloveva V, Knox J, Perry J, Perron M, Stray KM, Barauskas O, Feng JY, Xu Y, Lee G, Rheingold AL, Ray AS, Bannister R, Strickley R, Swaminathan S, Lee WA, Bavari S, Cihlar T, Lo MK, Warren TK, Mackman RL.

J Med Chem. 2017 Mar 9;60(5):1648-1661. doi: 10.1021/acs.jmedchem.6b01594. Epub 2017 Feb 14.

PMID:
28124907
13.

TLR7 Agonist GS-9620 Is a Potent Inhibitor of Acute HIV-1 Infection in Human Peripheral Blood Mononuclear Cells.

Bam RA, Hansen D, Irrinki A, Mulato A, Jones GS, Hesselgesser J, Frey CR, Cihlar T, Yant SR.

Antimicrob Agents Chemother. 2016 Dec 27;61(1). pii: e01369-16. doi: 10.1128/AAC.01369-16. Print 2017 Jan.

14.

Antiviral Activity of Bictegravir (GS-9883), a Novel Potent HIV-1 Integrase Strand Transfer Inhibitor with an Improved Resistance Profile.

Tsiang M, Jones GS, Goldsmith J, Mulato A, Hansen D, Kan E, Tsai L, Bam RA, Stepan G, Stray KM, Niedziela-Majka A, Yant SR, Yu H, Kukolj G, Cihlar T, Lazerwith SE, White KL, Jin H.

Antimicrob Agents Chemother. 2016 Nov 21;60(12):7086-7097. Print 2016 Dec.

15.

Accelerating Drug Development: Antiviral Therapies for Emerging Viruses as a Model.

Everts M, Cihlar T, Bostwick JR, Whitley RJ.

Annu Rev Pharmacol Toxicol. 2017 Jan 6;57:155-169. doi: 10.1146/annurev-pharmtox-010716-104533. Epub 2016 Jul 22. Review.

PMID:
27483339
16.

Rapid In Vitro Evaluation of Antiretroviral Barrier to Resistance at Therapeutic Drug Levels.

Mulato A, Hansen D, Thielen A, Porter D, Stepan G, White K, Daeumer M, Cihlar T, Yant SR.

AIDS Res Hum Retroviruses. 2016 Dec;32(12):1237-1247. Epub 2016 Jul 25.

PMID:
27356854
17.

Current status and prospects of HIV treatment.

Cihlar T, Fordyce M.

Curr Opin Virol. 2016 Jun;18:50-6. doi: 10.1016/j.coviro.2016.03.004. Epub 2016 Mar 28. Review.

18.

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.

19.

GS-5806 Inhibits a Broad Range of Respiratory Syncytial Virus Clinical Isolates by Blocking the Virus-Cell Fusion Process.

Perron M, Stray K, Kinkade A, Theodore D, Lee G, Eisenberg E, Sangi M, Gilbert BE, Jordan R, Piedra PA, Toms GL, Mackman R, Cihlar T.

Antimicrob Agents Chemother. 2015 Dec 14;60(3):1264-73. doi: 10.1128/AAC.01497-15.

20.

The Interferon Type I/III Response to Respiratory Syncytial Virus Infection in Airway Epithelial Cells Can Be Attenuated or Amplified by Antiviral Treatment.

McCutcheon KM, Jordan R, Mawhorter ME, Noton SL, Powers JG, Fearns R, Cihlar T, Perron M.

J Virol. 2015 Nov 25;90(4):1705-17. doi: 10.1128/JVI.02417-15. Print 2016 Feb 15.

21.

Targeting HIV Reservoir in Infected CD4 T Cells by Dual-Affinity Re-targeting Molecules (DARTs) that Bind HIV Envelope and Recruit Cytotoxic T Cells.

Sloan DD, Lam CY, Irrinki A, Liu L, Tsai A, Pace CS, Kaur J, Murry JP, Balakrishnan M, Moore PA, Johnson S, Nordstrom JL, Cihlar T, Koenig S.

PLoS Pathog. 2015 Nov 5;11(11):e1005233. doi: 10.1371/journal.ppat.1005233. eCollection 2015.

22.

Intracellular Activation of Tenofovir Alafenamide and the Effect of Viral and Host Protease Inhibitors.

