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Items: 1 to 20 of 107

1.

Discovery and Evaluation of BMS-708163, a Potent, Selective and Orally Bioavailable γ-Secretase Inhibitor.

Gillman KW, Starrett JE Jr, Parker MF, Xie K, Bronson JJ, Marcin LR, McElhone KE, Bergstrom CP, Mate RA, Williams R, Meredith JE Jr, Burton CR, Barten DM, Toyn JH, Roberts SB, Lentz KA, Houston JG, Zaczek R, Albright CF, Decicco CP, Macor JE, Olson RE.

ACS Med Chem Lett. 2010 Mar 22;1(3):120-4. doi: 10.1021/ml1000239. eCollection 2010 Jun 10.

2.

Discovery of BIIB042, a Potent, Selective, and Orally Bioavailable γ-Secretase Modulator.

Peng H, Talreja T, Xin Z, Cuervo JH, Kumaravel G, Humora MJ, Xu L, Rohde E, Gan L, Jung MY, Shackett MN, Chollate S, Dunah AW, Snodgrass-Belt PA, Arnold HM, Taveras AG, Rhodes KJ, Scannevin RH.

ACS Med Chem Lett. 2011 Aug 5;2(10):786-91. doi: 10.1021/ml200175q. eCollection 2011 Oct 13.

3.

Pharmacodynamics of selective inhibition of γ-secretase by avagacestat.

Albright CF, Dockens RC, Meredith JE Jr, Olson RE, Slemmon R, Lentz KA, Wang JS, Denton RR, Pilcher G, Rhyne PW, Raybon JJ, Barten DM, Burton C, Toyn JH, Sankaranarayanan S, Polson C, Guss V, White R, Simutis F, Sanderson T, Gillman KW, Starrett JE Jr, Bronson J, Sverdlov O, Huang SP, Castaneda L, Feldman H, Coric V, Zaczek R, Macor JE, Houston J, Berman RM, Tong G.

J Pharmacol Exp Ther. 2013 Mar;344(3):686-95. doi: 10.1124/jpet.112.199356. Epub 2012 Dec 28.

4.

Discovery of SCH 900229, a Potent Presenilin 1 Selective γ-Secretase Inhibitor for the Treatment of Alzheimer's Disease.

Wu WL, Domalski M, Burnett DA, Josien H, Bara T, Rajagopalan M, Xu R, Clader J, Greenlee WJ, Brunskill A, Hyde LA, Del Vecchio RA, Cohen-Williams ME, Song L, Lee J, Terracina G, Zhang Q, Nomeir A, Parker EM, Zhang L.

ACS Med Chem Lett. 2012 Apr 9;3(11):892-6. doi: 10.1021/ml300044f. eCollection 2012 Nov 8.

5.

Begacestat (GSI-953): a novel, selective thiophene sulfonamide inhibitor of amyloid precursor protein gamma-secretase for the treatment of Alzheimer's disease.

Martone RL, Zhou H, Atchison K, Comery T, Xu JZ, Huang X, Gong X, Jin M, Kreft A, Harrison B, Mayer SC, Aschmies S, Gonzales C, Zaleska MM, Riddell DR, Wagner E, Lu P, Sun SC, Sonnenberg-Reines J, Oganesian A, Adkins K, Leach MW, Clarke DW, Huryn D, Abou-Gharbia M, Magolda R, Bard J, Frick G, Raje S, Forlow SB, Balliet C, Burczynski ME, Reinhart PH, Wan HI, Pangalos MN, Jacobsen JS.

J Pharmacol Exp Ther. 2009 Nov;331(2):598-608. doi: 10.1124/jpet.109.152975. Epub 2009 Aug 11.

6.

Modulation of γ-secretase by EVP-0015962 reduces amyloid deposition and behavioral deficits in Tg2576 mice.

Rogers K, Felsenstein KM, Hrdlicka L, Tu Z, Albayya F, Lee W, Hopp S, Miller MJ, Spaulding D, Yang Z, Hodgdon H, Nolan S, Wen M, Costa D, Blain JF, Freeman E, De Strooper B, Vulsteke V, Scrocchi L, Zetterberg H, Portelius E, Hutter-Paier B, Havas D, Ahlijanian M, Flood D, Leventhal L, Shapiro G, Patzke H, Chesworth R, Koenig G.

