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Items: 34

1.

Synthesis and Anti-HCV Activities of 4'-Fluoro-2'-Substituted Uridine Triphosphates and Nucleotide Prodrugs: Discovery of 4'-Fluoro-2'- C-methyluridine 5'-Phosphoramidate Prodrug (AL-335) for the Treatment of Hepatitis C Infection.

Wang G, Dyatkina N, Prhavc M, Williams C, Serebryany V, Hu Y, Huang Y, Wan J, Wu X, Deval J, Fung A, Jin Z, Tan H, Shaw K, Kang H, Zhang Q, Tam Y, Stoycheva A, Jekle A, Smith DB, Beigelman L.

J Med Chem. 2019 May 9;62(9):4555-4570. doi: 10.1021/acs.jmedchem.9b00143. Epub 2019 Apr 19.

PMID:
30951311
2.

Structure-activity relationship analysis of mitochondrial toxicity caused by antiviral ribonucleoside analogs.

Jin Z, Kinkade A, Behera I, Chaudhuri S, Tucker K, Dyatkina N, Rajwanshi VK, Wang G, Jekle A, Smith DB, Beigelman L, Symons JA, Deval J.

Antiviral Res. 2017 Jul;143:151-161. doi: 10.1016/j.antiviral.2017.04.005. Epub 2017 Apr 12.

3.

Synthesis and Anti-Influenza Activity of Pyridine, Pyridazine, and Pyrimidine C-Nucleosides as Favipiravir (T-705) Analogues.

Wang G, Wan J, Hu Y, Wu X, Prhavc M, Dyatkina N, Rajwanshi VK, Smith DB, Jekle A, Kinkade A, Symons JA, Jin Z, Deval J, Zhang Q, Tam Y, Chanda S, Blatt L, Beigelman L.

J Med Chem. 2016 May 26;59(10):4611-24. doi: 10.1021/acs.jmedchem.5b01933. Epub 2016 Apr 27.

PMID:
27120583
4.

Sulfonyl-polyol N,N-dichloroamines with rapid, broad-spectrum antimicrobial activity.

Shiau TP, Low E, Kim B, Turtle ED, Francavilla C, O'Mahony DJ, Friedman L, D'Lima L, Jekle A, Debabov D, Zuck M, Alvarez NJ, Anderson M, Najafi RR, Jain RK.

Bioorg Med Chem Lett. 2013 Oct 15;23(20):5650-3. doi: 10.1016/j.bmcl.2013.08.027. Epub 2013 Aug 17.

PMID:
23999044
5.

Broad-spectrum virucidal activity of (NVC-422) N,N-dichloro-2,2-dimethyltaurine against viral ocular pathogens in vitro.

Jekle A, Abdul Rani S, Celeri C, Zuck M, Xu P, Wang L, Najafi-Tagol K, Anderson M, Stroman D, Debabov D.

Invest Ophthalmol Vis Sci. 2013 Feb 19;54(2):1244-51. doi: 10.1167/iovs.12-10700.

PMID:
23341010
6.

NVC-422 inactivates Staphylococcus aureus toxins.

Jekle A, Yoon J, Zuck M, Najafi R, Wang L, Shiau T, Francavilla C, Rani SA, Eitzinger C, Nagl M, Anderson M, Debabov D.

Antimicrob Agents Chemother. 2013 Feb;57(2):924-9. doi: 10.1128/AAC.01945-12. Epub 2012 Dec 3.

7.

N-chlorotaurine and its analogues N,N-dichloro-2,2-dimethyltaurine and N-monochloro-2,2-dimethyltaurine are safe and effective bactericidal agents in ex vivo corneal infection models.

Teuchner B, Eitzinger C, Lutz M, Hager T, Schmid E, Bechrakis NE, Zuck M, Jekle A, Debabov D, Anderson M, Nagl M.

Acta Ophthalmol. 2012 Dec;90(8):e632-7. doi: 10.1111/j.1755-3768.2012.02501.x. Epub 2012 Sep 12.

