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Page 1
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
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.
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: price ea. J Med Chem. 2006 Oct 19;49(21):6147-50. doi: 10.1021/jm060884i. J Med Chem. 2006. PMID: 17034118
Design, synthesis, and SAR of macrocyclic tertiary carbinamine BACE-1 inhibitors.
Lindsley SR, Moore KP, Rajapakse HA, Selnick HG, Young MB, Zhu H, Munshi S, Kuo L, McGaughey GB, Colussi D, Crouthamel MC, Lai MT, Pietrak B, Price EA, Sankaranarayanan S, Simon AJ, Seabrook GR, Hazuda DJ, Pudvah NT, Hochman JH, Graham SL, Vacca JP, Nantermet PG. Lindsley SR, et al. Among authors: price ea. Bioorg Med Chem Lett. 2007 Jul 15;17(14):4057-61. doi: 10.1016/j.bmcl.2007.04.072. Epub 2007 Apr 27. Bioorg Med Chem Lett. 2007. PMID: 17482814
Discovery of isonicotinamide derived beta-secretase inhibitors: in vivo reduction of beta-amyloid.
Stanton MG, Stauffer SR, Gregro AR, Steinbeiser M, Nantermet P, Sankaranarayanan S, Price EA, Wu G, Crouthamel MC, Ellis J, Lai MT, Espeseth AS, Shi XP, Jin L, Colussi D, Pietrak B, Huang Q, Xu M, Simon AJ, Graham SL, Vacca JP, Selnick H. Stanton MG, et al. Among authors: price ea. J Med Chem. 2007 Jul 26;50(15):3431-3. doi: 10.1021/jm070272d. Epub 2007 Jun 21. J Med Chem. 2007. PMID: 17583334
Strategies toward improving the brain penetration of macrocyclic tertiary carbinamine BACE-1 inhibitors.
Moore KP, Zhu H, Rajapakse HA, McGaughey GB, Colussi D, Price EA, Sankaranarayanan S, Simon AJ, Pudvah NT, Hochman JH, Allison T, Munshi SK, Graham SL, Vacca JP, Nantermet PG. Moore KP, et al. Among authors: price ea. Bioorg Med Chem Lett. 2007 Nov 1;17(21):5831-5. doi: 10.1016/j.bmcl.2007.08.040. Epub 2007 Aug 23. Bioorg Med Chem Lett. 2007. PMID: 17827011
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: price ea. 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
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. Among authors: price ea. 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
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. Among authors: price ea. 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
73 results