Birkus G, Bam RA, Willkom M, Frey CR, Tsai L, Stray KM, Yant SR, Cihlar T.

Antimicrob Agents Chemother. 2015 Oct 26;60(1):316-22. doi: 10.1128/AAC.01834-15. Print 2016 Jan.

23.

Antiviral Efficacy of a Respiratory Syncytial Virus (RSV) Fusion Inhibitor in a Bovine Model of RSV Infection.

Jordan R, Shao M, Mackman RL, Perron M, Cihlar T, Lewis SA, Eisenberg EJ, Carey A, Strickley RG, Chien JW, Anderson ML, McEligot HA, Behrens NE, Gershwin LJ.

Antimicrob Agents Chemother. 2015 Aug;59(8):4889-900. doi: 10.1128/AAC.00487-15. Epub 2015 Jun 8.

24.

Discovery of an oral respiratory syncytial virus (RSV) fusion inhibitor (GS-5806) and clinical proof of concept in a human RSV challenge study.

Mackman RL, Sangi M, Sperandio D, Parrish JP, Eisenberg E, Perron M, Hui H, Zhang L, Siegel D, Yang H, Saunders O, Boojamra C, Lee G, Samuel D, Babaoglu K, Carey A, Gilbert BE, Piedra PA, Strickley R, Iwata Q, Hayes J, Stray K, Kinkade A, Theodore D, Jordan R, Desai M, Cihlar T.

J Med Chem. 2015 Feb 26;58(4):1630-43. doi: 10.1021/jm5017768. Epub 2015 Jan 27.

PMID:
25574686
25.

Abyssomicin 2 reactivates latent HIV-1 by a PKC- and HDAC-independent mechanism.

León B, Navarro G, Dickey BJ, Stepan G, Tsai A, Jones GS, Morales ME, Barnes T, Ahmadyar S, Tsiang M, Geleziunas R, Cihlar T, Pagratis N, Tian Y, Yu H, Linington RG.

Org Lett. 2015 Jan 16;17(2):262-5. doi: 10.1021/ol503349y. Epub 2015 Jan 5.

26.

Quantitative microscopy of functional HIV post-entry complexes reveals association of replication with the viral capsid.

Peng K, Muranyi W, Glass B, Laketa V, Yant SR, Tsai L, Cihlar T, Müller B, Kräusslich HG.

Elife. 2014 Dec 17;3:e04114. doi: 10.7554/eLife.04114.

27.

A pharmacogenetic candidate gene study of tenofovir-associated Fanconi syndrome.

Dahlin A, Wittwer M, de la Cruz M, Woo JM, Bam R, Scharen-Guivel V, Flaherty J, Ray AS, Cihlar T, Gupta SK, Giacomini KM.

Pharmacogenet Genomics. 2015 Feb;25(2):82-92. doi: 10.1097/FPC.0000000000000110.

28.

Human respiratory syncytial virus memphis 37 causes acute respiratory disease in perinatal lamb lung.

Derscheid RJ, van Geelen A, Gallup JM, Kienzle T, Shelly DA, Cihlar T, King RR, Ackermann MR.

Biores Open Access. 2014 Apr 1;3(2):60-9. doi: 10.1089/biores.2013.0044.

29.

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.

PLoS Pathog. 2014 Apr 10;10(4):e1004071. doi: 10.1371/journal.ppat.1004071. eCollection 2014 Apr.

30.

Tenofovir alafenamide is not a substrate for renal organic anion transporters (OATs) and does not exhibit OAT-dependent cytotoxicity.

Bam RA, Yant SR, Cihlar T.

Antivir Ther. 2014;19(7):687-92. doi: 10.3851/IMP2770. Epub 2014 Apr 4.

PMID:
24699134
31.

Contribution of the organic anion transporter OAT2 to the renal active tubular secretion of creatinine and mechanism for serum creatinine elevations caused by cobicistat.

Lepist EI, Zhang X, Hao J, Huang J, Kosaka A, Birkus G, Murray BP, Bannister R, Cihlar T, Huang Y, Ray AS.

Kidney Int. 2014 Aug;86(2):350-7. doi: 10.1038/ki.2014.66. Epub 2014 Mar 19.

32.

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
33.

