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Page 1
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. 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.
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. J Alzheimers Dis. 2005 Apr;7(2):139-48; discussion 173-80. doi: 10.3233/jad-2005-7207. J Alzheimers Dis. 2005. PMID: 15851852
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. 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
LRRTM3 promotes processing of amyloid-precursor protein by BACE1 and is a positional candidate gene for late-onset Alzheimer's disease.
Majercak J, Ray WJ, Espeseth A, Simon A, Shi XP, Wolffe C, Getty K, Marine S, Stec E, Ferrer M, Strulovici B, Bartz S, Gates A, Xu M, Huang Q, Ma L, Shughrue P, Burchard J, Colussi D, Pietrak B, Kahana J, Beher D, Rosahl T, Shearman M, Hazuda D, Sachs AB, Koblan KS, Seabrook GR, Stone DJ. Majercak J, et al. Proc Natl Acad Sci U S A. 2006 Nov 21;103(47):17967-72. doi: 10.1073/pnas.0605461103. Epub 2006 Nov 10. Proc Natl Acad Sci U S A. 2006. PMID: 17098871 Free PMC article.
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: espeseth as. J Med Chem. 2004 Dec 16;47(26):6447-50. doi: 10.1021/jm049379g. J Med Chem. 2004. PMID: 15588077
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: espeseth as. 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: espeseth as. J Med Chem. 2006 Oct 19;49(21):6147-50. doi: 10.1021/jm060884i. J Med Chem. 2006. PMID: 17034118
Discovery of oxadiazoyl tertiary carbinamine inhibitors of beta-secretase (BACE-1).
Rajapakse HA, Nantermet PG, Selnick HG, Munshi S, McGaughey GB, Lindsley SR, Young MB, Lai MT, Espeseth AS, Shi XP, Colussi D, Pietrak B, Crouthamel MC, Tugusheva K, Huang Q, Xu M, Simon AJ, Kuo L, Hazuda DJ, Graham S, Vacca JP. Rajapakse HA, et al. Among authors: espeseth as. J Med Chem. 2006 Dec 14;49(25):7270-3. doi: 10.1021/jm061046r. J Med Chem. 2006. PMID: 17149856
Discovery and X-ray crystallographic analysis of a spiropiperidine iminohydantoin inhibitor of beta-secretase.
Barrow JC, Stauffer SR, Rittle KE, Ngo PL, Yang Z, Selnick HG, Graham SL, Munshi S, McGaughey GB, Holloway MK, Simon AJ, Price EA, Sankaranarayanan S, Colussi D, Tugusheva K, Lai MT, Espeseth AS, Xu M, Huang Q, Wolfe A, Pietrak B, Zuck P, Levorse DA, Hazuda D, Vacca JP. Barrow JC, et al. Among authors: espeseth as. J Med Chem. 2008 Oct 23;51(20):6259-62. doi: 10.1021/jm800914n. Epub 2008 Sep 24. J Med Chem. 2008. PMID: 18811140
68 results