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Items: 1 to 20 of 91

1.

Efficacy of SPI-1865, a novel gamma-secretase modulator, in multiple rodent models.

Loureiro RM, Dumin JA, McKee TD, Austin WF, Fuller NO, Hubbs JL, Shen R, Jonker J, Ives J, Bronk BS, Tate B.

Alzheimers Res Ther. 2013 Apr 18;5(2):19. doi: 10.1186/alzrt173. eCollection 2013.

2.

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.

3.

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
4.

Independent generation of Abeta42 and Abeta38 peptide species by gamma-secretase.

Czirr E, Cottrell BA, Leuchtenberger S, Kukar T, Ladd TB, Esselmann H, Paul S, Schubenel R, Torpey JW, Pietrzik CU, Golde TE, Wiltfang J, Baumann K, Koo EH, Weggen S.

J Biol Chem. 2008 Jun 20;283(25):17049-54. doi: 10.1074/jbc.M802912200. Epub 2008 Apr 21.

5.

Dynamics of Aβ42 reduction in plasma, CSF and brain of rats treated with the γ-secretase modulator, GSM-10h.

Hawkins J, Harrison DC, Ahmed S, Davis RP, Chapman T, Marshall I, Smith B, Mead TL, Medhurst A, Giblin GM, Hall A, Gonzalez MI, Richardson J, Hussain I.

Neurodegener Dis. 2011;8(6):455-64. doi: 10.1159/000324511. Epub 2011 Mar 10.

PMID:
21389687
6.

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.

7.

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
8.

The γ-Secretase Modulator, BMS-932481, Modulates Aβ Peptides in the Plasma and Cerebrospinal Fluid of Healthy Volunteers.

Soares HD, Gasior M, Toyn JH, Wang JS, Hong Q, Berisha F, Furlong MT, Raybon J, Lentz KA, Sweeney F, Zheng N, Akinsanya B, Berman RM, Thompson LA, Olson RE, Morrison J, Drexler DM, Macor JE, Albright CF, Ahlijanian MK, AbuTarif M.

J Pharmacol Exp Ther. 2016 Jul;358(1):138-50. doi: 10.1124/jpet.116.232256. Epub 2016 Apr 20.

9.

γ-Secretase modulator in Alzheimer's disease: shifting the end.

Xia W, Wong ST, Hanlon E, Morin P.

J Alzheimers Dis. 2012;31(4):685-96. doi: 10.3233/JAD-2012-120751. Review.

PMID:
22710916
11.

Chronic treatment with a novel γ-secretase modulator, JNJ-40418677, inhibits amyloid plaque formation in a mouse model of Alzheimer's disease.

Van Broeck B, Chen JM, Tréton G, Desmidt M, Hopf C, Ramsden N, Karran E, Mercken M, Rowley A.

Br J Pharmacol. 2011 May;163(2):375-89. doi: 10.1111/j.1476-5381.2011.01207.x.

12.

Amyloid beta 42 peptide (Abeta42)-lowering compounds directly bind to Abeta and interfere with amyloid precursor protein (APP) transmembrane dimerization.

Richter L, Munter LM, Ness J, Hildebrand PW, Dasari M, Unterreitmeier S, Bulic B, Beyermann M, Gust R, Reif B, Weggen S, Langosch D, Multhaup G.

Proc Natl Acad Sci U S A. 2010 Aug 17;107(33):14597-602. doi: 10.1073/pnas.1003026107. Epub 2010 Aug 2.

13.

Pharmacological characterization of the novel γ-secretase modulator AS2715348, a potential therapy for Alzheimer's disease, in rodents and nonhuman primates.

Mitani Y, Akashiba H, Saita K, Yarimizu J, Uchino H, Okabe M, Asai M, Yamasaki S, Nozawa T, Ishikawa N, Shitaka Y, Ni K, Matsuoka N.

Neuropharmacology. 2014 Apr;79:412-9. doi: 10.1016/j.neuropharm.2013.12.013. Epub 2013 Dec 25.

PMID:
24373902
14.

Discovery of novel triazolobenzazepinones as γ-secretase modulators with central Aβ42 lowering in rodents and rhesus monkeys.

Fischer C, Zultanski SL, Zhou H, Methot JL, Shah S, Hayashi I, Hughes BL, Moxham CM, Bays NW, Smotrov N, Hill AD, Pan BS, Wu Z, Moy LY, Tanga F, Kenific C, Cruz JC, Walker D, Bouthillette M, Nikov GN, Deshmukh SV, Jeliazkova-Mecheva VV, Diaz D, Michener MS, Cook JJ, Munoz B, Shearman MS.

Bioorg Med Chem Lett. 2015 Sep 1;25(17):3488-94. doi: 10.1016/j.bmcl.2015.07.003. Epub 2015 Jul 9.

PMID:
26212776
15.

First and second generation γ-secretase modulators (GSMs) modulate amyloid-β (Aβ) peptide production through different mechanisms.

Borgegard T, Juréus A, Olsson F, Rosqvist S, Sabirsh A, Rotticci D, Paulsen K, Klintenberg R, Yan H, Waldman M, Stromberg K, Nord J, Johansson J, Regner A, Parpal S, Malinowsky D, Radesater AC, Li T, Singh R, Eriksson H, Lundkvist J.

J Biol Chem. 2012 Apr 6;287(15):11810-9. doi: 10.1074/jbc.M111.305227. Epub 2012 Feb 13.

16.

Dynamics of Abeta turnover and deposition in different beta-amyloid precursor protein transgenic mouse models following gamma-secretase inhibition.

Abramowski D, Wiederhold KH, Furrer U, Jaton AL, Neuenschwander A, Runser MJ, Danner S, Reichwald J, Ammaturo D, Staab D, Stoeckli M, Rueeger H, Neumann U, Staufenbiel M.

J Pharmacol Exp Ther. 2008 Nov;327(2):411-24. doi: 10.1124/jpet.108.140327. Epub 2008 Aug 7.

17.

Therapeutic potential of gamma-secretase inhibitors and modulators.

Imbimbo BP.

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

PMID:
18220933
18.

Selective modulation of Abeta42 production in Alzheimer's disease: non-steroidal anti-inflammatory drugs and beyond.

Leuchtenberger S, Beher D, Weggen S.

Curr Pharm Des. 2006;12(33):4337-55. Review.

PMID:
17105431
19.

Discovery of a novel pharmacological and structural class of gamma secretase modulators derived from the extract of Actaea racemosa.

Findeis MA, Schroeder F, McKee TD, Yager D, Fraering PC, Creaser SP, Austin WF, Clardy J, Wang R, Selkoe D, Eckman CB.

ACS Chem Neurosci. 2012 Nov 21;3(11):941-51. doi: 10.1021/cn3000857. Epub 2012 Aug 28.

20.

Generation of Abeta38 and Abeta42 is independently and differentially affected by familial Alzheimer disease-associated presenilin mutations and gamma-secretase modulation.

Page RM, Baumann K, Tomioka M, Pérez-Revuelta BI, Fukumori A, Jacobsen H, Flohr A, Luebbers T, Ozmen L, Steiner H, Haass C.

J Biol Chem. 2008 Jan 11;283(2):677-83. Epub 2007 Oct 24.

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