Study of marine natural products including resorcyclic acid lactones from Humicola fuscoatra that reactivate latent HIV-1 expression in an in vitro model of central memory CD4+ T cells.

Mejia EJ, Loveridge ST, Stepan G, Tsai A, Jones GS, Barnes T, White KN, Drašković M, Tenney K, Tsiang M, Geleziunas R, Cihlar T, Pagratis N, Tian Y, Yu H, Crews P.

J Nat Prod. 2014 Mar 28;77(3):618-24. doi: 10.1021/np400889x. Epub 2014 Feb 4.

34.

GS-8374, a prototype phosphonate-containing inhibitor of HIV-1 protease, effectively inhibits protease mutants with amino acid insertions.

Grantz Šašková K, Kozíšek M, Stray K, de Jong D, Rezáová P, Brynda J, van Maarseveen NM, Nijhuis M, Cihlár T, Konvalinka J.

J Virol. 2014 Mar;88(6):3586-90. doi: 10.1128/JVI.02688-13. Epub 2013 Dec 26.

35.

Multiple classes of antiviral agents exhibit in vitro activity against human rhinovirus type C.

Mello C, Aguayo E, Rodriguez M, Lee G, Jordan R, Cihlar T, Birkus G.

Antimicrob Agents Chemother. 2014;58(3):1546-55. doi: 10.1128/AAC.01746-13. Epub 2013 Dec 23.

36.

Human respiratory syncytial virus Memphis 37 grown in HEp-2 cells causes more severe disease in lambs than virus grown in Vero cells.

Derscheid RJ, van Geelen A, McGill JL, Gallup JM, Cihlar T, Sacco RE, Ackermann MR.

Viruses. 2013 Nov 22;5(11):2881-97. doi: 10.3390/v5112881.

37.

Non-catalytic site HIV-1 integrase inhibitors disrupt core maturation and induce a reverse transcription block in target cells.

Balakrishnan M, Yant SR, Tsai L, O'Sullivan C, Bam RA, Tsai A, Niedziela-Majka A, Stray KM, Sakowicz R, Cihlar T.

PLoS One. 2013 Sep 9;8(9):e74163. doi: 10.1371/journal.pone.0074163. eCollection 2013.

38.

Evaluation of the effect of cobicistat on the in vitro renal transport and cytotoxicity potential of tenofovir.

Stray KM, Bam RA, Birkus G, Hao J, Lepist EI, Yant SR, Ray AS, Cihlar T.

Antimicrob Agents Chemother. 2013 Oct;57(10):4982-9. doi: 10.1128/AAC.00712-13. Epub 2013 Jul 29.

39.

Mutations in adenosine deaminase-like (ADAL) protein confer resistance to the antiproliferative agents N6-cyclopropyl-PMEDAP and GS-9219.

Frey CR, Andrei G, Votruba I, Cannizzaro C, Han B, Fung W, Hung M, Liu X, Geleziunas R, Fiten P, Opdenakker G, Snoeck R, Cihlar T.

Anticancer Res. 2013 May;33(5):1899-912.

PMID:
23645737
40.

Mutations in multiple domains of Gag drive the emergence of in vitro resistance to the phosphonate-containing HIV-1 protease inhibitor GS-8374.

Stray KM, Callebaut C, Glass B, Tsai L, Xu L, Müller B, Kräusslich HG, Cihlar T.

J Virol. 2013 Jan;87(1):454-63. doi: 10.1128/JVI.01211-12. Epub 2012 Oct 24.

41.

Sugar-modified derivatives of cytostatic 7-(het)aryl-7-deazaadenosines: 2'-C-methylribonucleosides, 2'-deoxy-2'-fluoroarabinonucleosides, arabinonucleosides and 2'-deoxyribonucleosides.

Nauš P, Perlíková P, Bourderioux A, Pohl R, Slavětínská L, Votruba I, Bahador G, Birkuš G, Cihlář T, Hocek M.

Bioorg Med Chem. 2012 Sep 1;20(17):5202-14. doi: 10.1016/j.bmc.2012.07.003. Epub 2012 Jul 20.

PMID:
22877872
42.

Topical tenofovir, a microbicide effective against HIV, inhibits herpes simplex virus-2 replication.

