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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: price e. J Alzheimers Dis. 2005 Apr;7(2):139-48; discussion 173-80. doi: 10.3233/jad-2005-7207. J Alzheimers Dis. 2005. PMID: 15851852
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: price ea. 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.
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: price ea. J Med Chem. 2008 Oct 23;51(20):6259-62. doi: 10.1021/jm800914n. Epub 2008 Sep 24. J Med Chem. 2008. PMID: 18811140
In vivo beta-secretase 1 inhibition leads to brain Abeta lowering and increased alpha-secretase processing of amyloid precursor protein without effect on neuregulin-1.
Sankaranarayanan S, Price EA, Wu G, Crouthamel MC, Shi XP, Tugusheva K, Tyler KX, Kahana J, Ellis J, Jin L, Steele T, Stachel S, Coburn C, Simon AJ. Sankaranarayanan S, et al. J Pharmacol Exp Ther. 2008 Mar;324(3):957-69. doi: 10.1124/jpet.107.130039. Epub 2007 Dec 21. J Pharmacol Exp Ther. 2008. PMID: 18156464
Acute gamma-secretase inhibition of nonhuman primate CNS shifts amyloid precursor protein (APP) metabolism from amyloid-beta production to alternative APP fragments without amyloid-beta rebound.
Cook JJ, Wildsmith KR, Gilberto DB, Holahan MA, Kinney GG, Mathers PD, Michener MS, Price EA, Shearman MS, Simon AJ, Wang JX, Wu G, Yarasheski KE, Bateman RJ. Cook JJ, et al. Among authors: price ea. J Neurosci. 2010 May 12;30(19):6743-50. doi: 10.1523/JNEUROSCI.1381-10.2010. J Neurosci. 2010. PMID: 20463236 Free PMC article.
Rapid P1 SAR of brain penetrant tertiary carbinamine derived BACE inhibitors.
Zhu H, Young MB, Nantermet PG, Graham SL, Colussi D, Lai MT, Pietrak B, Price EA, Sankaranarayanan S, Shi XP, Tugusheva K, Holahan MA, Michener MS, Cook JJ, Simon A, Hazuda DJ, Vacca JP, Rajapakse HA. Zhu H, et al. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1779-82. doi: 10.1016/j.bmcl.2010.01.005. Epub 2010 Jan 11. Bioorg Med Chem Lett. 2010. PMID: 20122828
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. J Med Chem. 2006 Oct 19;49(21):6147-50. doi: 10.1021/jm060884i. J Med Chem. 2006. PMID: 17034118
1,310 results