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Items: 18

1.

Methyl-substitution of an iminohydantoin spiropiperidine β-secretase (BACE-1) inhibitor has a profound effect on its potency.

Egbertson M, McGaughey GB, Pitzenberger SM, Stauffer SR, Coburn CA, Stachel SJ, Yang W, Barrow JC, Neilson LA, McWherter M, Perlow D, Fahr B, Munshi S, Allison TJ, Holloway K, Selnick HG, Yang Z, Swestock J, Simon AJ, Sankaranarayanan S, Colussi D, Tugusheva K, Lai MT, Pietrak B, Haugabook S, Jin L, Chen IW, Holahan M, Stranieri-Michener M, Cook JJ, Vacca J, Graham SL.

Bioorg Med Chem Lett. 2015 Nov 1;25(21):4812-4819. doi: 10.1016/j.bmcl.2015.06.082. Epub 2015 Jun 29.

PMID:
26195137
2.

Intracellular clusterin interacts with brain isoforms of the bridging integrator 1 and with the microtubule-associated protein Tau in Alzheimer's disease.

Zhou Y, Hayashi I, Wong J, Tugusheva K, Renger JJ, Zerbinatti C.

PLoS One. 2014 Jul 22;9(7):e103187. doi: 10.1371/journal.pone.0103187. eCollection 2014.

3.

A sensitive aβ oligomer assay discriminates Alzheimer's and aged control cerebrospinal fluid.

Savage MJ, Kalinina J, Wolfe A, Tugusheva K, Korn R, Cash-Mason T, Maxwell JW, Hatcher NG, Haugabook SJ, Wu G, Howell BJ, Renger JJ, Shughrue PJ, McCampbell A.

J Neurosci. 2014 Feb 19;34(8):2884-97. doi: 10.1523/JNEUROSCI.1675-13.2014.

4.

Characterization of plasma β-secretase (BACE1) activity and soluble amyloid precursor proteins as potential biomarkers for Alzheimer's disease.

Wu G, Sankaranarayanan S, Wong J, Tugusheva K, Michener MS, Shi X, Cook JJ, Simon AJ, Savage MJ.

J Neurosci Res. 2012 Dec;90(12):2247-58. doi: 10.1002/jnr.23122. Epub 2012 Sep 18.

PMID:
22987781
5.

SAR of tertiary carbinamine derived BACE1 inhibitors: role of aspartate ligand amine pKa in enzyme inhibition.

Rajapakse HA, Nantermet PG, Selnick HG, Barrow JC, McGaughey GB, Munshi S, Lindsley SR, Young MB, Ngo PL, Holloway MK, 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.

Bioorg Med Chem Lett. 2010 Mar 15;20(6):1885-9. doi: 10.1016/j.bmcl.2010.01.137. Epub 2010 Feb 4.

PMID:
20176482
6.

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.

Bioorg Med Chem Lett. 2010 Mar 1;20(5):1779-82. doi: 10.1016/j.bmcl.2010.01.005. Epub 2010 Jan 11.

PMID:
20122828
7.

Identification of a small molecule beta-secretase inhibitor that binds without catalytic aspartate engagement.

Steele TG, Hills ID, Nomland AA, de León P, Allison T, McGaughey G, Colussi D, Tugusheva K, Haugabook SJ, Espeseth AS, Zuck P, Graham SL, Stachel SJ.

Bioorg Med Chem Lett. 2009 Jan 1;19(1):17-20. doi: 10.1016/j.bmcl.2008.11.027. Epub 2008 Nov 13.

PMID:
19036583
8.

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.

J Pharmacol Exp Ther. 2009 Jan;328(1):131-40. doi: 10.1124/jpet.108.143628. Epub 2008 Oct 14.

9.

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.

J Med Chem. 2008 Oct 23;51(20):6259-62. doi: 10.1021/jm800914n. Epub 2008 Sep 24.

PMID:
18811140
10.

Decrease in age-adjusted cerebrospinal fluid beta-secretase activity in Alzheimer's subjects.

Wu G, Sankaranarayanan S, Tugusheva K, Kahana J, Seabrook G, Shi XP, King E, Devanarayan V, Cook JJ, Simon AJ.

Clin Biochem. 2008 Aug;41(12):986-96. doi: 10.1016/j.clinbiochem.2008.04.022. Epub 2008 May 6.

PMID:
18489907
11.

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.

J Pharmacol Exp Ther. 2008 Mar;324(3):957-69. Epub 2007 Dec 21.

12.

Design and synthesis of 2,3,5-substituted imidazolidin-4-one inhibitors of BACE-1.

Barrow JC, Rittle KE, Ngo PL, Selnick HG, Graham SL, Pitzenberger SM, McGaughey GB, Colussi D, Lai MT, Huang Q, Tugusheva K, Espeseth AS, Simon AJ, Munshi SK, Vacca JP.

ChemMedChem. 2007 Jul;2(7):995-9. No abstract available.

PMID:
17458843
13.

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.

J Med Chem. 2006 Dec 14;49(25):7270-3.

PMID:
17149856
14.

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.

Anal Biochem. 2005 Jul 1;342(1):144-51.

PMID:
15958191
15.

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.

J Alzheimers Dis. 2005 Apr;7(2):139-48; discussion 173-80.

PMID:
15851852
16.

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.

J Biol Chem. 2005 May 6;280(18):17792-7. Epub 2005 Feb 25.

17.

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.

J Med Chem. 2004 Dec 16;47(26):6447-50.

PMID:
15588077
18.

Beta-secretase cleavage at amino acid residue 34 in the amyloid beta peptide is dependent upon gamma-secretase activity.

Shi XP, Tugusheva K, Bruce JE, Lucka A, Wu GX, Chen-Dodson E, Price E, Li Y, Xu M, Huang Q, Sardana MK, Hazuda DJ.

J Biol Chem. 2003 Jun 6;278(23):21286-94. Epub 2003 Mar 27.

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