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Page 1
Enhancement of alpha -helicity in the HIV-1 inhibitory peptide DP178 leads to an increased affinity for human monoclonal antibody 2F5 but does not elicit neutralizing responses in vitro. Implications for vaccine design.
Joyce JG, Hurni WM, Bogusky MJ, Garsky VM, Liang X, Citron MP, Danzeisen RC, Miller MD, Shiver JW, Keller PM. Joyce JG, et al. J Biol Chem. 2002 Nov 29;277(48):45811-20. doi: 10.1074/jbc.M205862200. Epub 2002 Sep 16. J Biol Chem. 2002. PMID: 12237296 Free article.
CCR5 antagonists: bicyclic isoxazolidines as conformationally constrained N-1-substituted pyrrolidines.
Lynch CL, Gentry AL, Hale JJ, Mills SG, MacCoss M, Malkowitz L, Springer MS, Gould SL, DeMartino JA, Siciliano SJ, Cascieri MA, Doss G, Carella A, Carver G, Holmes K, Schleif WA, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller M, Emini EA. Lynch CL, et al. Among authors: danzeisen r. Bioorg Med Chem Lett. 2002 Feb 25;12(4):677-9. doi: 10.1016/s0960-894x(01)00835-6. Bioorg Med Chem Lett. 2002. PMID: 11844699
1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 3: polar functionality and its effect on anti-HIV-1 activity.
Hale JJ, Budhu RJ, Mills SG, MacCoss M, Gould SL, DeMartino JA, Springer MS, Siciliano SJ, Malkowitz L, Schleif WA, Hazuda D, Miller M, Kessler J, Danzeisen R, Holmes K, Lineberger J, Carella A, Carver G, Emini EA. Hale JJ, et al. Among authors: danzeisen r. Bioorg Med Chem Lett. 2002 Oct 21;12(20):2997-3000. doi: 10.1016/s0960-894x(02)00605-4. Bioorg Med Chem Lett. 2002. PMID: 12270192
1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 4: synthesis of N-1 acidic functionality affording analogues with enhanced antiviral activity against HIV.
Lynch CL, Hale JJ, Budhu RJ, Gentry AL, Mills SG, Chapman KT, MacCoss M, Malkowitz L, Springer MS, Gould SL, DeMartino JA, Siciliano SJ, Cascieri MA, Carella A, Carver G, Holmes K, Schleif WA, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller M, Emini EA. Lynch CL, et al. Among authors: danzeisen r. Bioorg Med Chem Lett. 2002 Oct 21;12(20):3001-4. doi: 10.1016/s0960-894x(02)00606-6. Bioorg Med Chem Lett. 2002. PMID: 12270193
Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 1: Discovery and SAR study of 4-pyrazolylpiperidine side chains.
Shen DM, Shu M, Mills SG, Chapman KT, Malkowitz L, Springer MS, Gould SL, DeMartino JA, Siciliano SJ, Kwei GY, Carella A, Carver G, Holmes K, Schleif WA, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller MD, Emini EA. Shen DM, et al. Among authors: danzeisen r. Bioorg Med Chem Lett. 2004 Feb 23;14(4):935-9. doi: 10.1016/j.bmcl.2003.12.004. Bioorg Med Chem Lett. 2004. PMID: 15012997
Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 2: Discovery of potent, selective, and orally bioavailable compounds.
Shen DM, Shu M, Willoughby CA, Shah S, Lynch CL, Hale JJ, Mills SG, Chapman KT, Malkowitz L, Springer MS, Gould SL, DeMartino JA, Siciliano SJ, Lyons K, Pivnichny JV, Kwei GY, Carella A, Carver G, Holmes K, Schleif WA, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller MD, Emini EA. Shen DM, et al. Among authors: danzeisen r. Bioorg Med Chem Lett. 2004 Feb 23;14(4):941-5. doi: 10.1016/j.bmcl.2003.12.005. Bioorg Med Chem Lett. 2004. PMID: 15012998
Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 3: SAR studies on the benzylpyrazole segment.
Shu M, Loebach JL, Parker KA, Mills SG, Chapman KT, Shen DM, Malkowitz L, Springer MS, Gould SL, DeMartino JA, Siciliano SJ, Salvo JD, Lyons K, Pivnichny JV, Kwei GY, Carella A, Carver G, Holmes K, Schleif WA, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller MD, Emini EA. Shu M, et al. Among authors: danzeisen r. Bioorg Med Chem Lett. 2004 Feb 23;14(4):947-52. doi: 10.1016/j.bmcl.2003.12.006. Bioorg Med Chem Lett. 2004. PMID: 15012999
Syntheses and biological evaluation of 5-(piperidin-1-yl)-3-phenyl-pentylsulfones as CCR5 antagonists.
Shankaran K, Donnelly KL, Shah SK, Caldwell CG, Chen P, Finke PE, Oates B, MacCoss M, Mills SG, DeMartino JA, Gould SL, Malkowitz L, Siciliano SJ, Springer MS, Kwei G, Carella A, Carver G, Danzeisen R, Hazuda D, Holmes K, Kessler J, Lineberger J, Miller MD, Emini EA, Schleif WA. Shankaran K, et al. Among authors: danzeisen r. Bioorg Med Chem Lett. 2004 Jul 5;14(13):3589-93. doi: 10.1016/j.bmcl.2004.03.112. Bioorg Med Chem Lett. 2004. PMID: 15177481
52 results