8.

Efficacy of NVC-422 against Staphylococcus aureus biofilms in a sheep biofilm model of sinusitis.

Singhal D, Jekle A, Debabov D, Wang L, Khosrovi B, Anderson M, Foreman A, Wormald PJ.

Int Forum Allergy Rhinol. 2012 Jul-Aug;2(4):309-15. doi: 10.1002/alr.21038. Epub 2012 Mar 20.

PMID:
22434724
9.

Antimicrobial and anticoagulant activities of N-chlorotaurine, N,N-dichloro-2,2-dimethyltaurine, and N-monochloro-2,2-dimethyltaurine in human blood.

Martini C, Hammerer-Lercher A, Zuck M, Jekle A, Debabov D, Anderson M, Nagl M.

Antimicrob Agents Chemother. 2012 Apr;56(4):1979-84. doi: 10.1128/AAC.05685-11. Epub 2012 Jan 17.

10.

Virucidal mechanism of action of NVC-422, a novel antimicrobial drug for the treatment of adenoviral conjunctivitis.

Yoon J, Jekle A, Najafi R, Ruado F, Zuck M, Khosrovi B, Memarzadeh B, Debabov D, Wang L, Anderson M.

Antiviral Res. 2011 Dec;92(3):470-8. doi: 10.1016/j.antiviral.2011.10.009. Epub 2011 Oct 15.

PMID:
22024427
11.

Development of tetravalent, bispecific CCR5 antibodies with antiviral activity against CCR5 monoclonal antibody-resistant HIV-1 strains.

Schanzer J, Jekle A, Nezu J, Lochner A, Croasdale R, Dioszegi M, Zhang J, Hoffmann E, Dormeyer W, Stracke J, Schäfer W, Ji C, Heilek G, Cammack N, Brandt M, Umana P, Brinkmann U.

Antimicrob Agents Chemother. 2011 May;55(5):2369-78. doi: 10.1128/AAC.00215-10. Epub 2011 Feb 7.

12.

Evaluation of amide replacements in CCR5 antagonists as a means to increase intrinsic permeability. Part 2: SAR optimization and pharmacokinetic profile of a homologous azacyle series.

Wanner J, Chen L, Lemoine RC, Kondru R, Jekle A, Heilek G, deRosier A, Ji C, Berry PW, Rotstein DM.

Bioorg Med Chem Lett. 2010 Nov 15;20(22):6802-7. doi: 10.1016/j.bmcl.2010.08.118. Epub 2010 Sep 18.

PMID:
20855212
13.

Exploration of a new series of CCR5 antagonists: multi-dimensional optimization of a sub-series containing N-substituted pyrazoles.

Lemoine RC, Petersen AC, Setti L, Jekle A, Heilek G, deRosier A, Ji C, Berry P, Rotstein DM.

Bioorg Med Chem Lett. 2010 Aug 15;20(16):4753-6. doi: 10.1016/j.bmcl.2010.06.135. Epub 2010 Jul 1.

PMID:
20643548
14.

Biochemical characterization of the inhibition of the dengue virus RNA polymerase by beta-d-2'-ethynyl-7-deaza-adenosine triphosphate.

Latour DR, Jekle A, Javanbakht H, Henningsen R, Gee P, Lee I, Tran P, Ren S, Kutach AK, Harris SF, Wang SM, Lok SJ, Shaw D, Li J, Heilek G, Klumpp K, Swinney DC, Deval J.

Antiviral Res. 2010 Aug;87(2):213-22. doi: 10.1016/j.antiviral.2010.05.003. Epub 2010 May 12.

PMID:
20470829
15.

Synthesis, SAR and evaluation of [1,4']-bipiperidinyl-4-yl-imidazolidin-2-one derivatives as novel CCR5 antagonists.

Rotstein DM, Gabriel SD, Manser N, Filonova L, Padilla F, Sankuratri S, Ji C, deRosier A, Dioszegi M, Heilek G, Jekle A, Weller P, Berry P.

