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Page 1
BACE-1 inhibition by a series of psi[CH2NH] reduced amide isosteres.
Coburn CA, Stachel SJ, Jones KG, Steele TG, Rush DM, DiMuzio J, Pietrak BL, Lai MT, Huang Q, Lineberger J, Jin L, Munshi S, Katharine Holloway M, Espeseth A, Simon A, Hazuda D, Graham SL, Vacca JP. Coburn CA, et al. Among authors: lineberger j. Bioorg Med Chem Lett. 2006 Jul 15;16(14):3635-8. doi: 10.1016/j.bmcl.2006.04.076. Epub 2006 May 11. Bioorg Med Chem Lett. 2006. PMID: 16690314
Structure-based design of potent and selective cell-permeable inhibitors of human beta-secretase (BACE-1).
Stachel SJ, Coburn CA, Steele TG, Jones KG, Loutzenhiser EF, Gregro AR, Rajapakse HA, Lai MT, Crouthamel MC, Xu M, Tugusheva K, Lineberger JE, Pietrak BL, Espeseth AS, Shi XP, Chen-Dodson E, Holloway MK, Munshi S, Simon AJ, Kuo L, Vacca JP. Stachel SJ, et al. Among authors: lineberger je. J Med Chem. 2004 Dec 16;47(26):6447-50. doi: 10.1021/jm049379g. J Med Chem. 2004. PMID: 15588077
Compounds that bind APP and inhibit Abeta processing in vitro suggest a novel approach to Alzheimer disease therapeutics.
Espeseth AS, Xu M, Huang Q, Coburn CA, Jones KL, Ferrer M, Zuck PD, Strulovici B, Price EA, Wu G, Wolfe AL, Lineberger JE, Sardana M, Tugusheva K, Pietrak BL, Crouthamel MC, Lai MT, Dodson EC, Bazzo R, Shi XP, Simon AJ, Li Y, Hazuda DJ. Espeseth AS, et al. Among authors: lineberger je. J Biol Chem. 2005 May 6;280(18):17792-7. doi: 10.1074/jbc.M414331200. Epub 2005 Feb 25. J Biol Chem. 2005. PMID: 15737955 Free article.
Biochemical and cell-based assays for characterization of BACE-1 inhibitors.
Pietrak BL, Crouthamel MC, Tugusheva K, Lineberger JE, Xu M, DiMuzio JM, Steele T, Espeseth AS, Stachel SJ, Coburn CA, Graham SL, Vacca JP, Shi XP, Simon AJ, Hazuda DJ, Lai MT. Pietrak BL, et al. Among authors: lineberger je. Anal Biochem. 2005 Jul 1;342(1):144-51. doi: 10.1016/j.ab.2005.04.019. Anal Biochem. 2005. PMID: 15958191
Macrocyclic inhibitors of beta-secretase: functional activity in an animal model.
Stachel SJ, Coburn CA, Sankaranarayanan S, Price EA, Wu G, Crouthamel M, Pietrak BL, Huang Q, Lineberger J, Espeseth AS, Jin L, Ellis J, Holloway MK, Munshi S, Allison T, Hazuda D, Simon AJ, Graham SL, Vacca JP. Stachel SJ, et al. Among authors: lineberger j. J Med Chem. 2006 Oct 19;49(21):6147-50. doi: 10.1021/jm060884i. J Med Chem. 2006. PMID: 17034118
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: lineberger j. 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
Syntheses and SAR studies of 4-(heteroarylpiperdin-1-yl-methyl)-pyrrolidin-1-yl-acetic acid antagonists of the human CCR5 chemokine receptor.
Shankaran K, Donnelly KL, Shah SK, Guthikonda RN, MacCoss M, Mills SG, Gould SL, Malkowitz L, Siciliano SJ, Springer MS, Carella A, Carver G, Hazuda D, Holmes K, Kessler J, Lineberger J, Miller MD, Emini EA, Schleif WA. Shankaran K, et al. Among authors: lineberger j. Bioorg Med Chem Lett. 2004 Jul 5;14(13):3419-24. doi: 10.1016/j.bmcl.2004.04.078. Bioorg Med Chem Lett. 2004. PMID: 15177445
First demonstration of cerebrospinal fluid and plasma A beta lowering with oral administration of a beta-site amyloid precursor protein-cleaving enzyme 1 inhibitor in nonhuman primates.
Sankaranarayanan S, Holahan MA, Colussi D, Crouthamel MC, Devanarayan V, Ellis J, Espeseth A, Gates AT, Graham SL, Gregro AR, Hazuda D, Hochman JH, Holloway K, Jin L, Kahana J, Lai MT, Lineberger J, McGaughey G, Moore KP, Nantermet P, Pietrak B, Price EA, Rajapakse H, Stauffer S, Steinbeiser MA, Seabrook G, Selnick HG, Shi XP, Stanton MG, Swestock J, Tugusheva K, Tyler KX, Vacca JP, Wong J, Wu G, Xu M, Cook JJ, Simon AJ. Sankaranarayanan S, et al. Among authors: lineberger j. J Pharmacol Exp Ther. 2009 Jan;328(1):131-40. doi: 10.1124/jpet.108.143628. Epub 2008 Oct 14. J Pharmacol Exp Ther. 2009. PMID: 18854490
Novel mutations introduced at the beta-site of amyloid beta protein precursor enhance the production of amyloid beta peptide by BACE1 in vitro and in cells.
Shi XP, Tugusheva K, Bruce JE, Lucka A, Chen-Dodson E, Hu B, Wu GX, Price E, Register RB, Lineberger J, Miller R, Tang MJ, Espeseth A, Kahana J, Wolfe A, Crouthamel MC, Sankaranarayanan S, Simon A, Chen L, Lai MT, Pietrak B, DiMuzio J, Li Y, Xu M, Huang Q, Garsky V, Sardana MK, Hazuda DJ. Shi XP, et al. Among authors: lineberger j. J Alzheimers Dis. 2005 Apr;7(2):139-48; discussion 173-80. doi: 10.3233/jad-2005-7207. J Alzheimers Dis. 2005. PMID: 15851852
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: lineberger j. 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
42 results