Andrei G, Lisco A, Vanpouille C, Introini A, Balestra E, van den Oord J, Cihlar T, Perno CF, Snoeck R, Margolis L, Balzarini J.

Cell Host Microbe. 2011 Oct 20;10(4):379-89. doi: 10.1016/j.chom.2011.08.015.

43.

Synthesis and significant cytostatic activity of 7-hetaryl-7-deazaadenosines.

Bourderioux A, Naus P, Perlíková P, Pohl R, Pichová I, Votruba I, Dzubák P, Konecný P, Hajdúch M, Stray KM, Wang T, Ray AS, Feng JY, Birkus G, Cihlar T, Hocek M.

J Med Chem. 2011 Aug 11;54(15):5498-507. doi: 10.1021/jm2005173. Epub 2011 Jul 11.

PMID:
21711054
44.

A novel and efficient one-pot synthesis of symmetrical diamide (bis-amidate) prodrugs of acyclic nucleoside phosphonates and evaluation of their biological activities.

Jansa P, Baszczyňski O, Dračínský M, Votruba I, Zídek Z, Bahador G, Stepan G, Cihlar T, Mackman R, Holý A, Janeba Z.

Eur J Med Chem. 2011 Sep;46(9):3748-54. doi: 10.1016/j.ejmech.2011.05.040. Epub 2011 May 23.

PMID:
21664011
45.

Role of cathepsin A and lysosomes in the intracellular activation of novel antipapillomavirus agent GS-9191.

Birkus G, Kutty N, Frey CR, Shribata R, Chou T, Wagner C, McDermott M, Cihlar T.

Antimicrob Agents Chemother. 2011 May;55(5):2166-73. doi: 10.1128/AAC.01603-10. Epub 2011 Mar 7.

46.

In vitro characterization of GS-8374, a novel phosphonate-containing inhibitor of HIV-1 protease with a favorable resistance profile.

Callebaut C, Stray K, Tsai L, Williams M, Yang ZY, Cannizzaro C, Leavitt SA, Liu X, Wang K, Murray BP, Mulato A, Hatada M, Priskich T, Parkin N, Swaminathan S, Lee W, He GX, Xu L, Cihlar T.

Antimicrob Agents Chemother. 2011 Apr;55(4):1366-76. doi: 10.1128/AAC.01183-10. Epub 2011 Jan 18.

47.

GS-8374, a novel HIV protease inhibitor, does not alter glucose homeostasis in cultured adipocytes or in a healthy-rodent model system.

Hruz PW, Yan Q, Tsai L, Koster J, Xu L, Cihlar T, Callebaut C.

Antimicrob Agents Chemother. 2011 Apr;55(4):1377-82. doi: 10.1128/AAC.01184-10. Epub 2011 Jan 18.

48.

Phosphoramidate pronucleotides of cytostatic 6-aryl-7-deazapurine ribonucleosides.

Perlíková P, Pohl R, Votruba I, Shih R, Birkuš G, Cihlář T, Hocek M.

Bioorg Med Chem. 2011 Jan 1;19(1):229-42. doi: 10.1016/j.bmc.2010.11.029. Epub 2010 Dec 4.

PMID:
21134754
49.

Synthesis of ester prodrugs of 9-(S)-[3-hydroxy-2-(phosphonomethoxy)propyl]-2,6-diaminopurine (HPMPDAP) as anti-poxvirus agents.

Krecmerová M, Holý A, Andrei G, Pomeisl K, Tichý T, Brehová P, Masojídková M, Dracínský M, Pohl R, Laflamme G, Naesens L, Hui H, Cihlar T, Neyts J, De Clercq E, Balzarini J, Snoeck R.

J Med Chem. 2010 Oct 14;53(19):6825-37. doi: 10.1021/jm901828c.

PMID:
20809641
50.

CycloSal-phosphate pronucleotides of cytostatic 6-(Het)aryl-7-deazapurine ribonucleosides: Synthesis, cytostatic activity, and inhibition of adenosine kinases.

Spácilová P, Naus P, Pohl R, Votruba I, Snásel J, Zábranská H, Pichová I, Ameral R, Birkus G, Cihlár T, Hocek M.

ChemMedChem. 2010 Aug 2;5(8):1386-96. doi: 10.1002/cmdc.201000192.

PMID:
20533504

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