Bioorg Med Chem Lett. 2010 Jun 1;20(11):3219-22. doi: 10.1016/j.bmcl.2010.04.077. Epub 2010 Apr 22.

PMID:
20457517
16.

Novel hexahydropyrrolo[3,4-c]pyrrole CCR5 antagonists.

Rotstein DM, Melville CR, Padilla F, Cournoyer D, Lee EK, Lemoine R, Petersen AC, Setti LQ, Wanner J, Chen L, Filonova L, Loughhead DG, Manka J, Lin XF, Gleason S, Sankuratri S, Ji C, Derosier A, Dioszegi M, Heilek G, Jekle A, Berry P, Mau CI, Weller P.

Bioorg Med Chem Lett. 2010 May 15;20(10):3116-9. doi: 10.1016/j.bmcl.2010.03.095. Epub 2010 Mar 30.

PMID:
20417098
17.

Evaluation of a 4-aminopiperidine replacement in several series of CCR5 antagonists.

Lemoine RC, Petersen AC, Setti L, Chen L, Wanner J, Jekle A, Heilek G, deRosier A, Ji C, Rotstein DM.

Bioorg Med Chem Lett. 2010 Mar 15;20(6):1830-3. doi: 10.1016/j.bmcl.2010.02.004. Epub 2010 Feb 6.

PMID:
20176481
18.

Evaluation of a 3-amino-8-azabicyclo[3.2.1]octane replacement in the CCR5 antagonist maraviroc.

Lemoine RC, Petersen AC, Setti L, Baldinger T, Wanner J, Jekle A, Heilek G, deRosier A, Ji C, Rotstein DM.

Bioorg Med Chem Lett. 2010 Mar 1;20(5):1674-6. doi: 10.1016/j.bmcl.2010.01.080. Epub 2010 Jan 21.

PMID:
20137937
19.

Evaluation of secondary amide replacements in a series of CCR5 antagonists as a means to increase intrinsic membrane permeability. Part 1: Optimization of gem-disubstituted azacycles.

Lemoine RC, Petersen AC, Setti L, Wanner J, Jekle A, Heilek G, deRosier A, Ji C, Berry P, Rotstein D.

Bioorg Med Chem Lett. 2010 Jan 15;20(2):704-8. doi: 10.1016/j.bmcl.2009.11.072. Epub 2009 Dec 7.

PMID:
20004099
20.

Epitope switching as a novel escape mechanism of HIV to CCR5 monoclonal antibodies.

Jekle A, Chhabra M, Lochner A, Meier S, Chow E, Brandt M, Sankuratri S, Cammack N, Heilek G.

Antimicrob Agents Chemother. 2010 Feb;54(2):734-41. doi: 10.1128/AAC.00841-09. Epub 2009 Dec 7.

21.

Spiropiperidine CCR5 antagonists.

Rotstein DM, Gabriel SD, Makra F, Filonova L, Gleason S, Brotherton-Pleiss C, Setti LQ, Trejo-Martin A, Lee EK, Sankuratri S, Ji C, Derosier A, Dioszegi M, Heilek G, Jekle A, Berry P, Weller P, Mau CI.

Bioorg Med Chem Lett. 2009 Sep 15;19(18):5401-6. doi: 10.1016/j.bmcl.2009.07.122. Epub 2009 Jul 30.

PMID:
19674898
22.

CD4-BFFI: a novel, bifunctional HIV-1 entry inhibitor with high and broad antiviral potency.

Jekle A, Chow E, Kopetzki E, Ji C, Yan MJ, Nguyen R, Sankuratri S, Cammack N, Heilek G.

Antiviral Res. 2009 Sep;83(3):257-66. doi: 10.1016/j.antiviral.2009.06.005. Epub 2009 Jun 25.

PMID:
19559732
23.

CD4-anchoring HIV-1 fusion inhibitor with enhanced potency and in vivo stability.