Mol Neurodegener. 2012 Dec 18;7:61. doi: 10.1186/1750-1326-7-61.

7.

Reductions in beta-amyloid concentrations in vivo by the gamma-secretase inhibitors BMS-289948 and BMS-299897.

Anderson JJ, Holtz G, Baskin PP, Turner M, Rowe B, Wang B, Kounnas MZ, Lamb BT, Barten D, Felsenstein K, McDonald I, Srinivasan K, Munoz B, Wagner SL.

Biochem Pharmacol. 2005 Feb 15;69(4):689-98. Epub 2005 Jan 7.

PMID:
15670587
8.

Amyloid precursor protein selective gamma-secretase inhibitors for treatment of Alzheimer's disease.

Basi GS, Hemphill S, Brigham EF, Liao A, Aubele DL, Baker J, Barbour R, Bova M, Chen XH, Dappen MS, Eichenbaum T, Goldbach E, Hawkinson J, Lawler-Herbold R, Hu K, Hui T, Jagodzinski JJ, Keim PS, Kholodenko D, Latimer LH, Lee M, Marugg J, Mattson MN, McCauley S, Miller JL, Motter R, Mutter L, Neitzel ML, Ni H, Nguyen L, Quinn K, Ruslim L, Semko CM, Shapiro P, Smith J, Soriano F, Szoke B, Tanaka K, Tang P, Tucker JA, Ye XM, Yu M, Wu J, Xu YZ, Garofalo AW, Sauer JM, Konradi AW, Ness D, Shopp G, Pleiss MA, Freedman SB, Schenk D.

Alzheimers Res Ther. 2010 Dec 29;2(6):36. doi: 10.1186/alzrt60.

9.

Quantitative assessment of Aβ peptide in brain, cerebrospinal fluid and plasma following oral administration of γ-secretase inhibitor MRK-560 in rats.

Wu G, Wu Z, Na S, Hershey JC.

Int J Neurosci. 2015;125(8):616-24. doi: 10.3109/00207454.2014.952730. Epub 2015 Apr 28.

PMID:
25567290
10.

Dynamics of {beta}-amyloid reductions in brain, cerebrospinal fluid, and plasma of {beta}-amyloid precursor protein transgenic mice treated with a {gamma}-secretase inhibitor.

Barten DM, Guss VL, Corsa JA, Loo A, Hansel SB, Zheng M, Munoz B, Srinivasan K, Wang B, Robertson BJ, Polson CT, Wang J, Roberts SB, Hendrick JP, Anderson JJ, Loy JK, Denton R, Verdoorn TA, Smith DW, Felsenstein KM.

J Pharmacol Exp Ther. 2005 Feb;312(2):635-43. Epub 2004 Sep 27.

11.

Orally bioavailable and brain-penetrant pyridazine and pyridine-derived γ-secretase modulators reduced amyloidogenic Aβ peptides in vivo.

Huang Y, Li T, Eatherton A, Mitchell WL, Rong N, Ye L, Yang XJ, Jin S, Ding Y, Zhang J, Li Y, Wu Y, Jin Y, Sang Y, Cheng Z, Browne ER, Harrison DC, Hussain I, Wan Z, Hall A, Lau LF, Matsuoka Y.

Neuropharmacology. 2013 Jul;70:278-86. doi: 10.1016/j.neuropharm.2013.02.003. Epub 2013 Feb 26.

PMID:
23485401
12.

BIIB042, a novel γ-secretase modulator, reduces amyloidogenic Aβ isoforms in primates and rodents and plaque pathology in a mouse model of Alzheimer's disease.

Scannevin RH, Chollate S, Brennan MS, Snodgrass-Belt PA, Peng H, Xu L, Jung MY, Bussiere T, Arastu MF, Talreja T, Xin Z, Dunstan RW, Fahrer D, Rohde E, Dunah AW, Wang J, Kumaravel G, Taveras AG, Moore Arnold H, Rhodes KJ.

