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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: heilek g. 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, J., Fischer, S., Camm …
Previously, we have reported a CCR5 antibody-based bifunctional HIV-1 fusion inhibitor (BFFI) that was highly active in blocking R5 HIV-1 in …
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. Jekle A, et al. Among authors: heilek g. Antimicrob Agents Chemother. 2010 Feb;54(2):734-41. doi: 10.1128/AAC.00841-09. Epub 2009 Dec 7. Antimicrob Agents Chemother. 2010. PMID: 19995923 Free PMC article.
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. Schanzer J, et al. Among authors: heilek g. Antimicrob Agents Chemother. 2011 May;55(5):2369-78. doi: 10.1128/AAC.00215-10. Epub 2011 Feb 7. Antimicrob Agents Chemother. 2011. PMID: 21300827 Free PMC article.
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: heilek g. 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: heilek g. 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: heilek g. 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
40 results