Ji C, Kopetzki E, Jekle A, Stubenrauch KG, Liu X, Zhang J, Rao E, Schlothauer T, Fischer S, Cammack N, Heilek G, Ries S, Sankuratri S.

J Biol Chem. 2009 Feb 20;284(8):5175-85. doi: 10.1074/jbc.M808745200. Epub 2008 Dec 19.

24.

Closing two doors of viral entry: intramolecular combination of a coreceptor- and fusion inhibitor of HIV-1.

Kopetzki E, Jekle A, Ji C, Rao E, Zhang J, Fischer S, Cammack N, Sankuratri S, Heilek G.

Virol J. 2008 May 1;5:56. doi: 10.1186/1743-422X-5-56.

25.

Novel CCR5 monoclonal antibodies with potent and broad-spectrum anti-HIV activities.

Ji C, Brandt M, Dioszegi M, Jekle A, Schwoerer S, Challand S, Zhang J, Chen Y, Zautke L, Achhammer G, Baehner M, Kroetz S, Heilek-Snyder G, Schumacher R, Cammack N, Sankuratri S.

Antiviral Res. 2007 May;74(2):125-37. Epub 2006 Dec 5.

PMID:
17166600
26.

A novel potassium channel in lymphocyte mitochondria.

Szabò I, Bock J, Jekle A, Soddemann M, Adams C, Lang F, Zoratti M, Gulbins E.

J Biol Chem. 2005 Apr 1;280(13):12790-8. Epub 2005 Jan 4.

27.

In vivo evolution of human immunodeficiency virus type 1 toward increased pathogenicity through CXCR4-mediated killing of uninfected CD4 T cells.

Jekle A, Keppler OT, De Clercq E, Schols D, Weinstein M, Goldsmith MA.

J Virol. 2003 May;77(10):5846-54.

28.

Actinomycin D-induced apoptosis involves the potassium channel Kv1.3.

Bock J, Szabó I, Jekle A, Gulbins E.

Biochem Biophys Res Commun. 2002 Jul 12;295(2):526-31.

PMID:
12150982
29.

Coreceptor phenotype of natural human immunodeficiency virus with nef deleted evolves in vivo, leading to increased virulence.

Jekle A, Schramm B, Jayakumar P, Trautner V, Schols D, De Clercq E, Mills J, Crowe SM, Goldsmith MA.

J Virol. 2002 Jul;76(14):6966-73.

30.

CD95 signaling via ceramide-rich membrane rafts.

Grassme H, Jekle A, Riehle A, Schwarz H, Berger J, Sandhoff K, Kolesnick R, Gulbins E.

J Biol Chem. 2001 Jun 8;276(23):20589-96. Epub 2001 Mar 12.

31.

Physiology of apoptosis.

Gulbins E, Jekle A, Ferlinz K, Grassmé H, Lang F.

Am J Physiol Renal Physiol. 2000 Oct;279(4):F605-15. Review.

32.

CD95/CD95 ligand-mediated counterattack does not block T cell cytotoxicity.

Jekle A, Obst R, Lang F, Rammensee HG, Gulbins E.

Biochem Biophys Res Commun. 2000 Jun 7;272(2):395-9.

PMID:
10833425
33.

Stimulation of CD95 (Fas) blocks T lymphocyte calcium channels through sphingomyelinase and sphingolipids.

Lepple-Wienhues A, Belka C, Laun T, Jekle A, Walter B, Wieland U, Welz M, Heil L, Kun J, Busch G, Weller M, Bamberg M, Gulbins E, Lang F.

Proc Natl Acad Sci U S A. 1999 Nov 23;96(24):13795-800.

34.

The tyrosine kinase lck is required for CD95-independent caspase-8 activation and apoptosis in response to ionizing radiation.

Belka C, Marini P, Lepple-Wienhues A, Budach W, Jekle A, Los M, Lang F, Schulze-Osthoff K, Gulbins E, Bamberg M.

Oncogene. 1999 Sep 2;18(35):4983-92.

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