Neuropharmacology. 2016 Apr;103:57-68. doi: 10.1016/j.neuropharm.2015.12.006. Epub 2015 Dec 12.

PMID:
26690893
13.

A Potent and Orally Efficacious, Hydroxyethylamine-Based Inhibitor of β-Secretase.

Kaller MR, Harried SS, Albrecht B, Amarante P, Babu-Khan S, Bartberger MD, Brown J, Brown R, Chen K, Cheng Y, Citron M, Croghan MD, Graceffa R, Hickman D, Judd T, Kriemen C, La D, Li V, Lopez P, Luo Y, Masse C, Monenschein H, Nguyen T, Pennington LD, Miguel TS, Sickmier EA, Wahl RC, Weiss MM, Wen PH, Williamson T, Wood S, Xue M, Yang B, Zhang J, Patel V, Zhong W, Hitchcock S.

ACS Med Chem Lett. 2012 Mar 29;3(11):886-91. doi: 10.1021/ml3000148. eCollection 2012 Nov 8.

14.

γ-secretase inhibitors and modulators for the treatment of Alzheimer's disease: disappointments and hopes.

Imbimbo BP, Giardina GA.

Curr Top Med Chem. 2011;11(12):1555-70. Review.

PMID:
21510832
15.

In vivo characterization of Abeta(40) changes in brain and cerebrospinal fluid using the novel gamma-secretase inhibitor N-[cis-4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexyl]-1,1,1-trifluoromethanesulfonamide (MRK-560) in the rat.

Best JD, Jay MT, Otu F, Churcher I, Reilly M, Morentin-Gutierrez P, Pattison C, Harrison T, Shearman MS, Atack JR.

J Pharmacol Exp Ther. 2006 May;317(2):786-90. Epub 2006 Jan 27.

16.

Quantification of gamma-secretase modulation differentiates inhibitor compound selectivity between two substrates Notch and amyloid precursor protein.

Yang T, Arslanova D, Gu Y, Augelli-Szafran C, Xia W.

Mol Brain. 2008 Nov 4;1:15. doi: 10.1186/1756-6606-1-15.

17.

The novel gamma secretase inhibitor N-[cis-4-[(4-chlorophenyl)sulfonyl]-4-(2,5-difluorophenyl)cyclohexyl]-1,1,1-trifluoromethanesulfonamide (MRK-560) reduces amyloid plaque deposition without evidence of notch-related pathology in the Tg2576 mouse.

Best JD, Smith DW, Reilly MA, O'Donnell R, Lewis HD, Ellis S, Wilkie N, Rosahl TW, Laroque PA, Boussiquet-Leroux C, Churcher I, Atack JR, Harrison T, Shearman MS.

J Pharmacol Exp Ther. 2007 Feb;320(2):552-8. Epub 2006 Nov 10.

18.

Studies on the pharmacokinetics and metabolism of a gamma-secretase inhibitor BMS-299897, and exploratory investigation of CYP enzyme induction.

Zheng M, Wang J, Lubinski J, Flint OP, Krishna R, Yao M, Pursley JM, Thakur A, Boulton DW, Santone KS, Barten DM, Anderson JJ, Felsenstein KM, Hansel SB.

Xenobiotica. 2009 Jul;39(7):544-55. doi: 10.1080/00498250902928555.

PMID:
19480557
19.

Neuropathological and biochemical assessments of an Alzheimer's disease patient treated with the γ-secretase inhibitor semagacestat.

Roher AE, Maarouf CL, Kokjohn TA, Whiteside CM, Kalback WM, Serrano G, Belden C, Liebsack C, Jacobson SA, Sabbagh MN, Beach TG.

Am J Neurodegener Dis. 2014 Dec 5;3(3):115-33. eCollection 2014.

20.

Therapeutic potential of gamma-secretase inhibitors and modulators.

Imbimbo BP.

Curr Top Med Chem. 2008;8(1):54-61. Review.

PMID:
18220933

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