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Page 1
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. Rotstein DM, et al. Among authors: jekle a. Bioorg Med Chem Lett. 2009 Sep 15;19(18):5401-6. doi: 10.1016/j.bmcl.2009.07.122. Epub 2009 Jul 30. Bioorg Med Chem Lett. 2009. PMID: 19674898
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. Lemoine RC, et al. Among authors: jekle a. Bioorg Med Chem Lett. 2010 Jan 15;20(2):704-8. doi: 10.1016/j.bmcl.2009.11.072. Epub 2009 Dec 7. Bioorg Med Chem Lett. 2010. PMID: 20004099
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. Rotstein DM, et al. Among authors: jekle a. Bioorg Med Chem Lett. 2010 May 15;20(10):3116-9. doi: 10.1016/j.bmcl.2010.03.095. Epub 2010 Mar 30. Bioorg Med Chem Lett. 2010. PMID: 20417098
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. Wanner J, et al. Among authors: jekle a. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6802-7. doi: 10.1016/j.bmcl.2010.08.118. Epub 2010 Sep 18. Bioorg Med Chem Lett. 2010. PMID: 20855212
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. Ji C, et al. Among authors: jekle a. Antiviral Res. 2007 May;74(2):125-37. doi: 10.1016/j.antiviral.2006.11.003. Epub 2006 Dec 5. Antiviral Res. 2007. PMID: 17166600
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. Ji C, et al. Among authors: jekle a. J Biol Chem. 2009 Feb 20;284(8):5175-85. doi: 10.1074/jbc.M808745200. Epub 2008 Dec 19. J Biol Chem. 2009. PMID: 19097993 Free article.
Previously, we have reported a CCR5 antibody-based bifunctional HIV-1 fusion inhibitor (BFFI) that was highly active in blocking R5 HIV-1 infection but was ineffective against X4 viruses infecting human PBMCs (Kopetzki, E., Jekle, A., Ji, C., Rao, E., Zhang, …
Previously, we have reported a CCR5 antibody-based bifunctional HIV-1 fusion inhibitor (BFFI) that was highly active in blocking R5 H …
43 results